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

高品質保証

文献中の引用(65)

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 MnzqR5l1d3SxeHnjJGF{e2G7 MojpOFghcA>? M1HBVGROW09? MlnrR5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgRmFHOyClZXzsd{BmgHC{ZYPzbY5oKEGOSzDGNVE4PExibYX0ZY51KGOxZYjwdoV{e2mwZzDFUWw1KHerdHigTWM2OCCxZjCwMlYzKM7:TR?= NX\qTm1YOjF3N{K1PFk>
BAF3 NXTxVIg4S3m2b4TvfIlkKEG|c3H5 M2XUb|Q5KGh? MlLmSG1UVw>? MWjDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDCRWY{KGOnbHzzJIV5eHKnc4PpcochSUyNIFyxNVk3VSCvdYThcpQh[2:neIDy[ZN{cW6pIFXNUFQhf2m2aDDJR|UxKG:oIEKuNkDPxE1? NIXDbZgzOTV5MkW4PS=>
BAF3 NHq5c3NEgXSxdH;4bYMhSXO|YYm= MlXsOFghcA>? NXi0Oo15TE2VTx?= NHrkT|NEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBDSUZ|IHPlcIx{KGW6cILld5NqdmdiRV3MOE1CVEtid3n0bEBKSzVyIH;mJFAvOjhizszN M1\sU|IyPTd{NUi5
Kelly MVjDfZRwfG:6aXOgRZN{[Xl? MVvEUXNQ NWLLPVA4S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hU2WubImgZ4VtdHNiZYjwdoV{e2mwZzDBUGshTjFzN{TMJI12fGGwdDD3bZRpKEmFNUCgc4YhOC52MjFOwG0> NX7LW2RyOjF3N{K1PFk>
SH-SY5Y NFvs[HREgXSxdH;4bYMhSXO|YYm= M4rUNWROW09? NIr5[oxEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUUC2VWUXZJINmdGy|IHX4dJJme3OrbnegRWxMKEZzMUe0UEBufXSjboSge4l1cCCLQ{WwJI9nKDBwNUOg{txO MV6yNVU4OjV6OR?=
SMS-KCN NU\KNVlkS3m2b4TvfIlkKEG|c3H5 Mnz3SG1UVw>? MXvDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTUXMuU0OQIHPlcIx{KGW6cILld5NqdmdiQVzLJHIyOjd3UTDteZRidnRid3n0bEBKSzVyIH;mJFAvQTFizszN MX[yNVU4OjV6OR?=
BAF3 M2fzPGN6fG:2b4jpZ{BCe3OjeR?= MXy0PEBp MVTEUXNQ M1PaN2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KG2xdYPlJGJCTjNiY3XscJMh\XiycnXzd4lv\yCWZXytRWxMKHerdHigTWM2OCCxZjCwMlE6KM7:TR?= M2r6XVIyPTd{NUi5
3T3 MoD5SpVv[3Srb36gRZN{[Xl? MXmxJIg> NXT0TVNwTE2VTx?= MWLJcohq[mm2aX;uJI9nKFKRTjDhd5Nme3OnZDDhd{Boem:5dHig[oFkfG:{LXnu[JVk\WRiYYX0c5Bpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5yODFOwG0> NEPzeIYzOThzMkSxOC=>
3T3-E MYXGeY5kfGmxbjDBd5NigQ>? M162WFEhcA>? Ml2wSG1UVw>? M1fJVGlvcGmkaYTpc44hd2ZiVFnFNkBie3Onc4Pl[EBoem:5dHig[oFkfG:{LXnu[JVk\WRiYYX0c5Bpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC52NEig{txO NFKwcXczOThzMkSxOC=>
A549 MkfqT4lv[XOnIFHzd4F6 NFO3SJoyKGh? MlvCSG1UVw>? NUPHVpdwUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDjMW1GXCCtaX7hd4Uh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhUEeILXnu[JVk\WRiYYX0c5Bpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5yMEig{txO NY\BTIh2OjF6MUK0NVQ>
