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

高品質保証

文献中の引用(68)

カスタマーフィードバック(11)

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)は一種の有効なc-MetとALK阻害剤で、細胞試験でIC50値が11 nMと24 nMです。
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 MV\DfZRwfG:6aXOgRZN{[Xl? M4LTe|Q5KGh? M1fnRmROW09? M1XacmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KG2xdYPlJGJCTjNiY3XscJMh\XiycnXzd4lv\yCDTFugSlEyPzSOIH31eIFvfCClb3X4dJJme3OrbnegSW1NPCC5aYToJGlEPTBib3[gNE43OiEQvF2= MWCyNVU4OjV6OR?=
BAF3 MWjDfZRwfG:6aXOgRZN{[Xl? MnTVOFghcA>? M4DyTmROW09? NVH4THpHS3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhSkGIMzDj[YxteyCneIDy[ZN{cW6pIFHMT{BNOTF7Nl2gcZV1[W62IHPv[ZhxemW|c3nu[{BGVUx2IIfpeIghUUN3MDDv[kAzNjJizszN M3PocFIyPTd{NUi5
BAF3 NX3Ie4tKS3m2b4TvfIlkKEG|c3H5 MUG0PEBp NF6ycI1FVVOR M{jmb2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KG2xdYPlJGJCTjNiY3XscJMh\XiycnXzd4lv\yCHTVy0MWFNUyC5aYToJGlEPTBib3[gNE4zQCEQvF2= NXTDVoxPOjF3N{K1PFk>
Kelly NHj3b4FEgXSxdH;4bYMhSXO|YYm= M3HsemROW09? NHrS[JdEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBM\WyueTDj[YxteyCneIDy[ZN{cW6pIFHMT{BHOTF5NFygcZV1[W62IIfpeIghUUN3MDDv[kAxNjR{IN88US=> MV[yNVU4OjV6OR?=
SH-SY5Y NWL3PVNmS3m2b4TvfIlkKEG|c3H5 MkLkSG1UVw>? MWDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTTE1UYTW\IHPlcIx{KGW6cILld5NqdmdiQVzLJGYyOTd2TDDteZRidnRid3n0bEBKSzVyIH;mJFAvPTNizszN NIPhUWQzOTV5MkW4PS=>
SMS-KCN Ml:1R5l1d3SxeHnjJGF{e2G7 NH;DXIxFVVOR MkD2R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV21UNUuFTjDj[YxteyCneIDy[ZN{cW6pIFHMT{BTOTJ5NWGgcZV1[W62IIfpeIghUUN3MDDv[kAxNjlzIN88US=> M4[1NVIyPTd{NUi5
BAF3 MWTDfZRwfG:6aXOgRZN{[Xl? NXG0OFhMPDhiaB?= M4nZU2ROW09? M2XlVWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KG2xdYPlJGJCTjNiY3XscJMh\XiycnXzd4lv\yCWZXytRWxMKHerdHigTWM2OCCxZjCwMlE6KM7:TR?= NGfxTJozOTV5MkW4PS=>
3T3 NGDkdnZHfW6ldHnvckBCe3OjeR?= MoPNNUBp NF30cYhFVVOR NX32VpQxUW6qaXLpeIlwdiCxZjDSU24h[XO|ZYPz[YQh[XNiZ4Lve5RpKG[jY4Tvdk1qdmS3Y3XkJIF2fG:yaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIECuNFgh|ryP NWHKSWVzOjF6MUK0NVQ>
3T3-E NWrsVpJjTnWwY4Tpc44hSXO|YYm= NYLWfVRxOSCq Mlz5SG1UVw>? M131UWlvcGmkaYTpc44hd2ZiVFnFNkBie3Onc4Pl[EBoem:5dHig[oFkfG:{LXnu[JVk\WRiYYX0c5Bpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC52NEig{txO MnnoNlE5OTJ2MUS=
A549 MmHKT4lv[XOnIFHzd4F6 M1[2bFEhcA>? Ml;CSG1UVw>? M4S4PGlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiYz3NSXQhc2mwYYPlJIV5eHKnc4Pl[EBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGhITi2rbnT1Z4VlKGG3dH;wbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFAvODB6IN88US=> MnLiNlE5OTJ2MUS=
BAF3-BCL MVvGeY5kfGmxbjDBd5NigQ>? NIfXTpoyKGh? M{foVmROW09? MnnHTY5pcWKrdHnvckBw\iCDQlygZZN{\XO|ZXSgZZMh\3Kxd4ToJIZi[3Sxcj3pcoR2[2WmIHH1eI9xcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDFwMUW5JO69VQ>? NV;TW2d7OjF6MUK0NVQ>
HEK293 MXnGeY5kfGmxbjDBd5NigQ>? MVGxJIg> Ml3BSG1UVw>? NED2SnRKdmirYnn0bY9vKG:oIFHYUEBie3Onc4Pl[EBieyCpcn;3eIgh\mGldH;yMYlv\HWlZXSgZZV1d3Cqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMD6yPVQh|ryP NGO0eoszOThzMkSxOC=>
HEK293 NGjxcGFHfW6ldHnvckBCe3OjeR?= MXSxJIg> M3rMSGROW09? MV;Jcohq[mm2aX;uJI9nKEmUIHHzd4V{e2WmIHHzJIdzd3e2aDDmZYN1d3JvaX7keYNm\CCjdYTvdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAzNjh6NzFOwG0> NFL6OXgzOThzMkSxOC=>
