Crizotinib (PF-02341066) 化学構造
分子量: 450.34

高品質保証

文献中の引用(64)

カスタマーフィードバック(8)

Quality Control & MSDS

製品説明

  • Compare c-Met Inhibitors
    c-Met製品生物活性の比較
  • 研究分野
  • Combination Therapy
    併用療法
  • Crizotinib (PF-02341066)のメカニズム

製品の説明

生物活性

製品説明 Crizotinib (PF-02341066) は1種の有効な小分子の卵白の阻害剤の再編人プロテインキナーゼ、 Kiが 4 nM。
ターゲット c-Met ALK
IC50 11 nM 24 nM [1]
In vitro試験 PF-2341066 displays similar potency against c-Met phosphorylation in mIMCD3 mouse or MDCK canine epithelial cells with IC50 of 5 nM and 20 nM, respectivly. PF-2341066 shows improved or similar activity against NIH3T3 cells engineered to express c-Met ATP-binding site mutants V1092I or H1094R or the P-loop mutant M1250T with IC50 of 19 nM, 2 nM and 15 nM, respectively, compared with NIH3T3 cells expressing wild-type receptor with IC50 of 13 nM. In contrast, a marked shift in potency of PF-2341066 is observed against cells engineered to express c-Met activation loop mutants Y1230C and Y1235D with IC50 of 127 nM and 92 nM, respectively, compared with wild-type receptor. PF-2341066 also potently prevents the phosphorylation of c-Met in NCI-H69 and HOP92 cells, with IC50 of 13 nM and 16 nM, respectively, which express the endogenous c-Met variants R988C and T1010I, respectively. PF-2341066 is >1,000-fold selective for the VEGFR2 and PDGFRβ RTKs, >250-fold selective for IRK and Lck, and ∼40- to 60-fold selective for Tie2, TrkA, and TrkB, all compared with c-Met. PF-2341066 is 20- to 30-fold selective for RON and Axl RTKs. In contrast, PF-2341066 shows a near-equivalent IC50 of 24 nM against the nucleophosmin (NPM)-anaplastic lymphoma kinase (ALK) oncogenic fusion variant of the ALK RTK expressed by the KARPAS299 human anaplastic large cell lymphoma (ALCL) cell line. PF-2341066 inhibits c-Met–dependent neoplastic phenotypes of cancer cells and angiogenic phenotypes of endothelial cells. PF-2341066 suppresses human GTL-16 gastric carcinoma cell growth with IC50 of 9.7 nM. PF-2341066 induces apoptosis in GTL-16 cells with IC50 of 8.4 nM. PF-2341066 inhibits HGF-stimulated human NCI-H441 lung carcinoma cell migration and invasion with IC50 of 11 nM and 6.1 nM, respectively. PF-2341066 inhibits MDCK cell scattering with IC50 of 16 nM. PF-2341066 prevents HGF-stimulated c-Met phosphorylation, cell survival, and Matrigel invasion with IC50 of 11 nM, 14 nM and 35 nM, respectively. In addition, PF-2341066 prevents serum-stimulated HMVEC branching tubulogenesis (formation of vascular tubes) in fibrin gels. [1] PF-2341066 also potently inhibits NPM-ALK phosphorylation in Karpas299 or SU-DHL-1 ALCL cells with an IC50 of 24 nM. PF-2341066 potently prevents cell proliferation, which is associated with G(1)-S-phase cell cycle arrest and induction of apoptosis in ALK-positive ALCL cells with IC50 of 30 nM, but not ALK-negative lymphoma cells. [2] Besides, PF-2341066 prevents osteosarcoma behavior associated with primary tumor growth (i.e., proliferation and survival) as well as metastasis (eg, invasion and clonogenicity). [3]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
BAF3 MnfVR5l1d3SxeHnjJGF{e2G7 M1TsVFQ5KGh? M3LkOWROW09? NEHxPVNEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBDSUZ|IHPlcIx{KGW6cILld5NqdmdiQVzLJGYyOTd2TDDteZRidnRiY3;lfJBz\XO|aX7nJGVOVDRid3n0bEBKSzVyIH;mJFAvPjJizszN M2PwWlIyPTd{NUi5
BAF3 MVzDfZRwfG:6aXOgRZN{[Xl? NHm4cY01QCCq MUjEUXNQ M3LWeGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KG2xdYPlJGJCTjNiY3XscJMh\XiycnXzd4lv\yCDTFugUFEyQT[PIH31eIFvfCClb3X4dJJme3OrbnegSW1NPCC5aYToJGlEPTBib3[gNk4zKM7:TR?= M{e1elIyPTd{NUi5
BAF3 NW\ZSpJSS3m2b4TvfIlkKEG|c3H5 M3y1NVQ5KGh? MWrEUXNQ NG\rXIhEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBDSUZ|IHPlcIx{KGW6cILld5NqdmdiRV3MOE1CVEtid3n0bEBKSzVyIH;mJFAvOjhizszN MUiyNVU4OjV6OR?=
Kelly MY\DfZRwfG:6aXOgRZN{[Xl? NH\rV|dFVVOR M{DZPGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGtmdGy7IHPlcIx{KGW6cILld5NqdmdiQVzLJGYyOTd2TDDteZRidnRid3n0bEBKSzVyIH;mJFAvPDJizszN NVe5O2V7OjF3N{K1PFk>
SH-SY5Y MUHDfZRwfG:6aXOgRZN{[Xl? NGrCd|NFVVOR NYS3XIkyS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0hvU2m1XUBk\WyuczDlfJBz\XO|aX7nJGFNUyCIMUG3OGwhdXW2YX70JJdqfGhiSVO1NEBw\iByLkWzJO69VQ>? NF35O3IzOTV5MkW4PS=>