BAF3-BCL NYXlWGtETnWwY4Tpc44hSXO|YYm= MXqxJIg> M3fRUmROW09? NI\YOHlKdmirYnn0bY9vKG:oIFHCUEBie3Onc4Pl[EBieyCpcn;3eIgh\mGldH;yMYlv\HWlZXSgZZV1d3Cqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMT6xOVkh|ryP NFrUcYQzOThzMkSxOC=>
HEK293 MmTJSpVv[3Srb36gRZN{[Xl? NYfQdIhlOSCq NY\yWnc{TE2VTx?= NWTqNYZsUW6qaXLpeIlwdiCxZjDBXGwh[XO|ZYPz[YQh[XNiZ4Lve5RpKG[jY4Tvdk1qdmS3Y3XkJIF2fG:yaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIECuNlk1KM7:TR?= NFTOb5gzOThzMkSxOC=>
HEK293 MXHGeY5kfGmxbjDBd5NigQ>? NHfGeogyKGh? MnuzSG1UVw>? MmLHTY5pcWKrdHnvckBw\iCLUjDhd5Nme3OnZDDhd{Boem:5dHig[oFkfG:{LXnu[JVk\WRiYYX0c5Bpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOi56OEeg{txO NXHGWpBDOjF6MUK0NVQ>
Jurkat NV7kNFByTnWwY4Tpc44hSXO|YYm= MnTCNUBp MXvEUXNQ NInwR|BKdmirYnn0bY9vKG:oIFzDT{Bie3Onc4Pl[EBieyCpcn;3eIgh\mGldH;yMYlv\HWlZXSgZZV1d3Cqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMj63OFEh|ryP NXHUe3JTOjF6MUK0NVQ>
KARPAS299 NEXVXFNMcW6jc3WgRZN{[Xl? NXrZSYFQOSCq MWnEUXNQ Mn\qTY5pcWKrdHnvckBw\iCDTFugZZN{\XO|ZXSgZZMh\3Kxd4ToJIZi[3Sxcj3pcoR2[2WmIHH1eI9xcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEKg{txO M2XjSFIyQDF{NEG0
PAE MYPGeY5kfGmxbjDBd5NigQ>? MoGyNUBp NHP5UZhFVVOR Mo\oTY5pcWKrdHnvckBw\iCWUlvCJIF{e2W|c3XkJIF{KGe{b4f0bEBn[WO2b4KtbY5lfWOnZDDheZRweGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkO5PUDPxE1? MXKyNVgyOjRzNB?=
BAF3 NGiyRXpHfW6ldHnvckBCe3OjeR?= NVXicFVpOi1|IHS= MlXYSG1UVw>? NWPnUJR[UW6qaXLpeIlwdiCxZjDUSWwu\nW|ZXSgbY5{fWyrbjDy[YNmeHSxcjDlfJBz\XO|ZXSge4l1cCCLQ{WwJI9nKDFwNkSzJO69VQ>? M1S2[lI{PzR{MkWy
KARPAS299 MnTYR5l1d3SxeHnjJGF{e2G7 NGrQcFczNTNiZB?= MVPEUXNQ M2DLemlEPTB;MD6wOlQzKM7:TR?= NGHnboEzOzd2MkK1Ni=>
EBC1 NXjPR|lqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU[3NkBp Mn6xSG1UVw>? M2jYfmlEPTB;MD6wNlMh|ryP NIn6dmgzOzl7M{OyPC=>
HCT116 MoLSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTSO|IhcA>? MY\EUXNQ NGTnXotKSzVyPUG0MlgzKM7:TR?= Mk\RNlM6QTN|Mki=
MCF7 NVTKWmFqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUK3NkBp NHqxeYlFVVOR MXTJR|UxRTlwNUig{txO MXuyN|k6OzN{OB?=
MDA-MB-231 M1XxTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLJO|IhcA>? NGHpZlZFVVOR MUnJR|UxRTFyLkig{txO MlOxNlM6QTN|Mki=
MKN45 NF3pO2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXX[4Q4OiCq M{XBe2ROW09? M3nrWWlEPTB;MD6wNVMh|ryP NUf4eHZlOjN7OUOzNlg>
NCI-H441 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmr1O|IhcA>? MX7EUXNQ NX3hXIdsUUN3ME2xO{4zPSEQvF2= NGrITVUzOzl7M{OyPC=>