Jurkat M{H4e2Z2dmO2aX;uJGF{e2G7 NF;EOIgyKGh? NUXX[XFkTE2VTx?= NFGx[4hKdmirYnn0bY9vKG:oIFzDT{Bie3Onc4Pl[EBieyCpcn;3eIgh\mGldH;yMYlv\HWlZXSgZZV1d3Cqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMj63OFEh|ryP NYHINXluOjF6MUK0NVQ>
KARPAS299 MlO5T4lv[XOnIFHzd4F6 M3LkcFEhcA>? M3jK[GROW09? MmPhTY5pcWKrdHnvckBw\iCDTFugZZN{\XO|ZXSgZZMh\3Kxd4ToJIZi[3Sxcj3pcoR2[2WmIHH1eI9xcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEKg{txO NYfoUYFFOjF6MUK0NVQ>
PAE NGjOSFZHfW6ldHnvckBCe3OjeR?= MX:xJIg> MYfEUXNQ M3vXXGlvcGmkaYTpc44hd2ZiVGLLRkBie3Onc4Pl[EBieyCpcn;3eIgh\mGldH;yMYlv\HWlZXSgZZV1d3Cqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMD6zPVkh|ryP MWWyNVgyOjRzNB?=
BAF3 M{nSPWZ2dmO2aX;uJGF{e2G7 NXeyOJRqOi1|IHS= M{\yNmROW09? NWfk[ZF4UW6qaXLpeIlwdiCxZjDUSWwu\nW|ZXSgbY5{fWyrbjDy[YNmeHSxcjDlfJBz\XO|ZXSge4l1cCCLQ{WwJI9nKDFwNkSzJO69VQ>? MkfVNlM4PDJ{NUK=
KARPAS299 M1\wSmN6fG:2b4jpZ{BCe3OjeR?= Ml\INk0{KGR? NIGwRoFFVVOR MUPJR|UxRTBwME[0NkDPxE1? MmrRNlM4PDJ{NUK=
EBC1 NF3YdJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XReFczKGh? MVfEUXNQ MXPJR|UxRTBwMEKzJO69VQ>? MoP4NlM6QTN|Mki=
HCT116 NUTRNWUxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnG2O|IhcA>? M1rvZWROW09? Mo\1TWM2OD1zND64NkDPxE1? NWLPR2ZJOjN7OUOzNlg>
MCF7 NXzocIFrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzlXoRWPzJiaB?= MVXEUXNQ NXfyO4NwUUN3ME25MlU5KM7:TR?= NEG2bo0zOzl7M{OyPC=>
MDA-MB-231 MlO2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\GUVczKGh? NXnFcmk6TE2VTx?= M1;rOWlEPTB;MUCuPEDPxE1? MYOyN|k6OzN{OB?=
MKN45 M4fkRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXy3cHhxPzJiaB?= M3vTU2ROW09? NHTobotKSzVyPUCuNFE{KM7:TR?= NWGyO5ZHOjN7OUOzNlg>
NCI-H441 NYfoRmtlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fESFczKGh? M4nyZ2ROW09? M3vUb2lEPTB;MUeuNlUh|ryP MmKwNlM6QTN|Mki=
NCI-H661 NFLM[GxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHERm84OiCq M1PoNmROW09? NF73RWhKSzVyPUGxMlQ4KM7:TR?= M1zLTVI{QTl|M{K4
SK-MEL-28 M1jZ[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7rRXZWPzJiaB?= MlT4SG1UVw>? MmfRTWM2OD1zMD65O{DPxE1? MUmyN|k6OzN{OB?=
SKOV3 M4CxNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLTO|IhcA>? MmKxSG1UVw>? NXvLVXFDUUN3ME2xNk45PSEQvF2= M{HKd|I{QTl|M{K4
SNU5 MnnxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LkflczKGh? NYnYTFhmTE2VTx?= MYjJR|UxRTBwMEG2JO69VQ>? Mof6NlM6QTN|Mki=
NCI-H2228 M{PPeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXH4Tog2PzJiaB?= MWrEUXNQ M4HQemlvcGmkaYTpc44hd2ZiQVzLMYZ2e2mxbjDkdol3\W5iY3XscEBxem:uaX\ldoF1cW:wIIfpeIghUUN3MDDv[kAxNjFzODFOwG0> NUjFeVdlOjR2M{K5NFk>
NCI-H3122 M1G1Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXq3NkBp M2TPU2ROW09? M2Hhe2lvcGmkaYTpc44hd2ZiQVzLMYZ2e2mxbjDkdol3\W5iY3XscEBxem:uaX\ldoF1cW:wIIfpeIghUUN3MDDv[kAxNjFyODFOwG0> NVLSU4JtOjR2M{K5NFk>
NCI-H3122 NHnjV5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXEd2x6PzJiaB?= MXrEUXNQ NVnTcGxuUW6qaXLpeIlwdiCxZjDBUGsu\nW|aX;uJIRzcX[nbjDj[YxtKHC{b3zp[oVz[XSrb36gbY4hcHWvYX6gUmNKNUh|MUKyJINmdGy|IHjhdoJwemmwZzDBUGshTzF{NknBJI12fGGwdDD3bZRpKEmFNUCgc4YhOC54MkOg{txO MVyyOFQ{OjlyOR?=
NCI-H3122 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXz0ZYJMPzJiaB?= NVTtcFh7TE2VTx?= MmTrTY5pcWKrdHnvckBw\iCDTFut[pV{cW:wIHTybZZmdiClZXzsJJBzd2yrZnXyZZRqd25iaX6gbJVu[W5iTlPJMWg{OTJ{IHPlcIx{KGijcnLvdolv\yCDTFugUFEyQT[PIH31eIFvfCC5aYToJGlEPTBib3[gNE45OzhizszN NGqxU|IzPDR|MkmwPS=>