SMS-KCN M2PkcGN6fG:2b4jpZ{BCe3OjeR?= NGLZcFlFVVOR MoP1R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV21UNUuFTjDj[YxteyCneIDy[ZN{cW6pIFHMT{BTOTJ5NWGgcZV1[W62IIfpeIghUUN3MDDv[kAxNjlzIN88US=> NEnqVJUzOTV5MkW4PS=>
BAF3 MVnDfZRwfG:6aXOgRZN{[Xl? MYG0PEBp MlLWSG1UVw>? NE\1TpVEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBDSUZ|IHPlcIx{KGW6cILld5NqdmdiVHXsMWFNUyC5aYToJGlEPTBib3[gNE4yQSEQvF2= MV6yNVU4OjV6OR?=
3T3 NHzJbHZHfW6ldHnvckBCe3OjeR?= MYqxJIg> Mof1SG1UVw>? NWHPRY5ZUW6qaXLpeIlwdiCxZjDSU24h[XO|ZYPz[YQh[XNiZ4Lve5RpKG[jY4Tvdk1qdmS3Y3XkJIF2fG:yaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIECuNFgh|ryP NFvIclEzOThzMkSxOC=>
3T3-E MUDGeY5kfGmxbjDBd5NigQ>? NUD2S5NyOSCq NG\TSpBFVVOR MXHJcohq[mm2aX;uJI9nKFSLRUKgZZN{\XO|ZXSg[5Jwf3SqIH\hZ5Rwei2rbnT1Z4VlKGG3dH;wbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFAvPDR6IN88US=> NVPqeJdmOjF6MUK0NVQ>
A549 M3[4TmtqdmG|ZTDBd5NigQ>? NHHC[HUyKGh? M4HIT2ROW09? NXjpSIE2UW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDjMW1GXCCtaX7hd4Uh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhUEeILXnu[JVk\WRiYYX0c5Bpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5yMEig{txO MVGyNVgyOjRzNB?=
BAF3-BCL NGO0c4tHfW6ldHnvckBCe3OjeR?= NF7weXIyKGh? NWLBcpA6TE2VTx?= NIrtNZpKdmirYnn0bY9vKG:oIFHCUEBie3Onc4Pl[EBieyCpcn;3eIgh\mGldH;yMYlv\HWlZXSgZZV1d3Cqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMT6xOVkh|ryP MXuyNVgyOjRzNB?=
HEK293 M3v0b2Z2dmO2aX;uJGF{e2G7 MU[xJIg> MYrEUXNQ MmGwTY5pcWKrdHnvckBw\iCDWFygZZN{\XO|ZXSgZZMh\3Kxd4ToJIZi[3Sxcj3pcoR2[2WmIHH1eI9xcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMkm0JO69VQ>? NFjNdXozOThzMkSxOC=>
HEK293 M1zMWGZ2dmO2aX;uJGF{e2G7 MV:xJIg> NXi5S2MxTE2VTx?= NHjrR2dKdmirYnn0bY9vKG:oIFnSJIF{e2W|c3XkJIF{KGe{b4f0bEBn[WO2b4KtbY5lfWOnZDDheZRweGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iB{Lki4O{DPxE1? Mo\hNlE5OTJ2MUS=
Jurkat NVvmZ5M4TnWwY4Tpc44hSXO|YYm= M2fHNVEhcA>? NXvRW4VZTE2VTx?= MXPJcohq[mm2aX;uJI9nKEyFSzDhd5Nme3OnZDDhd{Boem:5dHig[oFkfG:{LXnu[JVk\WRiYYX0c5Bpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOi55NEGg{txO NH;4VIUzOThzMkSxOC=>
KARPAS299 NWDNcnM5U2mwYYPlJGF{e2G7 MUWxJIg> MX7EUXNQ NIjFdFNKdmirYnn0bY9vKG:oIFHMT{Bie3Onc4Pl[EBieyCpcn;3eIgh\mGldH;yMYlv\HWlZXSgZZV1d3Cqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMD6wNkDPxE1? NHH3VY4zOThzMkSxOC=>
PAE MVXGeY5kfGmxbjDBd5NigQ>? M4jMNlEhcA>? MVLEUXNQ Mki0TY5pcWKrdHnvckBw\iCWUlvCJIF{e2W|c3XkJIF{KGe{b4f0bEBn[WO2b4KtbY5lfWOnZDDheZRweGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkO5PUDPxE1? M2\QSFIyQDF{NEG0
BAF3 MXPGeY5kfGmxbjDBd5NigQ>? NGnNVnMzNTNiZB?= MWnEUXNQ MYnJcohq[mm2aX;uJI9nKFSHTD3meZNm\CCrboP1cIlvKHKnY3XweI9zKGW6cILld5Nm\CC5aYToJGlEPTBib3[gNU43PDNizszN M3LvS|I{PzR{MkWy
KARPAS299 M4PmXWN6fG:2b4jpZ{BCe3OjeR?= M3iwXFIuOyCm M1vD[WROW09? NW\oe4lxUUN3ME2wMlA3PDJizszN NIfV[2czOzd2MkK1Ni=>
EBC1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HUb|czKGh? M{noZ2ROW09? M1nwNmlEPTB;MD6wNlMh|ryP NXLlfGxjOjN7OUOzNlg>
HCT116 MkXXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTF[FB{PzJiaB?= NH\xXpJFVVOR MX;JR|UxRTF2LkiyJO69VQ>? MofZNlM6QTN|Mki=
MCF7 NFm1U2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmj0O|IhcA>? MoXmSG1UVw>? M2HlV2lEPTB;OT61PEDPxE1? NWjmV5RpOjN7OUOzNlg>
MDA-MB-231 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLDO|IhcA>? NFuzdlZFVVOR M1jkO2lEPTB;MUCuPEDPxE1? NGDMRZYzOzl7M{OyPC=>
MKN45 NWWyTllIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\3Xos4OiCq MkG0SG1UVw>? NEHUdGpKSzVyPUCuNFE{KM7:TR?= NV;DWncxOjN7OUOzNlg>
NCI-H441 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXOz[GpVPzJiaB?= M3[2W2ROW09? MYXJR|UxRTF5LkK1JO69VQ>? MYmyN|k6OzN{OB?=
NCI-H661 NXHQNJVFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LGNFczKGh? NILXTpZFVVOR M2PhfmlEPTB;MUGuOFch|ryP Ml25NlM6QTN|Mki=
SK-MEL-28 NX64TlB3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWW3NXdtPzJiaB?= NIrjb4dFVVOR NXvJU2ROUUN3ME2xNE46PyEQvF2= MV[yN|k6OzN{OB?=
SKOV3 NF3scY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;6ZZVvPzJiaB?= NVnnc2pQTE2VTx?= NUDyS3NGUUN3ME2xNk45PSEQvF2= Ml[yNlM6QTN|Mki=
SNU5 NFXMSHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnQU3M4OiCq M1\EfmROW09? MVrJR|UxRTBwMEG2JO69VQ>? MVWyN|k6OzN{OB?=
NCI-H2228 MlPPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjuUpc4OiCq NX;DVplWTE2VTx?= Mn7ETY5pcWKrdHnvckBw\iCDTFut[pV{cW:wIHTybZZmdiClZXzsJJBzd2yrZnXyZZRqd25id3n0bEBKSzVyIH;mJFAvOTF6IN88US=> M1ntNFI1PDN{OUC5