NCI-H661 MnzUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHrO|IhcA>? NIfHNFJFVVOR MnHQTWM2OD1zMT60O{DPxE1? M1TaVVI{QTl|M{K4
SK-MEL-28 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUCyU4lxPzJiaB?= MYTEUXNQ MoK4TWM2OD1zMD65O{DPxE1? NUHqUG1lOjN7OUOzNlg>
SKOV3 M2r4[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVq3NkBp NEPFSJpFVVOR MojtTWM2OD1zMj64OUDPxE1? NVrFOGJiOjN7OUOzNlg>
SNU5 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYe3NkBp M4TaNmROW09? Mlq4TWM2OD1yLkCxOkDPxE1? MlrXNlM6QTN|Mki=
NCI-H2228 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHnO|IhcA>? MojzSG1UVw>? MnfTTY5pcWKrdHnvckBw\iCDTFut[pV{cW:wIHTybZZmdiClZXzsJJBzd2yrZnXyZZRqd25id3n0bEBKSzVyIH;mJFAvOTF6IN88US=> M2XBclI1PDN{OUC5
NCI-H3122 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV63NkBp MmPtSG1UVw>? M{LWNGlvcGmkaYTpc44hd2ZiQVzLMYZ2e2mxbjDkdol3\W5iY3XscEBxem:uaX\ldoF1cW:wIIfpeIghUUN3MDDv[kAxNjFyODFOwG0> NGjNRmMzPDR|MkmwPS=>
NCI-H3122 M1[zV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;ZRnl5PzJiaB?= Mmr3SG1UVw>? MoT3TY5pcWKrdHnvckBw\iCDTFut[pV{cW:wIHTybZZmdiClZXzsJJBzd2yrZnXyZZRqd25iaX6gbJVu[W5iTlPJMWg{OTJ{IHPlcIx{KGijcnLvdolv\yCDTFugS|EzPjmDIH31eIFvfCC5aYToJGlEPTBib3[gNE43OjNizszN M1HUN|I1PDN{OUC5
NCI-H3122 MnLKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVO3NkBp M2PFVmROW09? M3XOPWlvcGmkaYTpc44hd2ZiQVzLMYZ2e2mxbjDkdol3\W5iY3XscEBxem:uaX\ldoF1cW:wIHnuJIh2dWGwIF7DTU1JOzF{MjDj[YxteyCqYYLic5JqdmdiQVzLJGwyOTl4TTDteZRidnRid3n0bEBKSzVyIH;mJFAvQDN6IN88US=> MoTDNlQ1OzJ7MEm=
NIH-3T3 Mo\OT4lv[XOnIFHzd4F6 NF3vVZUyKGh? MnP1SG1UVw>? MY\Jcohq[mm2aX;uJI9nKGi3bXHuJJdqdGRidInw[UBGVUx2LX\1d4VlKEGOSzDlfJBz\XO|ZXSgZZN{\XO|ZXSgZZMheGixc4Doc5J6dGG2ZXSgRWxMKGyndnXsJJdqfGhiSVO1NEBw\iByLkC4JO69VQ>? MUOyOFQ{OjlyOR?=
NIH-3T3 MXfLbY5ie2ViQYPzZZk> NF;ISosyKGh? MnjhSG1UVw>? MWfJcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIFexNlY6SSCvdYThcpQh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IIDoc5NxcG9vQVzLJIxmfmWuIIfpeIghUUN3MDDv[kAxNjZyNTFOwG0> NYe2bGR{OjR2M{K5NFk>
NIH-3T3 MXrLbY5ie2ViQYPzZZk> MYqxJIg> MX\EUXNQ NUDLXotvUW6qaXLpeIlwdiCxZjDoeY1idiCHTVy0MYZ2e2WmIFHMT{BUOTJyNmmgcZV1[W62IHX4dJJme3OnZDDhd5Nme3OnZDDhd{BxcG:|cHjvMWFNUyCuZY\lcEB4cXSqIFnDOVAhd2ZiMD62NlYh|ryP NYrk[4N7OjR2M{K5NFk>
NIH-3T3 NEnhfWJMcW6jc3WgRZN{[Xl? M120WFEhcA>? NUXpclRuTE2VTx?= MnX4TY5pcWKrdHnvckBw\iCqdX3hckBGVUx2LX\1d4VlKEGOSzDMNVE6Pk1ibYX0ZY51KGW6cILld5Nm\CCjc4Pld5Nm\CCjczDwbI9{eGixLVHMT{Bt\X[nbDD3bZRpKEmFNUCgc4YhOC56NEOg{txO NIO2SnIzPDR|MkmwPS=>