NIH-3T3 NF7OfYhMcW6jc3WgRZN{[Xl? MoXRNUBp MkHRSG1UVw>? M1SxZmlvcGmkaYTpc44hd2ZiaIXtZY4hf2muZDD0fZBmKEWPTESt[pV{\WRiQVzLJIV5eHKnc4Pl[EBie3Onc4Pl[EBieyCyaH;zdIhwenmuYYTl[EBCVEtibHX2[Ywhf2m2aDDJR|UxKG:oIECuNFgh|ryP NFThe4IzPDR|MkmwPS=>
NIH-3T3 MoTjT4lv[XOnIFHzd4F6 MnTYNUBp M3SxW2ROW09? MnHZTY5pcWKrdHnvckBw\iCqdX3hckBGVUx2LX\1d4VlKEGOSzDHNVI3QUFibYX0ZY51KGW6cILld5Nm\CCjc4Pld5Nm\CCjczDwbI9{eGixLVHMT{Bt\X[nbDD3bZRpKEmFNUCgc4YhOC54MEWg{txO NHHJeYszPDR|MkmwPS=>
NIH-3T3 NEPVcpZMcW6jc3WgRZN{[Xl? M33lPFEhcA>? M1jVcWROW09? MYfJcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIGOxNlA3YSCvdYThcpQh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IIDoc5NxcG9vQVzLJIxmfmWuIIfpeIghUUN3MDDv[kAxNjZ{NjFOwG0> MmezNlQ1OzJ7MEm=
NIH-3T3 M1naO2tqdmG|ZTDBd5NigQ>? M2LQXFEhcA>? MVnEUXNQ NUjZWVd[UW6qaXLpeIlwdiCxZjDoeY1idiCHTVy0MYZ2e2WmIFHMT{BNOTF7Nl2gcZV1[W62IHX4dJJme3OnZDDhd5Nme3OnZDDhd{BxcG:|cHjvMWFNUyCuZY\lcEB4cXSqIFnDOVAhd2ZiMD64OFMh|ryP M1XzU|I1PDN{OUC5
NIH-3T3 Mn7zT4lv[XOnIFHzd4F6 MnTnNUBp NIrofHBFVVOR MX3Jcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIFyxNVUzWiCvdYThcpQh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IIDoc5NxcG9vQVzLJIxmfmWuIIfpeIghUUN3MDDv[kAyNjB{NjFOwG0> MmLyNlQ1OzJ7MEm=
BAF3 NXn4TZdWTnWwY4Tpc44hSXO|YYm= MUS3NkBp MkD6SG1UVw>? M3;EPWlvcGmkaYTpc44hd2ZiTmDNM2FNUyC2cnHud4Zm[3SnZDDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIIfpeIghUUN3MDDv[kAxNjB3MTFOwG0> NIrCcogzPDR4OE[zNi=>
BAF3 NWTwUlVFS3m2b4TvfIlkKEG|c3H5 M4D5N|czKGh? Mmf5SG1UVw>? M2fGW2lEPTB;MD65PEDPxE1? NYHGbpNyOjR2Nki2N|I>
NIH-3T3 MnT2T4lv[XOnIFHzd4F6 NInRSFQyKGh? Moe0TY5pcWKrdHnvckBw\iCqdX3hckBGVUx2LX\1d4VlKEGOSzDGNVE4PExibYX0ZY51KGW6cILld5Nm\CCjc4Pld5Nm\CCjczDwbI9{eGixLVHMT{Bt\X[nbDD3bZRpKEmFNUCgc4YhOC5zNkWg{txO NHHrNmkzPDhzOUGxOi=>
NIH-3T3 NGLQR3hMcW6jc3WgRZN{[Xl? MVqxJIg> MmfTTY5pcWKrdHnvckBw\iCqdX3hckBGVUx2LX\1d4VlKEGOSzDDNVE2PllibYX0ZY51KGW6cILld5Nm\CCjc4Pld5Nm\CCjczDwbI9{eGixLVHMT{Bt\X[nbDD3bZRpKEmFNUCgc4YhOC52N{ig{txO M4H1[FI1QDF7MUG2
NIH-3T3 MXjLbY5ie2ViQYPzZZk> MVqxJIg> MXHJcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIFexNlAzWiCvdYThcpQh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IIDoc5NxcG9vQVzLJIxmfmWuIIfpeIghUUN3MDDv[kAyNjF2ODFOwG0> NF;hOJgzPDhzOUGxOi=>
NIH-3T3 MX;LbY5ie2ViQYPzZZk> NFXjdogyKGh? NYTPR4VlUW6qaXLpeIlwdiCxZjDoeY1idiCHTVy0MYZ2e2WmIFHMT{AyOTVzVHnud{BufXSjboSg[ZhxemW|c3XkJIF{e2W|c3XkJIF{KHCqb4PwbI8uSUyNIHzleoVtKHerdHigTWM2OCCxZjCzMlA{QSEQvF2= MnT3NlQ5OTlzMU[=
KARPAS299 MWfLbY5ie2ViQYPzZZk> M3;mfFkxKG2rbh?= MX\EUXNQ NGXNTnJKdmirYnn0bY9vKG:oIF7QUU1nfXOnZDDBUGsheGixc4Doc5J6dGG2aX;uJIV5eHKnc4Pl[EB4cXSqIFnDOVAhd2ZiMD6xNUDPxE1? NH\tXXYzPDlyMEe1NC=>
MKN 45 MVzLbY5ie2ViQYPzZZk> NYm2SoJyOSCq MnHCSG1UVw>? MWTJcohq[mm2aX;uJI9nKGNvTXX0JJBpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5yMjFOwG0> Mn72NlQ6ODB5NUC=
A549 MonIR5l1d3SxeHnjJGF{e2G7 NF[wZnI1QCCq MonPSG1UVw>? NUK1PIk4UUN3MDDv[kA1NjB6NDFOwG0> M2mwZVI1QTByOEOw
NCI-H1975 M4rvbGN6fG:2b4jpZ{BCe3OjeR?= NEPI[3E1QCCq MXzEUXNQ M{fFc2lEPTBib3[gO{42PTFizszN Mof2NlQ6ODB6M{C=
NCI-H1993 M1vBWGN6fG:2b4jpZ{BCe3OjeR?= NWfZeVIzPDhiaB?= M{iwVmROW09? MoXUTWM2OCCxZjCwMlA3OSEQvF2= NE\iR4UzPDlyMEizNC=>