NCI-H3122 MnTPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUm3NkBp NX\6dGY1TE2VTx?= MUDJcohq[mm2aX;uJI9nKEGOSz3meZNqd25iZILpeoVvKGOnbHygdJJwdGmoZYLheIlwdiC5aYToJGlEPTBib3[gNE4yODhizszN NUTGS3l6OjR2M{K5NFk>
NCI-H3122 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWS3NkBp NHv5Z5dFVVOR MkLxTY5pcWKrdHnvckBw\iCDTFut[pV{cW:wIHTybZZmdiClZXzsJJBzd2yrZnXyZZRqd25iaX6gbJVu[W5iTlPJMWg{OTJ{IHPlcIx{KGijcnLvdolv\yCDTFugS|EzPjmDIH31eIFvfCC5aYToJGlEPTBib3[gNE43OjNizszN M1nmflI1PDN{OUC5
NCI-H3122 M1vxRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHS[llHPzJiaB?= M2L0RWROW09? NGXBb4lKdmirYnn0bY9vKG:oIFHMT{1nfXOrb36g[JJqfmWwIHPlcIwheHKxbHnm[ZJifGmxbjDpckBpfW2jbjDOR2kuUDNzMkKgZ4VtdHNiaHHyZo9zcW6pIFHMT{BNOTF7Nl2gcZV1[W62IIfpeIghUUN3MDDv[kAxNjh|ODFOwG0> NUTvcFdsOjR2M{K5NFk>
NIH-3T3 MoPPT4lv[XOnIFHzd4F6 M4LR[|EhcA>? MXrEUXNQ NH:3NWxKdmirYnn0bY9vKG:oIHj1cYFvKHerbHSgeJlx\SCHTVy0MYZ2e2WmIFHMT{BmgHC{ZYPz[YQh[XO|ZYPz[YQh[XNicHjvd5Bpd3K7bHH0[YQhSUyNIHzleoVtKHerdHigTWM2OCCxZjCwMlA5KM7:TR?= NYSz[JlvOjR2M{K5NFk>
NIH-3T3 NGPyVYpMcW6jc3WgRZN{[Xl? NEPzR4MyKGh? NH3nS3JFVVOR M3r0UWlvcGmkaYTpc44hd2ZiaIXtZY4hTU2OND3meZNm\CCDTFugS|EzPjmDIH31eIFvfCCneIDy[ZN{\WRiYYPz[ZN{\WRiYYOgdIhwe3Cqbz3BUGshdGW4ZXyge4l1cCCLQ{WwJI9nKDBwNkC1JO69VQ>? MmG3NlQ1OzJ7MEm=
NIH-3T3 MkDRT4lv[XOnIFHzd4F6 MWCxJIg> NEjMZoZFVVOR MUTJcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIGOxNlA3YSCvdYThcpQh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IIDoc5NxcG9vQVzLJIxmfmWuIIfpeIghUUN3MDDv[kAxNjZ{NjFOwG0> NGTibJQzPDR|MkmwPS=>
NIH-3T3 M13hWGtqdmG|ZTDBd5NigQ>? M4HN[VEhcA>? MYDEUXNQ MnzlTY5pcWKrdHnvckBw\iCqdX3hckBGVUx2LX\1d4VlKEGOSzDMNVE6Pk1ibYX0ZY51KGW6cILld5Nm\CCjc4Pld5Nm\CCjczDwbI9{eGixLVHMT{Bt\X[nbDD3bZRpKEmFNUCgc4YhOC56NEOg{txO NV7LUmp5OjR2M{K5NFk>
NIH-3T3 MYfLbY5ie2ViQYPzZZk> MYixJIg> MofLSG1UVw>? NUnadZBLUW6qaXLpeIlwdiCxZjDoeY1idiCHTVy0MYZ2e2WmIFHMT{BNOTF3MmKgcZV1[W62IHX4dJJme3OnZDDhd5Nme3OnZDDhd{BxcG:|cHjvMWFNUyCuZY\lcEB4cXSqIFnDOVAhd2ZiMT6wNlYh|ryP NU\5c4FLOjR2M{K5NFk>
BAF3 MlvjSpVv[3Srb36gRZN{[Xl? NELEfow4OiCq MoD1SG1UVw>? NXjyd|BbUW6qaXLpeIlwdiCxZjDOVG0wSUyNIITyZY5{\mWldHXkJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36ge4l1cCCLQ{WwJI9nKDBwMEWxJO69VQ>? Mk\VNlQ1Pjh4M{K=
BAF3 MWPDfZRwfG:6aXOgRZN{[Xl? M{XYUlczKGh? M4ftXmROW09? MUHJR|UxRTBwOUig{txO MVGyOFQ3QDZ|Mh?=
NIH-3T3 M1niZmtqdmG|ZTDBd5NigQ>? MVyxJIg> M4LTe2lvcGmkaYTpc44hd2ZiaIXtZY4hTU2OND3meZNm\CCDTFugSlEyPzSOIH31eIFvfCCneIDy[ZN{\WRiYYPz[ZN{\WRiYYOgdIhwe3Cqbz3BUGshdGW4ZXyge4l1cCCLQ{WwJI9nKDBwMU[1JO69VQ>? NUfH[ZNZOjR6MUmxNVY>
NIH-3T3 NXPw[otnU2mwYYPlJGF{e2G7 NGDVVnkyKGh? NFPPb3JKdmirYnn0bY9vKG:oIHj1cYFvKEWPTESt[pV{\WRiQVzLJGMyOTV4WTDteZRidnRiZYjwdoV{e2WmIHHzd4V{e2WmIHHzJJBpd3OyaH:tRWxMKGyndnXsJJdqfGhiSVO1NEBw\iByLkS3PEDPxE1? MoO0NlQ5OTlzMU[=
NIH-3T3 NU\pcFF4U2mwYYPlJGF{e2G7 NYXmNGxjOSCq NX;X[3lPUW6qaXLpeIlwdiCxZjDoeY1idiCHTVy0MYZ2e2WmIFHMT{BIOTJyMmKgcZV1[W62IHX4dJJme3OnZDDhd5Nme3OnZDDhd{BxcG:|cHjvMWFNUyCuZY\lcEB4cXSqIFnDOVAhd2ZiMT6xOFgh|ryP M1PIe|I1QDF7MUG2
NIH-3T3 NIPFNJhMcW6jc3WgRZN{[Xl? NUjoO5pWOSCq MXHJcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIEGxOVFVcW6|IH31eIFvfCCneIDy[ZN{\WRiYYPz[ZN{\WRiYYOgdIhwe3Cqbz3BUGshdGW4ZXyge4l1cCCLQ{WwJI9nKDNwMEO5JO69VQ>? NH;wN2UzPDhzOUGxOi=>
KARPAS299 MlL6T4lv[XOnIFHzd4F6 MWK5NEBucW5? MV\EUXNQ NITTXHVKdmirYnn0bY9vKG:oIF7QUU1nfXOnZDDBUGsheGixc4Doc5J6dGG2aX;uJIV5eHKnc4Pl[EB4cXSqIFnDOVAhd2ZiMD6xNUDPxE1? Mlv4NlQ6ODB5NUC=
MKN 45 MWDLbY5ie2ViQYPzZZk> M3:1SlEhcA>? MX\EUXNQ MnXpTY5pcWKrdHnvckBw\iClLV3leEBxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEKg{txO MUWyOFkxODd3MB?=
A549 NUnUN3BXS3m2b4TvfIlkKEG|c3H5 MkTMOFghcA>? NFnt[lFFVVOR NGjzOm9KSzVyIH;mJFQvODh2IN88US=> M4n2cVI1QTByOEOw
NCI-H1975 MmP1R5l1d3SxeHnjJGF{e2G7 MUi0PEBp Ml\TSG1UVw>? NUPCb2dvUUN3MDDv[kA4NjV3MTFOwG0> NWTsO2RiOjR7MEC4N|A>
NCI-H1993 MkLtR5l1d3SxeHnjJGF{e2G7 MVS0PEBp NXO5XnY6TE2VTx?= NV7wPI1IUUN3MDDv[kAxNjB4MTFOwG0> NUPt[IVPOjR7MEC4N|A>
NCI-H1993 Ml:yRZBwfG:|aYOgRZN{[Xl? M2XMTlEh|ryP NVTHbZlROjRiaB?= MV\EUXNQ M1[0NoRw\XNibn;0JIlv\HWlZTDhdI9xfG:|aYO= M{LMd|I1QTByOEOw
NIH-3T3 M4LJOWN6fG:2b4jpZ{BCe3OjeR?= MofUOFghcA>? MmTZSG1UVw>? NVzVVZNYUUN3MDDv[kAxNjN4NDFOwG0> NX35bHkyOjR7MEC4N|A>
EBC1 MoXkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHhXHY4OiCq M1L3fWROW09? MUXJR|UxKG:oIECuNFA3QSEQvF2= NGPRd4EzPDlyMEizNS=>