NIH-3T3 M4nGeWtqdmG|ZTDBd5NigQ>? M3\5dFEhcA>? M3f4[2ROW09? NI\nTI1KdmirYnn0bY9vKG:oIHj1cYFvKEWPTESt[pV{\WRiQVzLJGwyOTV{UjDteZRidnRiZYjwdoV{e2WmIHHzd4V{e2WmIHHzJJBpd3OyaH:tRWxMKGyndnXsJJdqfGhiSVO1NEBw\iBzLkCyOkDPxE1? MlLSNlQ1OzJ7MEm=
BAF3 M2XtOWZ2dmO2aX;uJGF{e2G7 MYm3NkBp NVXOdmg4TE2VTx?= MmXsTY5pcWKrdHnvckBw\iCQUF2vRWxMKHS{YX7z[oVkfGWmIHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25id3n0bEBKSzVyIH;mJFAvODVzIN88US=> Moq0NlQ1Pjh4M{K=
BAF3 M1zuWWN6fG:2b4jpZ{BCe3OjeR?= NHLiVVI4OiCq M2XLcGROW09? NVnBXZJHUUN3ME2wMlk5KM7:TR?= MmS2NlQ1Pjh4M{K=
NIH-3T3 NHnaNIZMcW6jc3WgRZN{[Xl? NW[1SFVyOSCq NEn0NIZKdmirYnn0bY9vKG:oIHj1cYFvKEWPTESt[pV{\WRiQVzLJGYyOTd2TDDteZRidnRiZYjwdoV{e2WmIHHzd4V{e2WmIHHzJJBpd3OyaH:tRWxMKGyndnXsJJdqfGhiSVO1NEBw\iByLkG2OUDPxE1? NHToelUzPDhzOUGxOi=>
NIH-3T3 MlLVT4lv[XOnIFHzd4F6 MnXTNUBp NEPlZ|hKdmirYnn0bY9vKG:oIHj1cYFvKEWPTESt[pV{\WRiQVzLJGMyOTV4WTDteZRidnRiZYjwdoV{e2WmIHHzd4V{e2WmIHHzJJBpd3OyaH:tRWxMKGyndnXsJJdqfGhiSVO1NEBw\iByLkS3PEDPxE1? NVjVZWt6OjR6MUmxNVY>
NIH-3T3 Mn7DT4lv[XOnIFHzd4F6 NGjncJkyKGh? M1;jUmlvcGmkaYTpc44hd2ZiaIXtZY4hTU2OND3meZNm\CCDTFugS|EzODKUIH31eIFvfCCneIDy[ZN{\WRiYYPz[ZN{\WRiYYOgdIhwe3Cqbz3BUGshdGW4ZXyge4l1cCCLQ{WwJI9nKDFwMUS4JO69VQ>? NG\0fpozPDhzOUGxOi=>
NIH-3T3 MV;LbY5ie2ViQYPzZZk> NGTQTo4yKGh? NF\wTmlKdmirYnn0bY9vKG:oIHj1cYFvKEWPTESt[pV{\WRiQVzLJFEyPTGWaX7zJI12fGGwdDDlfJBz\XO|ZXSgZZN{\XO|ZXSgZZMheGixc4Doc{1CVEtibHX2[Ywhf2m2aDDJR|UxKG:oIEOuNFM6KM7:TR?= M4nKb|I1QDF7MUG2
KARPAS299 M4PTOWtqdmG|ZTDBd5NigQ>? NEfXRVI6OCCvaX6= M{fh[mROW09? NXjTU3c5UW6qaXLpeIlwdiCxZjDOVG0u\nW|ZXSgRWxMKHCqb4PwbI9zgWyjdHnvckBmgHC{ZYPz[YQhf2m2aDDJR|UxKG:oIECuNVEh|ryP NX73e3R3OjR7MEC3OVA>
MKN 45 NX3GUpd{U2mwYYPlJGF{e2G7 MlXiNUBp NVfiXJl2TE2VTx?= MlLkTY5pcWKrdHnvckBw\iClLV3leEBxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEKg{txO MWmyOFkxODd3MB?=
A549 NW\vOVkyS3m2b4TvfIlkKEG|c3H5 MmSwOFghcA>? NXK0OVVxTE2VTx?= MkHFTWM2OCCxZjC0MlA5PCEQvF2= M1zYSlI1QTByOEOw
NCI-H1975 MWLDfZRwfG:6aXOgRZN{[Xl? M{fzO|Q5KGh? MnHuSG1UVw>? MVjJR|UxKG:oIEeuOVUyKM7:TR?= M3rzVVI1QTByOEOw
NCI-H1993 M3rGdGN6fG:2b4jpZ{BCe3OjeR?= NEHwS3o1QCCq M2jz[mROW09? MVjJR|UxKG:oIECuNFYyKM7:TR?= M3;UZVI1QTByOEOw
NCI-H1993 MYjBdI91d3OrczDBd5NigQ>? MXOxJO69VQ>? Mn3GNlQhcA>? NUnwSpJqTE2VTx?= MoCw[I9meyCwb4SgbY5lfWOnIHHwc5B1d3Orcx?= NIf1foczPDlyMEizNC=>