NCI-H1993 NWfIXJhrSXCxdH;zbZMhSXO|YYm= NULyRY1yOSEQvF2= NYf0ZlR6OjRiaB?= MmXrSG1UVw>? MkD6[I9meyCwb4SgbY5lfWOnIHHwc5B1d3Orcx?= MVKyOFkxODh|MB?=
NIH-3T3 MVjDfZRwfG:6aXOgRZN{[Xl? Mo\sOFghcA>? NYjFeXdHTE2VTx?= NE\2T2hKSzVyIH;mJFAvOzZ2IN88US=> M2m2b|I1QTByOEOw
EBC1 M37lPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPUO|IhcA>? NIHYdW1FVVOR MnPBTWM2OCCxZjCwMlAxPjlizszN MkfBNlQ6ODB6M{G=
KARPAS299 M1XhWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13vcFczKGh? NYDXc3o1TE2VTx?= NEHaV3FKSzVyIH;mJFAvOiEQvF2= MUOyOFkxODh|MR?=
NB1 M1fY[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTFTWM2OD17MT65PEBvVQ>? NVK2ToM{W0GQR1XS
NCI-SNU-5 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NViyWG46UUN3ME2xNFUvPzVibl2= M1rMTHNCVkeHUh?=
SR M4LUNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojuTWM2OD1zMk[uN|Ehdk1? NYL2TZNbW0GQR1XS
SF539 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTJyND6yOEBvVQ>? MnTNV2FPT0WU
SU-DHL-1 NFnFV4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LueGlEPTB;M{O2MlgzKG6P MY\TRW5ITVJ?
SCC-3 M2LJZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTN3Nj63OkBvVQ>? M3HDRXNCVkeHUh?=
DEL MoKxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLUTWM2OD1|NkmuPUBvVQ>? Mn3jV2FPT0WU
CTV-1 NF3Ic4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLTfng5UUN3ME21PVYvPDhibl2= MXnTRW5ITVJ?
EM-2 NWLrdmhUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLTTWM2OD14MEGuN|Qhdk1? NGP2fppUSU6JRWK=
MHH-CALL-2 NIPz[WZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVm4VXJtUUN3ME22PFIvPTdibl2= MY\TRW5ITVJ?
KM12 NWXQeY03T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\GemlEPTB;N{C2Mlkhdk1? M{nkNnNCVkeHUh?=
KINGS-1 MlnQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTd2OT63OUBvVQ>? M3m2SHNCVkeHUh?=
MEG-01 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY[xNWxUUUN3ME24OVcvPjZibl2= NFeze5JUSU6JRWK=
BV-173 NFPGXHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFr1[mJKSzVyPUGuNFU6QTdizszN M3jzXnNCVkeHUh?=
LAMA-84 M4nqUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDKOGJvUUN3ME2xMlM5Ojh{IN88US=> Mn3CV2FPT0WU
KARPAS-299 NVvobJZiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTFwNEC4OlEh|ryP MWPTRW5ITVJ?
K-562 M13CeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULaR3pTUUN3ME2xMlczOjZ7IN88US=> Mom4V2FPT0WU
SK-LMS-1 MoPJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zYWGlEPTB;MT63Olg3PyEQvF2= NHHzblJUSU6JRWK=
MOLT-16 NGHGdVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXKTWM2OD1zLkm1OVc2KM7:TR?= MojPV2FPT0WU
CMK MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYG3TGsyUUN3ME2xMlk3OTV7IN88US=> NWLTZm82W0GQR1XS
ST486 NH71RotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfCWXpoUUN3ME2yMlQ{ODd|IN88US=> M1;p[nNCVkeHUh?=
CI-1 NWK3UoFLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIr2OnBKSzVyPUKuOFk3PTlizszN NUHKVlJqW0GQR1XS
KP-N-RT-BM-1 NGD0[HFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MorvTWM2OD1{LkewNVIzKM7:TR?= MXrTRW5ITVJ?
ALL-PO M1HHOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3O5b2lEPTB;Mz6xPFIxPyEQvF2= M2\WOXNCVkeHUh?=
KS-1 NGSyV5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;EcmpKSzVyPUOuNlEzOjVizszN Mk\FV2FPT0WU
Becker NGPaWGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPvU2NZUUN3ME20MlI{QTNizszN M3XtZnNCVkeHUh?=