KARPAS299 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYe3NkBp NX7UWYFETE2VTx?= MXXJR|UxKG:oIECuNkDPxE1? NYXvN|M{OjR7MEC4N|E>
NB1 NVH6elRFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mof5TWM2OD17MT65PEBvVQ>? NVK2b5JUW0GQR1XS
NCI-SNU-5 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLJdIpvUUN3ME2xNFUvPzVibl2= M4jqdHNCVkeHUh?=
SR NUPMNHRST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHxNWhKSzVyPUGyOk4{OSCwTR?= NV7yeYd{W0GQR1XS
SF539 NXS4VW9nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGX1fFdKSzVyPUKwOE4zPCCwTR?= NXO0bG46W0GQR1XS
SU-DHL-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTWdYNZUUN3ME2zN|YvQDJibl2= NGH0[HRUSU6JRWK=
SCC-3 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPUTWM2OD1|NU[uO|Yhdk1? MYfTRW5ITVJ?
DEL NW[3RoFTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHWWFlKSzVyPUO2PU46KG6P NWPCT5psW0GQR1XS
CTV-1 NH3UfmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zOd2lEPTB;NUm2MlQ5KG6P MnzQV2FPT0WU
EM-2 MmruS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTZyMT6zOEBvVQ>? M3HpOHNCVkeHUh?=
MHH-CALL-2 NF23[4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTZ6Mj61O{BvVQ>? MUjTRW5ITVJ?
KM12 NHOyd3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTpTIlKSzVyPUewOk46KG6P NI\oZ4FUSU6JRWK=
KINGS-1 NHuzb5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LBfmlEPTB;N{S5Mlc2KG6P MXrTRW5ITVJ?
MEG-01 MknZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjTZ3ZKSzVyPUi1O{43PiCwTR?= NVXvXlRDW0GQR1XS
BV-173 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnvTWM2OD1zLkC1PVk4KM7:TR?= MVTTRW5ITVJ?
LAMA-84 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzFSphKSzVyPUGuN|gzQDJizszN M1XyR3NCVkeHUh?=
KARPAS-299 NFPjZ2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVrROpB6UUN3ME2xMlQxQDZzIN88US=> NFfwZW1USU6JRWK=
K-562 NWPZOol[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHqTWM2OD1zLkeyNlY6KM7:TR?= M2Hx[nNCVkeHUh?=
SK-LMS-1 Ml3BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHWbolnUUN3ME2xMlc3QDZ5IN88US=> MmPHV2FPT0WU
MOLT-16 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIC0NmNKSzVyPUGuPVU2PzVizszN MWLTRW5ITVJ?
CMK NHXYSWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTFwOU[xOVkh|ryP M4XWWHNCVkeHUh?=
ST486 MojNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTJwNEOwO|Mh|ryP M{jy[3NCVkeHUh?=
CI-1 M{jWemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jvXWlEPTB;Mj60PVY2QSEQvF2= Ml:yV2FPT0WU
KP-N-RT-BM-1 MoSwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTJwN{CxNlIh|ryP NUXUc|l6W0GQR1XS
ALL-PO NInRZpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjJTWM2OD1|LkG4NlA4KM7:TR?= M37jSnNCVkeHUh?=
KS-1 MoXiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjybYxKSzVyPUOuNlEzOjVizszN NEi4cGNUSU6JRWK=
Becker MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3mOpBxUUN3ME20MlI{QTNizszN Mk\JV2FPT0WU
GDM-1 NIL4XWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkC3TWM2OD12LkK0OlE4KM7:TR?= MVnTRW5ITVJ?
BC-1 NV7aUWVJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnS3TWM2OD12LkS5Nlc4KM7:TR?= MoPYV2FPT0WU
NB14 NXr1boJWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTRwOEO1NlQh|ryP NVL3PWFoW0GQR1XS
NOS-1 NGPZXmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fzcGlEPTB;NT6zN|g4PCEQvF2= M3G3PXNCVkeHUh?=
MZ1-PC MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTVwOEKxOVEh|ryP NF\RUpJUSU6JRWK=
A498 MoP3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXoTWM2OD14LkC4OFc{KM7:TR?= MYLTRW5ITVJ?
EW-16 MnvNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTZwM{e3O|Mh|ryP MVTTRW5ITVJ?
NALM-6 NGry[WJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTZwNkizPFch|ryP M{K2TnNCVkeHUh?=
EB-3 MmLzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\DT4ZKSzVyPUeuNFczOzNizszN MXzTRW5ITVJ?
697 M1fTU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml25TWM2OD17LkK0N|I6KM7:TR?= M1HjWnNCVkeHUh?=
Ramos-2G6-4C10 M3fDRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjGTWM2OD17LkW5PFQzKM7:TR?= NFL3eHJUSU6JRWK=
KNS-81-FD MkfrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTlwNkm2OVMh|ryP MkXDV2FPT0WU
HUTU-80 NXS5bXZqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTlwN{S2OFIh|ryP NYW2dlBRW0GQR1XS