NIH-3T3 M1zVWmN6fG:2b4jpZ{BCe3OjeR?= Ml;LOFghcA>? NGnOS29FVVOR NHvxXHlKSzVyIH;mJFAvOzZ2IN88US=> M3zieVI1QTByOEOw
EBC1 NFrzT3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnXengyPzJiaB?= NHSyUGVFVVOR M4HvSWlEPTBib3[gNE4xODZ7IN88US=> NX3kXpRMOjR7MEC4N|E>
KARPAS299 MlXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoO2O|IhcA>? NWrrOpc3TE2VTx?= MnPuTWM2OCCxZjCwMlIh|ryP NEns[lkzPDlyMEizNS=>
NB1 NVfHO|Y4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LPc2lEPTB;OUGuPVghdk1? NYKybJllW0GQR1XS
NCI-SNU-5 NH;3SGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTFyNT63OUBvVQ>? MUnTRW5ITVJ?
SR M4O5bWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LBTmlEPTB;MUK2MlMyKG6P MoOwV2FPT0WU
SF539 MljWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVH1eGVNUUN3ME2yNFQvOjRibl2= NWniWpJvW0GQR1XS
SU-DHL-1 NHjLSJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnOTHBVUUN3ME2zN|YvQDJibl2= NHn2NmVUSU6JRWK=
SCC-3 NW\YcFlLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIX2WXFKSzVyPUO1Ok44PiCwTR?= Mk\MV2FPT0WU
DEL M3z0PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTN4OT65JI5O M2fOdXNCVkeHUh?=
CTV-1 M2T0UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2i0dmlEPTB;NUm2MlQ5KG6P NFT5eJNUSU6JRWK=
EM-2 MoLIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTZyMT6zOEBvVQ>? MVHTRW5ITVJ?
MHH-CALL-2 NF[ycI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYCzNopxUUN3ME22PFIvPTdibl2= NVPTXGFRW0GQR1XS
KM12 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDaTWM2OD15ME[uPUBvVQ>? MYDTRW5ITVJ?
KINGS-1 MkixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTd2OT63OUBvVQ>? MofLV2FPT0WU
MEG-01 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnHc3pLUUN3ME24OVcvPjZibl2= Mn:0V2FPT0WU
BV-173 M3\YTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\0WHdGUUN3ME2xMlA2QTl5IN88US=> M4DPenNCVkeHUh?=
LAMA-84 M1q4Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPoTWM2OD1zLkO4NlgzKM7:TR?= Ml;QV2FPT0WU
KARPAS-299 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHBTWM2OD1zLkSwPFYyKM7:TR?= M4DNRXNCVkeHUh?=
K-562 M{TOOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTFwN{KyOlkh|ryP M4DITnNCVkeHUh?=
SK-LMS-1 NGLPVFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfTTWM2OD1zLke2PFY4KM7:TR?= MlrCV2FPT0WU
MOLT-16 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTFwOUW1O|Uh|ryP MWPTRW5ITVJ?
CMK NFv5W3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTFwOU[xOVkh|ryP MXrTRW5ITVJ?