GDM-1 NHzvclNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDRTWM2OD12LkK0OlE4KM7:TR?= M4nlOHNCVkeHUh?=
BC-1 M1PVZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTRwNEmyO|ch|ryP MojTV2FPT0WU
NB14 NHfkclZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\obmZKSzVyPUSuPFM2OjRizszN M1GwVXNCVkeHUh?=
NOS-1 M2fUXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TiNWlEPTB;NT6zN|g4PCEQvF2= Ml:0V2FPT0WU
MZ1-PC MoHSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjJSnFzUUN3ME21MlgzOTVzIN88US=> NF\sTXNUSU6JRWK=
A498 MnXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XrVGlEPTB;Nj6wPFQ4OyEQvF2= M{jMcnNCVkeHUh?=
EW-16 NHnlSHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXK4[4l[UUN3ME22MlM4Pzd|IN88US=> NUnYe3Q2W0GQR1XS
NALM-6 NHPPTXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUL3e2Z[UUN3ME22MlY5Ozh5IN88US=> M{jVUXNCVkeHUh?=
EB-3 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTdwMEeyN|Mh|ryP MlHhV2FPT0WU
697 MnPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTlwMkSzNlkh|ryP MVnTRW5ITVJ?
Ramos-2G6-4C10 M3K4bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTlwNUm4OFIh|ryP NYHObpZKW0GQR1XS
KNS-81-FD NVrVOYtpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTlwNkm2OVMh|ryP M1\MTXNCVkeHUh?=
HUTU-80 NI\BeppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLFR4hKSzVyPUmuO|Q3PDJizszN M2CxcXNCVkeHUh?=
LS-411N M2Wyemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITpTmpKSzVyPUGwMlA2PjdizszN MUTTRW5ITVJ?
RPMI-8402 NVvNV3ZDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;Eb4xKSzVyPUGwMlEyPiEQvF2= M3zNT3NCVkeHUh?=
KU812 MlHZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTFyLkK5PVEh|ryP M3zoR3NCVkeHUh?=
EW-1 M3nsXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnn1TWM2OD1zMD60OFI2KM7:TR?= M4PjcHNCVkeHUh?=
HC-1 Mmi4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mme2TWM2OD1zMD60PFQ1KM7:TR?= MXPTRW5ITVJ?
NB69 NHixbYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTFyLkWwOFMh|ryP M4HxS3NCVkeHUh?=
MFH-ino NHXGW|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHTbYhKSzVyPUGwMlg{ODNizszN MVnTRW5ITVJ?
CCRF-CEM NEjFc2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrtOXNKSzVyPUGxMlU6PyEQvF2= M4\Yc3NCVkeHUh?=
SK-N-DZ NUnXTVh6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\PfohOUUN3ME2xNk4xPDN4IN88US=> MYHTRW5ITVJ?
NCI-H720 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXSwVXBTUUN3ME2xNk4yPzB3IN88US=> NYXFbXlMW0GQR1XS
HCC1187 NGTWcVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTF{LkKwOFEh|ryP MnXaV2FPT0WU
IST-SL2 NF3lT|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTF{LkS4O|Ih|ryP M4DZeXNCVkeHUh?=
KE-37 NUHOSnVqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPHSmg4UUN3ME2xNk44QTZ4IN88US=> M3rudnNCVkeHUh?=
HCC1599 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\te2lEPTB;MUKuPVA3QSEQvF2= NIj2UmlUSU6JRWK=
A4-Fuk NH7xZmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDQTWM2OD1zMj65OVg3KM7:TR?= NXn2PGZOW0GQR1XS
NKM-1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjIbmU6UUN3ME2xN{4zQTJ3IN88US=> NUC4N5h6W0GQR1XS
BE-13 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XZW2lEPTB;MUOuO|k5QSEQvF2= NIOwR4JUSU6JRWK=
MV-4-11 NUSxO|FsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrTTWM2OD1zND6wN|I1KM7:TR?= M4\CenNCVkeHUh?=