LS-411N MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfF[WRKSzVyPUGwMlA2PjdizszN MlvSV2FPT0WU
RPMI-8402 M3Ozemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTFyLkGxOkDPxE1? MkDXV2FPT0WU
KU812 NYLzcW1PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLI[lhNUUN3ME2xNE4zQTlzIN88US=> NWDTRlZNW0GQR1XS
EW-1 Mo\oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDLeYdKSzVyPUGwMlQ1OjVizszN Moj4V2FPT0WU
HC-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jaV2lEPTB;MUCuOFg1PCEQvF2= Ml7sV2FPT0WU
NB69 M2n6WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTFyLkWwOFMh|ryP NWjHenhQW0GQR1XS
MFH-ino NInkXJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXsTmJKSzVyPUGwMlg{ODNizszN M3nPT3NCVkeHUh?=
CCRF-CEM NFj0PZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTFzLkW5O{DPxE1? MV7TRW5ITVJ?
SK-N-DZ MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjpWm5KSzVyPUGyMlA1OzZizszN NXHNWG9FW0GQR1XS
NCI-H720 NUXhXmNKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HT[mlEPTB;MUKuNVcxPSEQvF2= M2HYVHNCVkeHUh?=
HCC1187 MmPPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTF{LkKwOFEh|ryP M2i4WHNCVkeHUh?=
IST-SL2 NY[0NY53T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHDOlNuUUN3ME2xNk41QDd{IN88US=> NIXSZZdUSU6JRWK=
KE-37 NFTWWVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmT3TWM2OD1zMj63PVY3KM7:TR?= NIf1UG1USU6JRWK=
HCC1599 NIm3OWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\TUmpKSzVyPUGyMlkxPjlizszN NFTFW3VUSU6JRWK=
A4-Fuk NG\rcopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHRTWM2OD1zMj65OVg3KM7:TR?= Mn3TV2FPT0WU
NKM-1 NFzM[IpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTF|LkK5NlUh|ryP NGLvNFhUSU6JRWK=
BE-13 NXO0flZQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1qzOmlEPTB;MUOuO|k5QSEQvF2= M{nGeHNCVkeHUh?=
MV-4-11 NH\De5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXObYZ[UUN3ME2xOE4xOzJ2IN88US=> NIjsRZVUSU6JRWK=
OPM-2 NGS5UIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHSSmVVUUN3ME2xOE41ODh3IN88US=> M4XUSHNCVkeHUh?=
KARPAS-422 NYfPdVFOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXFWZdKSzVyPUG0MlUyOjZizszN Mlq3V2FPT0WU
RPMI-8226 M4PKe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvTTWM2OD1zND64PVE2KM7:TR?= MnvZV2FPT0WU
KARPAS-45 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2e4PWlEPTB;MUWuO|cyPiEQvF2= M1y3UHNCVkeHUh?=
SK-PN-DW NXjITnB5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTF3Lki2N|Eh|ryP NHLhSJZUSU6JRWK=
LC-2 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjpTWM2OD1zNj6xOVA3KM7:TR?= NFfXT2dUSU6JRWK=
NCI-H1648 Mm\rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGf4TVFKSzVyPUG2MlI2PCEQvF2= NULnOndPW0GQR1XS
RL95-2 NX3hXXM4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XQXWlEPTB;MU[uN|k4QCEQvF2= NXfW[2hPW0GQR1XS
KNS-42 M{G3bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjsZpFuUUN3ME2xOk44Ojd2IN88US=> NGfWeGNUSU6JRWK=
RPMI-6666 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYT2VVNsUUN3ME2xOk46OjFzIN88US=> M4nFWXNCVkeHUh?=
SIG-M5 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLxTWM2OD1zNz6xPVA{KM7:TR?= M3qyWXNCVkeHUh?=
VA-ES-BJ MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTF5Lke0OVEh|ryP NEfQVJpUSU6JRWK=
MONO-MAC-6 NFnmcnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTF5LkmzNVIh|ryP MUfTRW5ITVJ?
LAN-6 M2\JXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVWxPFR1UUN3ME2xPE44PTV5IN88US=> MWjTRW5ITVJ?
A388 MoLQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\ldmVbUUN3ME2xPU4{ODV7IN88US=> MXPTRW5ITVJ?
SK-NEP-1 M2TTcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH[xfWxKSzVyPUKwMlIyOzJizszN M{HtUnNCVkeHUh?=
TE-10 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTJyLkWyNlEh|ryP MXTTRW5ITVJ?
HL-60 M324Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXwfGp7UUN3ME2yNE46ODl7IN88US=> NIiwepVUSU6JRWK=
MC116 M1jH[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoD6TWM2OD1{MT63NlIyKM7:TR?= MXTTRW5ITVJ?
SW962 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvRVWZWUUN3ME2yNU44QTF3IN88US=> M1nzWXNCVkeHUh?=
NOMO-1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYm4TnU1UUN3ME2yNk43PTZ2IN88US=> NIfWW3pUSU6JRWK=
CTB-1 MlvvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zNWGlEPTB;MkKuPFY4OSEQvF2= MVfTRW5ITVJ?