ST486 MnHuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHi4UWFKSzVyPUKuOFMxPzNizszN M2n5W3NCVkeHUh?=
CI-1 M4TG[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3X6V2lEPTB;Mj60PVY2QSEQvF2= M4n1VnNCVkeHUh?=
KP-N-RT-BM-1 MkfiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rWNWlEPTB;Mj63NFEzOiEQvF2= MluwV2FPT0WU
ALL-PO NVnITm5PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPvcZU5UUN3ME2zMlE5OjB5IN88US=> NUXTcHZtW0GQR1XS
KS-1 M4XUUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULyUmhkUUN3ME2zMlIyOjJ3IN88US=> MXjTRW5ITVJ?
Becker MoHYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTvTWM2OD12LkKzPVMh|ryP MkTPV2FPT0WU
GDM-1 NWjCSGtWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILrSGpKSzVyPUSuNlQ3OTdizszN NEf3N|BUSU6JRWK=
BC-1 NIjveJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17QOmlEPTB;ND60PVI4PyEQvF2= M4jlcXNCVkeHUh?=
NB14 NInzRY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV[xVoNiUUN3ME20Mlg{PTJ2IN88US=> MYjTRW5ITVJ?
NOS-1 NHf6c5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfLOZZKSzVyPUWuN|M5PzRizszN NX3MenhLW0GQR1XS
MZ1-PC MnjzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{foOGlEPTB;NT64NlE2OSEQvF2= NYPxO45IW0GQR1XS
A498 MknzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmGyTWM2OD14LkC4OFc{KM7:TR?= NHfpSI1USU6JRWK=
EW-16 MlzES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LBdmlEPTB;Nj6zO|c4OyEQvF2= Mle2V2FPT0WU
NALM-6 MlPpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXxTWM2OD14Lk[4N|g4KM7:TR?= M1H5S3NCVkeHUh?=
EB-3 MnzPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGGySlVKSzVyPUeuNFczOzNizszN NU[0dZFGW0GQR1XS
697 M4rPUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULaV4s3UUN3ME25MlI1OzJ7IN88US=> MmX6V2FPT0WU
Ramos-2G6-4C10 NXO0SoV3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrsTWM2OD17LkW5PFQzKM7:TR?= NFzFS|RUSU6JRWK=
KNS-81-FD NYTERo1kT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzPTWM2OD17Lk[5OlU{KM7:TR?= NIfySolUSU6JRWK=
HUTU-80 MojrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoT5TWM2OD17Lke0OlQzKM7:TR?= M1GzO3NCVkeHUh?=
LS-411N M33SZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTFyLkC1Olch|ryP MXPTRW5ITVJ?
RPMI-8402 M33LZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTQTWM2OD1zMD6xNVYh|ryP MoXnV2FPT0WU
KU812 M3XsVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTFyLkK5PVEh|ryP M1TRW3NCVkeHUh?=
EW-1 MoH3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33ofWlEPTB;MUCuOFQzPSEQvF2= MmfGV2FPT0WU
HC-1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXiTWM2OD1zMD60PFQ1KM7:TR?= MnHPV2FPT0WU
NB69 NGrHOHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fHemlEPTB;MUCuOVA1OyEQvF2= M1\W[nNCVkeHUh?=
MFH-ino NIThXI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fPTGlEPTB;MUCuPFMxOyEQvF2= M3HUd3NCVkeHUh?=
CCRF-CEM Mk\PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWC3flljUUN3ME2xNU42QTdizszN MY\TRW5ITVJ?
SK-N-DZ MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXmwcoZvUUN3ME2xNk4xPDN4IN88US=> NV3ZNodEW0GQR1XS
NCI-H720 NHvnSGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTF{LkG3NFUh|ryP NHrL[nFUSU6JRWK=
HCC1187 NGn4RpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nFfmlEPTB;MUKuNlA1OSEQvF2= NWL5eW0xW0GQR1XS
IST-SL2 MorqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrkPXNIUUN3ME2xNk41QDd{IN88US=> NHjtfnNUSU6JRWK=
KE-37 MlrJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTF{Lke5OlYh|ryP MnTLV2FPT0WU
HCC1599 NXmzTlZUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M162OGlEPTB;MUKuPVA3QSEQvF2= NIfrflhUSU6JRWK=
A4-Fuk MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLkbnhPUUN3ME2xNk46PTh4IN88US=> M{T3b3NCVkeHUh?=
NKM-1 MoX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\yZmlEPTB;MUOuNlkzPSEQvF2= MU\TRW5ITVJ?