OPM-2 M2jOZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NESxNJNKSzVyPUG0MlQxQDVizszN NFvDdpVUSU6JRWK=
KARPAS-422 NUDZdmNIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm[0TWM2OD1zND61NVI3KM7:TR?= MXvTRW5ITVJ?
RPMI-8226 MkTPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LlTGlEPTB;MUSuPFkyPSEQvF2= MVHTRW5ITVJ?
KARPAS-45 NFTRb49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTF3Lke3NVYh|ryP MnLpV2FPT0WU
SK-PN-DW NEnIcmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknxTWM2OD1zNT64OlMyKM7:TR?= M2DKTHNCVkeHUh?=
LC-2 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\5UVZKSzVyPUG2MlE2ODZizszN MVHTRW5ITVJ?
NCI-H1648 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX72blQ6UUN3ME2xOk4zPTRizszN MXnTRW5ITVJ?
RL95-2 NHj3W4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTF4LkO5O|gh|ryP M1XFVnNCVkeHUh?=
KNS-42 MkHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;Ne2lEPTB;MU[uO|I4PCEQvF2= NELRVINUSU6JRWK=
RPMI-6666 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLmOppKSzVyPUG2MlkzOTFizszN MmeyV2FPT0WU
SIG-M5 NYTmVWdJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DCUWlEPTB;MUeuNVkxOyEQvF2= M4r6XnNCVkeHUh?=
VA-ES-BJ MlnCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vvS2lEPTB;MUeuO|Q2OSEQvF2= NWTkWGx{W0GQR1XS
MONO-MAC-6 NVXw[lJ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\LdJl6UUN3ME2xO{46OzF{IN88US=> MX7TRW5ITVJ?
LAN-6 NVn5fGt4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTF6Lke1OVch|ryP MYnTRW5ITVJ?
A388 NVfvW5BbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTlTWM2OD1zOT6zNFU6KM7:TR?= MUjTRW5ITVJ?
SK-NEP-1 NX7ZUXFYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7qWIxKSzVyPUKwMlIyOzJizszN NH7tUGtUSU6JRWK=
TE-10 NHj5TIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zY[2lEPTB;MkCuOVIzOSEQvF2= MXTTRW5ITVJ?
HL-60 M4PQWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;xTWM2OD1{MD65NFk6KM7:TR?= MV;TRW5ITVJ?
MC116 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTJzLkeyNlEh|ryP MkDkV2FPT0WU
SW962 NHjzXXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLMTWM2OD1{MT63PVE2KM7:TR?= M4PU[nNCVkeHUh?=
NOMO-1 NH65NGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjrTWM2OD1{Mj62OVY1KM7:TR?= NEnrSnFUSU6JRWK=
CTB-1 NF\VRlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHnR5pKSzVyPUKyMlg3PzFizszN MnOwV2FPT0WU
MRK-nu-1 M3n1U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTJ{LkmwO|Qh|ryP Mmn3V2FPT0WU
GR-ST MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTPZppRUUN3ME2yN{44PiEQvF2= MmiwV2FPT0WU
HH M{nafGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvvOYlKSzVyPUK0MlAxOyEQvF2= NXXQb3lEW0GQR1XS
NCI-H1963 NWPrOVFUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTJ2LkC3PFIh|ryP M2LwZ3NCVkeHUh?=
QIMR-WIL MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1radmlEPTB;MkSuPFc4OiEQvF2= NVThc2NIW0GQR1XS
CGTH-W-1 MmXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFS3W4xKSzVyPUK1MlA4OjNizszN MnToV2FPT0WU
LP-1 M2CxOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LFV2lEPTB;MkWuOlU2OSEQvF2= MmDZV2FPT0WU
NCI-H748 MonzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTJ4LkWxN|ch|ryP MkL4V2FPT0WU
PF-382 MkXiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVv5TpBKUUN3ME2yO{4zOjJ|IN88US=> MXXTRW5ITVJ?