MRK-nu-1 MoHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTJ{LkmwO|Qh|ryP NYfR[2VrW0GQR1XS
GR-ST NUTVfHJYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfRTWM2OD1{Mz63OkDPxE1? NXrSNnJLW0GQR1XS
HH NGnGVFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHH0[VdKSzVyPUK0MlAxOyEQvF2= NGn3OnZUSU6JRWK=
NCI-H1963 M3rHVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vpZmlEPTB;MkSuNFc5OiEQvF2= MkDGV2FPT0WU
QIMR-WIL NVHFTFZDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTJ2Lki3O|Ih|ryP MXHTRW5ITVJ?
CGTH-W-1 NXLnU25wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELKe5RKSzVyPUK1MlA4OjNizszN M3\aUXNCVkeHUh?=
LP-1 NGe0OYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH72OZpKSzVyPUK1MlY2PTFizszN MnPEV2FPT0WU
NCI-H748 M3XWWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3ZdoVNUUN3ME2yOk42OTN5IN88US=> NVLLcGNmW0GQR1XS
PF-382 NWDNUpI1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEflUmZKSzVyPUK3MlIzOjNizszN NVPmWIVjW0GQR1XS
ATN-1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUjJR|UxRTJ5LkO3N|Ih|ryP M3\WZnNCVkeHUh?=
L-540 Mk\uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\sTWM2OD1{Nz62OFU6KM7:TR?= MXLTRW5ITVJ?
LXF-289 NEK1WnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTJ5Lke1NVkh|ryP Mn61V2FPT0WU
LS-513 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFm1c5BKSzVyPUK4MlE5ODdizszN M2jZTHNCVkeHUh?=
NCI-H1581 M1G2UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDETWM2OD1|MD6zPVc3KM7:TR?= MUXTRW5ITVJ?
ES6 MnP3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzuTWM2OD1|MD62PFk6KM7:TR?= M1yye3NCVkeHUh?=
SW982 NWTUVo9ZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmW1TWM2OD1|MD64OVY3KM7:TR?= M3;FR3NCVkeHUh?=
DOHH-2 MmjaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1X4bmlEPTB;M{GuOVg6OyEQvF2= Mn24V2FPT0WU
DB Mmf0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXETWM2OD1|Mz65OFMyKM7:TR?= MnXUV2FPT0WU
MPP-89 MkPPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mkn5TWM2OD1|ND6xO|U3KM7:TR?= NIDSbpdUSU6JRWK=
LB831-BLC MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LNcGlEPTB;M{SuOVE5PCEQvF2= NVLDRplmW0GQR1XS
NB5 NFzScWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLXTWM2OD1|ND64OVM2KM7:TR?= NHnDOHhUSU6JRWK=
GB-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlW3TWM2OD1|NT6wOFY6KM7:TR?= Mn\ZV2FPT0WU
TE-15 NGPTNoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nBbGlEPTB;M{WuNlI{QCEQvF2= NYrhOGNiW0GQR1XS
LC4-1 NYr3cm5OT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIGxSndKSzVyPUO1MlM5PDdizszN M1rGWnNCVkeHUh?=
NCI-H747 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnm4TWM2OD1|Nj6xN|Y6KM7:TR?= MUXTRW5ITVJ?
NTERA-S-cl-D1 M2j2T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXT3WotHUUN3ME2zPE44OzR5IN88US=> M4PYN3NCVkeHUh?=
SK-MM-2 NHn1R5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDRcYlKSzVyPUSwMlEyPDZizszN M2\3Z3NCVkeHUh?=
TGW M2f6b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjSTWM2OD12MT6wOVY{KM7:TR?= NV32eFBWW0GQR1XS
ONS-76 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXsTWM2OD12Mj60PFg{KM7:TR?= MUjTRW5ITVJ?
CPC-N MoK2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3rPGFvUUN3ME20Nk46QTdzIN88US=> M{CzWnNCVkeHUh?=
ES4 NX:zcJhvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHvTWM2OD12ND60NVU{KM7:TR?= M2rZ[XNCVkeHUh?=
Daudi MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTR3LkC4Nlch|ryP M1XY[HNCVkeHUh?=
MOLT-4 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFHIU|hKSzVyPUS1MlA5PTNizszN NYXJOnllW0GQR1XS
HT-144 NV3iPIt6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTR4LkeyOkDPxE1? NWjNSG9KW0GQR1XS
SW872 NF3KSVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEKzUo1KSzVyPUS4MlE6OzNizszN MVjTRW5ITVJ?
D-283MED NVG5eGJuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1e0cGlEPTB;NEiuN|U1OiEQvF2= MmG4V2FPT0WU
NCI-H2126 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXflVosyUUN3ME20PE45PDd4IN88US=> NIDaT5lUSU6JRWK=
NCI-SNU-16 M2[0U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHmfJN7UUN3ME20PU4zOTR|IN88US=> M3T0XXNCVkeHUh?=
CESS NWDrU3NqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTR7LkWwPFgh|ryP MUnTRW5ITVJ?
A101D MmHlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELwN5dKSzVyPUS5Mlk4OzZizszN NHfqcIRUSU6JRWK=