BE-13 NYXIS|BsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFqxRYVKSzVyPUGzMlc6QDlizszN MnXGV2FPT0WU
MV-4-11 NGm3VIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\yTWM2OD1zND6wN|I1KM7:TR?= NYD6cmxZW0GQR1XS
OPM-2 NXW0WHpwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVOwSmZoUUN3ME2xOE41ODh3IN88US=> NVe1SYpuW0GQR1XS
KARPAS-422 NHrY[IRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3tTWM2OD1zND61NVI3KM7:TR?= M3\uZXNCVkeHUh?=
RPMI-8226 M3S5cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrOc4xKSzVyPUG0Mlg6OTVizszN MW\TRW5ITVJ?
KARPAS-45 NXLIcHZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\Rfm5LUUN3ME2xOU44PzF4IN88US=> M3ryfnNCVkeHUh?=
SK-PN-DW Moi2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDiTWM2OD1zNT64OlMyKM7:TR?= M{j4WHNCVkeHUh?=
LC-2 NUDzT2pXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\3WGlKSzVyPUG2MlE2ODZizszN MWDTRW5ITVJ?
NCI-H1648 NHzkOmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTF4LkK1OEDPxE1? MmTsV2FPT0WU
RL95-2 M4jOXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17tcmlEPTB;MU[uN|k4QCEQvF2= MlHPV2FPT0WU
KNS-42 M2rTb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M333dWlEPTB;MU[uO|I4PCEQvF2= MVnTRW5ITVJ?
RPMI-6666 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4OySWlEPTB;MU[uPVIyOSEQvF2= NVHyZVB2W0GQR1XS
SIG-M5 M1zqXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rSNmlEPTB;MUeuNVkxOyEQvF2= MVPTRW5ITVJ?
VA-ES-BJ MnTNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvTN5hKSzVyPUG3Mlc1PTFizszN MnHFV2FPT0WU
MONO-MAC-6 M1fRUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVyzfVQzUUN3ME2xO{46OzF{IN88US=> M4C3WXNCVkeHUh?=
LAN-6 M2j5Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2j5cmlEPTB;MUiuO|U2PyEQvF2= M{HvSHNCVkeHUh?=
A388 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rEemlEPTB;MUmuN|A2QSEQvF2= MkXwV2FPT0WU
SK-NEP-1 NHq3W2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTJyLkKxN|Ih|ryP NHnMdJdUSU6JRWK=
TE-10 NWm5[GZlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LScmlEPTB;MkCuOVIzOSEQvF2= MXzTRW5ITVJ?
HL-60 NX;NU4o2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3IWoY1UUN3ME2yNE46ODl7IN88US=> M{fyV3NCVkeHUh?=
MC116 Mo\lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzrPFRkUUN3ME2yNU44OjJzIN88US=> NVK0RY1LW0GQR1XS
SW962 NIGyVoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3qb2dtUUN3ME2yNU44QTF3IN88US=> Mlu1V2FPT0WU
NOMO-1 NEfLSpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTJ{Lk[1OlQh|ryP MlnUV2FPT0WU
CTB-1 M4\nRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvHT4pKSzVyPUKyMlg3PzFizszN MmroV2FPT0WU
MRK-nu-1 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF:zOmFKSzVyPUKyMlkxPzRizszN MXnTRW5ITVJ?
GR-ST M2\PZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTJ|Lke2JO69VQ>? NXnBe|BxW0GQR1XS
HH MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nHSGlEPTB;MkSuNFA{KM7:TR?= MXjTRW5ITVJ?
NCI-H1963 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzCTWM2OD1{ND6wO|gzKM7:TR?= NG\kV2ZUSU6JRWK=
QIMR-WIL MojtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjRUXBKSzVyPUK0Mlg4PzJizszN NFPVb4RUSU6JRWK=
CGTH-W-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nh[GlEPTB;MkWuNFczOyEQvF2= Mk[5V2FPT0WU
LP-1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXy5elV3UUN3ME2yOU43PTVzIN88US=> NILXUodUSU6JRWK=
NCI-H748 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTJ4LkWxN|ch|ryP Ml3wV2FPT0WU
PF-382 NVT3V5YyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DwdWlEPTB;MkeuNlIzOyEQvF2= MoXVV2FPT0WU
ATN-1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHf5NJJKSzVyPUK3MlM4OzJizszN MV\TRW5ITVJ?