ATN-1 MkWxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rPVGlEPTB;MkeuN|c{OiEQvF2= M4TpT3NCVkeHUh?=
L-540 M4TKbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3KzZWlEPTB;MkeuOlQ2QSEQvF2= MmLqV2FPT0WU
LXF-289 MkLhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4DjdWlEPTB;MkeuO|UyQSEQvF2= MYDTRW5ITVJ?
LS-513 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjJSVFKSzVyPUK4MlE5ODdizszN NXjCUWdTW0GQR1XS
NCI-H1581 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjZeZNKSzVyPUOwMlM6PzZizszN MWrTRW5ITVJ?
ES6 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjGUolnUUN3ME2zNE43QDl7IN88US=> NV3PSo1TW0GQR1XS
SW982 M1nubGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTNyLki1OlYh|ryP NIG2NJdUSU6JRWK=
DOHH-2 M{SyPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvNVoxKUUN3ME2zNU42QDl|IN88US=> M{joOXNCVkeHUh?=
DB MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTN|Lkm0N|Eh|ryP Ml:2V2FPT0WU
MPP-89 NELZeFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTN2LkG3OVYh|ryP MUfTRW5ITVJ?
LB831-BLC MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlm0TWM2OD1|ND61NVg1KM7:TR?= Ml7iV2FPT0WU
NB5 MmLtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkL1TWM2OD1|ND64OVM2KM7:TR?= M4nVZnNCVkeHUh?=
GB-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHmOmNKSzVyPUO1MlA1PjlizszN M2jvN3NCVkeHUh?=
TE-15 MmnFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHWySoRKSzVyPUO1MlIzOzhizszN NWTLcFh2W0GQR1XS
LC4-1 M3nIbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXPTWM2OD1|NT6zPFQ4KM7:TR?= MoXMV2FPT0WU
NCI-H747 M4TaRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml:5TWM2OD1|Nj6xN|Y6KM7:TR?= M2f4XHNCVkeHUh?=
NTERA-S-cl-D1 M{\ndWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\EXpp[UUN3ME2zPE44OzR5IN88US=> MVTTRW5ITVJ?
SK-MM-2 NWDrS2pVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\NcZVKSzVyPUSwMlEyPDZizszN NHPWT5FUSU6JRWK=
TGW NI\aZ4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;XWGhKSzVyPUSxMlA2PjNizszN MYPTRW5ITVJ?
ONS-76 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2f2PWlEPTB;NEKuOFg5OyEQvF2= NIfNfZlUSU6JRWK=
CPC-N MnXqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXRN2NqUUN3ME20Nk46QTdzIN88US=> NI\6[JZUSU6JRWK=
ES4 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTYTWM2OD12ND60NVU{KM7:TR?= NGfGOVZUSU6JRWK=
Daudi Mlz2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml6wTWM2OD12NT6wPFI4KM7:TR?= NHnWOIlUSU6JRWK=
MOLT-4 NYDyUG1wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFrBe|hKSzVyPUS1MlA5PTNizszN M{PYN3NCVkeHUh?=
HT-144 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3WdpNKSzVyPUS2MlczPiEQvF2= NIfXZ41USU6JRWK=
SW872 M1LPbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXJ[5VKSzVyPUS4MlE6OzNizszN MUDTRW5ITVJ?
D-283MED MoXKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPZVYlKSzVyPUS4MlM2PDJizszN MmjTV2FPT0WU
NCI-H2126 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlyyTWM2OD12OD64OFc3KM7:TR?= MmPiV2FPT0WU
NCI-SNU-16 NHX2SIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjlN3NKSzVyPUS5MlIyPDNizszN M3n0bXNCVkeHUh?=
CESS MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDhSJdKSzVyPUS5MlUxQDhizszN MnrhV2FPT0WU
A101D MoHXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fFR2lEPTB;NEmuPVc{PiEQvF2= MnPpV2FPT0WU