... Click to View More Cell Line Experimental Data

In vivo試験 In the GTL-16 model, PF-2341066 reveals the ability to cause marked regression of large established tumors (>600 mm3) in both the 50 mg/kg/day and 75 mg/kg/day treatment cohorts, with a 60% decrease in mean tumor volume over the 43-day administration schedule. In an another study, PF-2341066 displays the ability to completely inhibits GTL-16 tumor growth for >3 months, with only 1 of 12 mice exhibiting a significant increase in tumor growth over the 3-month treatment schedule at 50 mg/kg/day. In the NCI-H441 NSCLC model, a 43% decrease in mean tumor volume is observed at 50 mg/kg/day during the 38-day PF-2341066 administration cycle. In the Caki-1 RCC model, a 53% decrease in mean tumor volume is observed to be associated with decreased volume of each tumor by at least 30% at 50 mg/kg/day during the 33-day PF-2341066 administration cycle. PF-2341066 also reveals near-complete prevention of the growth of established tumors at 50 mg/kg/day in the U87MG glioblastoma or PC-3 prostate carcinoma xenograft models, with 97% or 84% inhibition on the final study day, respectively. In contrast, PF-2341066 p.o. given at 50 mg/kg/day does not significantly inhibit tumor growth in the MDA-MB-231 breast carcinoma model, or the DLD-1 colon carcinoma model. A significant dose-dependent reduction of CD31–positive endothelial cells is observed at 12.5 mg/kg/day, 25 mg/kg/day, and 50 mg/kg/day in GTL-16 tumors, indicating that inhibition of MVD shows a dose-dependent correlation to antitumor efficacy. PF-2341066 displays a significant dose-dependent reduction of human VEGFA and IL-8 plasma levels in both the GTL-16 and U87MG models. Marked inhibition of phosphorylated c-Met, Akt, Erk, PLCλ1, and STAT5 levels is observed in GTL-16 tumors following p.o. administration of PF-2341066.[1] P.o. administration of PF-2341066 to severe combined immunodeficient-Beige mice bearing Karpas299 ALCL tumor xenografts leads to dose-dependent antitumor efficacy with complete regression of all tumors at the 100 mg/kg/d dose within 15 days of initial compound administration. In addition, inhibition of key NPM-ALK signaling mediators, including phospholipase C-gamma, signal transducers and activators of transcription 3, extracellular signal-regulated kinases, and Akt by PF-2341066 are observed at concentrations or dose levels, which correlated with inhibition of NPM-ALK phosphorylation and function.[2] PF-2341066 prevents osteosarcoma behavior associated with primary tumor growth (eg, proliferation and survival) as well as metastasis (eg, invasion and clonogenicity). In nude mice treated with PF-2341066 via oral gavage, the growth and associated osteolysis and extracortical bone matrix formation of osteosarcoma xenografts are prevented by PF-2341066.[3] Treatment of c-MET-amplified GTL-16 xenografts with 50 mg/kg PF-2341066 elicits tumor regression that is associated with a slow reduction in 18F-FDG uptake and decreases expression of the glucose transporter 1, GLUT-1.[4]
臨床試験 PF-2341066 is currently in a Phase III clinical trial in the treatment of non squamous lung cancer.
特集

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

Cellular kinase phosphorylation ELISA assays Cells are seeded in 96-well plates in media supplemented with 10% fetal bovine serum (FBS) and transferred to serum-free media [with 0.04% bovine serum albumin (BSA)] after 24 h. In experiments investigating ligand-dependent RTK phosphorylation, corresponding growth factors are added for up to 20 min. After incubation of cells with PF-2341066 for 1 h and/or appropriate ligands for the designated times, cells are washed once with HBSS supplemented with 1 mM Na3VO4, and protein lysates are generated from cells. Subsequently, phosphorylation of selected protein kinases is assessed by a sandwich ELISA method using specific capture antibodies used to coat 96-well plates and a detection antibody specific for phosphorylated tyrosine residues. Antibody-coated plates are (a) incubated in the presence of protein lysates at 4°C overnight; (b) washed seven times in 1% Tween 20 in PBS; (c) incubated in a horseradish peroxidase–conjugated anti–total-phosphotyrosine (PY-20) antibody (1:500) for 30 min; (d) washed seven times again; (e) incubated in 3,3′,5,5′-tetramethyl benzidine peroxidase substrate to initiate a colorimetric reaction that is stopped by adding 0.09 N H2SO4; and (f) measured for absorbance in 450 nm using a spectrophotometer.

細胞アッセイ: [1]

細胞株 GTL-16 gastric carcinoma cells and T47D breast carcinoma cells
濃度 0-256 nM
反応時間 1 hour
実験の流れ Cells including GTL-16 gastric carcinoma cells and T47D breast carcinoma cells are seeded in 96-well plates in media supplemented with 10% fetal bovine serum (FBS) and transferred to serum-free media [with 0.04% bovine serum albumin (BSA)] after 24 hours. In experiments investigating ligand-dependent RTK phosphorylation, corresponding growth factors are added for up to 20 minutes. After incubation of cells with PF-2341066 for 1 hour and/or appropriate ligands for the designated times, cells are washed once with HBSS supplemented with 1 mM Na3VO4, and protein lysates are generated from cells. Subsequently, phosphorylation of selected protein kinases is assessed by a sandwich ELISA method using specific capture antibodies used to coat 96-well plates and a detection antibody specific for phosphorylated tyrosine residues. Antibody-coated plates are (a) incubated in the presence of protein lysates at 4 °C overnight; (b) washed seven times in 1% Tween 20 in PBS; (c) incubated in a horseradish peroxidase–conjugated anti–total-phosphotyrosine (PY-20) antibody (1:500) for 30 min; (d) washed seven times again; (e) incubated in 3,3,5,5-tetramethyl benzidine peroxidase substrate to initiate a colorimetric reaction that is stopped by adding 0.09 N H2SO4; and (f) measured for absorbance in 450 nm using a spectrophotometer.

動物実験: [1]

動物モデル Female or male nu/nu mice bearing NCI-H441,or DLD-1, or MDA-MB-231
製剤
投薬量 12.5 mg/kg/day, 25 mg/kg/day, and 50 mg/kg/day
投与方法 Administered via p.o.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Crizotinib (PF-02341066) SDF
分子量 450.34
化学式

C21H22Cl2FN5O

CAS No. 877399-52-5
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 9 mg/mL (19.98 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo 5% DMSO+30% PEG 300+dd H2O 5mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 3-((R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine

カスタマーフィードバック (8)


Click to enlarge
Rating
Source Nat Med , 2011, 17, 1116-1120. Crizotinib (PF-02341066) purchased from Selleck
Method Western blot
Cell Lines RCT-E565 transplanted tumors
Concentrations 25 mg/kg/d, 50 mg/kg/d
Incubation Time 0-21 d
Results We then treated mice bearing RCT-E565 tumor transplants with PF02341066, a c-Met inhibitor currently in clinical development. PF02341066 abrogated both p-Akt and p-S6RP signals as well as tumor growth.

Click to enlarge
Rating
Source Cancer Cell , 2011, 19, 679–690. Crizotinib (PF-02341066) purchased from Selleck
Method Cell Growth Inhibition Assay
Cell Lines Ba/F3 cells
Concentrations
Incubation Time 48 h
Results The sensitivities of L1196M-driven Ba/F3 cell clones to PF-02341066 were lower, closely resembling that of the Ba/F3 parental cells. The therapeutic indexes of CH5424802 and PF-02341066, the IC50 ratio of EML4-ALK L1196M-driven cell clones to the parental cells, were 7- to 12-fold and 1- to 2-fold.