L-540 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXG3VlU1UUN3ME2yO{43PDV7IN88US=> NX:xWJQ6W0GQR1XS
LXF-289 MoHHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTJ5Lke1NVkh|ryP M3iwcXNCVkeHUh?=
LS-513 NGHOZ|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnURXl7UUN3ME2yPE4yQDB5IN88US=> M37xZ3NCVkeHUh?=
NCI-H1581 NFz5Z2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HrbGlEPTB;M{CuN|k4PiEQvF2= MWLTRW5ITVJ?
ES6 M2n3WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEna[m9KSzVyPUOwMlY5QTlizszN NVvYNVd2W0GQR1XS
SW982 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjLTWM2OD1|MD64OVY3KM7:TR?= MYLTRW5ITVJ?
DOHH-2 Mn7zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjiTWM2OD1|MT61PFk{KM7:TR?= NIH3U|RUSU6JRWK=
DB NWnP[oFKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlP6TWM2OD1|Mz65OFMyKM7:TR?= M33OUnNCVkeHUh?=
MPP-89 NF;ySJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTN2LkG3OVYh|ryP M3TUVHNCVkeHUh?=
LB831-BLC M4HxSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPtbIdKSzVyPUO0MlUyQDRizszN MoDoV2FPT0WU
NB5 NFnTbGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTN2Lki1N|Uh|ryP MVjTRW5ITVJ?
GB-1 MlzCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX32VHkyUUN3ME2zOU4xPDZ7IN88US=> NGXGWmdUSU6JRWK=
TE-15 NYTqdm5TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\keohjUUN3ME2zOU4zOjN6IN88US=> Mn3sV2FPT0WU
LC4-1 NUHZcnVOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTN3LkO4OFch|ryP NIXNZnpUSU6JRWK=
NCI-H747 NELWWFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PBO2lEPTB;M{[uNVM3QSEQvF2= MkfiV2FPT0WU
NTERA-S-cl-D1 MkPwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fISGlEPTB;M{iuO|M1PyEQvF2= MXPTRW5ITVJ?
SK-MM-2 NV7pW2RjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXqXo5KSzVyPUSwMlEyPDZizszN NXvUdm1IW0GQR1XS
TGW MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\jfph5UUN3ME20NU4xPTZ|IN88US=> MlrnV2FPT0WU
ONS-76 MojES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vjeGlEPTB;NEKuOFg5OyEQvF2= NX\lZlg4W0GQR1XS
CPC-N MkjuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nxcWlEPTB;NEKuPVk4OSEQvF2= MoDGV2FPT0WU
ES4 NHfTfJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY[2dGVKUUN3ME20OE41OTV|IN88US=> M{nu[3NCVkeHUh?=
Daudi MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;JTWM2OD12NT6wPFI4KM7:TR?= NU\MR3NHW0GQR1XS
MOLT-4 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPUTI1ZUUN3ME20OU4xQDV|IN88US=> MVLTRW5ITVJ?
HT-144 Ml\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDwWJNKSzVyPUS2MlczPiEQvF2= MYXTRW5ITVJ?
SW872 M{Hkemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;XTWM2OD12OD6xPVM{KM7:TR?= M1\4T3NCVkeHUh?=
D-283MED NE\YWXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPYTGJKSzVyPUS4MlM2PDJizszN NWjmbXdWW0GQR1XS
NCI-H2126 NGLWdHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;lb4xDUUN3ME20PE45PDd4IN88US=> NYLWOI9pW0GQR1XS
NCI-SNU-16 NX36bVhNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;Od2lEPTB;NEmuNlE1OyEQvF2= NYDwNmlqW0GQR1XS
CESS NFLXPZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LINmlEPTB;NEmuOVA5QCEQvF2= MVzTRW5ITVJ?
A101D M{LqV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jBc2lEPTB;NEmuPVc{PiEQvF2= NGLGXFNUSU6JRWK=

... 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

文献中の引用 (65)

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