... 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 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 9 mg/mL (19.98 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
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 (68)

Frequently Asked Questions

  • Question 1
    Could you tell me whether this product represents the pure R-form of crizotinib, or is the the racemic Crizotinib, so a mixture of the S- and the R-form?

    Answer: Our S1068 Crizotinib is R enantiomer(except batch 05 and 06, they are racemate), and S7505 is S enantiomer.

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は一種の二重Met/Axl阻害剤で、IC50値が48 nMと10.3 nMです。

  • Erlotinib

    Erlotinibは一種のEGFR阻害剤で、このIC50値が2 nMです。Erlotinibは、EGFRに対する敏感性は人間c-Src或いはv-Abに対する敏感性より1000倍以上が高くなります。

  • R428 (BGB324)

    R428 (BGB324)は一種のAxl阻害剤で、IC50値が14 nMです。R428 (BGB324)は、Axlに作用する選択性はAblに作用する選択性より100倍以上が高くなって、MerとTyro3に作用する選択性より50倍-100倍が高くなって、InsR、EGFR、HER2とPDGFRβに作用する選択性より100倍余りが高くなります。

  • Pexidartinib (PLX3397)

    Pexidartinib (PLX3397)は一種の経口有効な多ターゲットCSF-1R、KitとFlt3受容体チロシンキナーゼ阻害剤で、IC50値が20 nM、10 nMと160 nMにそれぞれ分かれることです。臨床3期。

  • Foretinib (GSK1363089)

    Foretinib (GSK1363089)は一種のATP競争性的なHGFRとVEGFRの阻害剤です。Foretinib (GSK1363089)はMetとKDRに作用する効果が一番強くて、無細胞試験でこのIC50が0.4 nM と 0.9 nMに分かれますが、Ron、Flt-1/3/4、Kit、PDGFRα/βとTie-2に作用する効果が少し弱くて、FGFR1とEGFRに抑制活性を殆ど表しません。臨床2期。

  • Capmatinib (INCB28060)

    Capmatinib (INCB28060)は一種の新たで、ATP競争性的なc-MET阻害剤で、無細胞実験でIC50値が0.13 nMです。Capmatinib (INCB28060)はRONβ、EGFRとHER-3に活性を表しません。臨床1期。

    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)は初めの非ATP競争性的なc-Met阻害剤で、無細胞実験でKi値が0.355 μMです。Tivantinib (ARQ 197)はRonに作用する活性が殆どなくて、EGFR、InsR、PDGFRαとFGFR1/4を抑制する作用がありません。臨床3期。

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

  • PHA-665752

    PHA-665752は一種の有効で、選択性的で、ATP競争性的なc-Met阻害剤で、無細胞実験でIC50値が9 nMです。PHA-665752はc-Metに作用する選択性はRTKsとSTKsに作用する選択性より50倍以上が高くなります。

  • BMS-777607

    BMS-777607は一種のMet関連の阻害剤で、無細胞実験でc-Met、Axl、RonとTyro3に作用する時のIC50値が3.9 nM、1.1 nM、1.8 nMと4.3 nMにそれぞれ分かれることです。BMS-777607は、Met関連ターゲットに作用する選択性はLck、VEGFR-2とTrkA/Bに作用する選択性より40倍が高くなって、他の受容体と非受容体のキナーゼに作用する選択性より500倍が高くなります。臨床 1/2期。

    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