Click to enlarge
Rating
Source Cancer Cell , 2011, 19, 679–690. Crizotinib (PF-02341066) purchased from Selleck
Method Immunoblot analysis, Tumor growth inhibition Assay
Cell Lines xenograft models
Concentrations 100 mg/kg
Incubation Time 8 days
Results We showed that administration of CH5424802 led to significant tumor regression against both native EML4-ALK- and L1196M-driven tumors. On the other hand, PF-02341066 (100 mg/kg) resulted in no significant tumor growth inhibition against L1196M-driven tumors. Furthermore, we confirmed that phospho-STAT3, one of the downstream targets of ALK, was abolished in both tumors that were treated with CH5424802.

Click to enlarge
Rating
Source J Biomol Screen , 2011, 16, 141-154. Crizotinib (PF-02341066) purchased from Selleck
Method VimPro-Fluc-MDA-MB-231 spheroid viability, Western blot
Cell Lines MDA-MB-231 spheroids
Concentrations
Incubation Time
Results When Vimpro-Fluc downregulation reaches ≥70%, then downregulation of vimentin protein expression is more pronounced. of the modulators tested—U0126, dasatinib,axitinib, and pF2341066-all downregulated Vimpro-Fluc activity by ≥70%, which correlated with a significant down-reglation of vimentin protein expression. Finally, dose-response curves were generated with both U0126 (iC50 = 2.5 µM) and axitinib (iC50 = 0.25 µM), demonstrating that these small molecules modulate Vimpro-Fluc activity in a dose-dependent manner, indicating that their respective target(s) and signaling pathways play a significant role in maintaining vimentin expression and possibly mesenchymal homeostasis (Fig. B)

Click to enlarge
Rating
Source J Biomol Screen , 2011, 16, 141-154. Crizotinib (PF-02341066) purchased from Selleck
Method Secondary assay
Cell Lines MDA-MB-231 spheroids
Concentrations 10 µM
Incubation Time
Results U0126, pF2341066, axitinib, and pKC412 caused significant inhibition of the invasive potential of Mda-Mb-231 spheroids. Conversely, dasatinib, a potent inhibitor of vimentin gene expression, did not significantly alter the invasive potential of Mda-Mb-231 spheroids.

Click to enlarge
Rating
Source Int J Proteomics , 2011, 2011, 215496. Crizotinib (PF-02341066) purchased from Selleck
Method CEER assay
Cell Lines H1993 cell line
Concentrations 0-10 μM
Incubation Time 4 h
Results In the c-MET amplified cell line H1993, activation of this pathway was blocked by the treatment with PF-2341066, a c-MET kinase inhibitor.

Click to enlarge
Rating
Source Int J Proteomics, 2011, 2011, Article ID 215496. Crizotinib (PF-02341066) purchased from Selleck
Method Nikon inverted-phase microscope
Cell Lines lung tumor cell lines
Concentrations 0.1/1 µM
Incubation Time two weeks
Results Large colony formation of H1993 cells, whose proliferation in tissue culture was potently blocked by treatment with the c-MET kinase inhibitor PF-2341066, was also inhibited by treatment with the same inhibitor.

Click to enlarge
Rating
Source Dr. Zhang of Tianjin Medical University. Crizotinib (PF-02341066) purchased from Selleck
Method Western blot
Cell Lines MDA-MB-231 cell line
Concentrations 0-100 nM
Incubation Time
Results

文献中の引用 (64)

技術サポート&よくある質問(FAQ)

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

電話番号: +1-832-582-8158 Ext:3月曜日〜金曜日 9:00 AM–5:00 PM (米国中部標準時)

他の質問がある場合は、お気軽くお問合せください。

* 必須

Related c-Met 阻害剤

  • NPS-1034

    NPS-1034 is a dual Met/Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively.

  • Erlotinib

    Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.

  • R428 (BGB324)

    R428 (BGB324) is an inhibitor of Axl with IC50 of 14 nM, >100-fold selective for Axl versus Abl. Selectivty for Axl is also greater than Mer and Tyro3 (50-to-100- fold more selective) and InsR, EGFR, HER2, and PDGFRβ (100- fold more selective).

  • Pexidartinib (PLX3397)

    Pexidartinib (PLX3397) is an oral, potent mutil-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit, and Flt3 with IC50 of 20 nM, 10 nM and 160 nM, respectively. Phase 3.

  • Foretinib (GSK1363089)

    Foretinib (GSK1363089)は、目標が会ったATP競争的活性部位阻害剤とKDRで、IC50がそれぞれ0.4 nM と 0.9 nMです。

  • Capmatinib (INCB28060)

    Capmatinib (INCB28060)は、IC50が0.13nMによりあるc-METキナーゼの新しい、ATP競争的阻害剤です。

    Features:Inactive against RONβ, another member of the c-MET RTK family, as well as EGFR and HER-3 (members of the EGFR RTK family).

  • Tivantinib (ARQ 197)

    Tivantinib (ARQ 197)は、小説と選択的な人間のc-Met受容体型チロシンキナーゼ阻害剤で、 IC50 が0.1 μM。

    Features:The first selective c-Met inhibitor to be advanced into human clinical trials.

  • PHA-665752

    PHA-665752は、9nMのIC50による強力で、選択的で、ATP競争的c-Met阻害剤です。

  • BMS-777607

    BMS777607は分子が小さいMet関連キナーゼ阻害剤、c-Met, Axl, Ron 、Tyro3に作用する時、IC50がそれぞれ3.9nM、1.1nM、1.8nMと4.3nMになる。

    Features:A potent inhibitor of the Met family, and >40-fold selectivity vs. Lck, VEGFR2, and TrkA/B and >500-fold selective vs. other receptor and non-receptor kinases.

最近チェックしたアイテム

Tags: Crizotinib (PF-02341066)を買う | Crizotinib (PF-02341066)供給者 | Crizotinib (PF-02341066)を購入する | Crizotinib (PF-02341066)費用 | Crizotinib (PF-02341066)生産者 | オーダーCrizotinib (PF-02341066) | Crizotinib (PF-02341066)代理店
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
お問い合わせ