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

高品質保証

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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 NWThfIlmS3m2b4TvfIlkKEG|c3H5 M2\CT|Q5KGh? MWjEUXNQ MkHvR5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgRmFHOyClZXzsd{BmgHC{ZYPzbY5oKEGOSzDGNVE4PExibYX0ZY51KGOxZYjwdoV{e2mwZzDFUWw1KHerdHigTWM2OCCxZjCwMlYzKM7:TR?= NIDifZkzOTV5MkW4PS=>
BAF3 M3XJ[2N6fG:2b4jpZ{BCe3OjeR?= M2X5fFQ5KGh? MXPEUXNQ Mlq4R5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgRmFHOyClZXzsd{BmgHC{ZYPzbY5oKEGOSzDMNVE6Pk1ibYX0ZY51KGOxZYjwdoV{e2mwZzDFUWw1KHerdHigTWM2OCCxZjCyMlIh|ryP M1j1[|IyPTd{NUi5
BAF3 NWHuUGZyS3m2b4TvfIlkKEG|c3H5 M3L5N|Q5KGh? NW\OO2JsTE2VTx?= M36y[WN6fG:2b4jpZ4l1gSCjZ3HpcpN1KG2xdYPlJGJCTjNiY3XscJMh\XiycnXzd4lv\yCHTVy0MWFNUyC5aYToJGlEPTBib3[gNE4zQCEQvF2= MoDFNlE2PzJ3OEm=
Kelly NGDFdJVEgXSxdH;4bYMhSXO|YYm= MnXtSG1UVw>? Mn;TR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gT4VtdHliY3XscJMh\XiycnXzd4lv\yCDTFugSlEyPzSOIH31eIFvfCC5aYToJGlEPTBib3[gNE41OiEQvF2= M2GzOlIyPTd{NUi5
SH-SY5Y M3TNZWN6fG:2b4jpZ{BCe3OjeR?= NEm0bpdFVVOR NHThW25EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUUC2VWUXZJINmdGy|IHX4dJJme3OrbnegRWxMKEZzMUe0UEBufXSjboSge4l1cCCLQ{WwJI9nKDBwNUOg{txO NXzD[YJoOjF3N{K1PFk>
SMS-KCN Mlv4R5l1d3SxeHnjJGF{e2G7 NIX0bGhFVVOR NF3NNGhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUVVNvS1POJINmdGy|IHX4dJJme3OrbnegRWxMKFJzMke1VUBufXSjboSge4l1cCCLQ{WwJI9nKDBwOUGg{txO M{PTXFIyPTd{NUi5
BAF3 NIfFfYxEgXSxdH;4bYMhSXO|YYm= M1vjSVQ5KGh? MVPEUXNQ MUHDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDCRWY{KGOnbHzzJIV5eHKnc4PpcochXGWuLVHMT{B4cXSqIFnDOVAhd2ZiMD6xPUDPxE1? Mk\aNlE2PzJ3OEm=
3T3 NXmxZpZITnWwY4Tpc44hSXO|YYm= MlrtNUBp MYrEUXNQ NXK5UXJNUW6qaXLpeIlwdiCxZjDSU24h[XO|ZYPz[YQh[XNiZ4Lve5RpKG[jY4Tvdk1qdmS3Y3XkJIF2fG:yaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIECuNFgh|ryP MlfFNlE5OTJ2MUS=
3T3-E Mly3SpVv[3Srb36gRZN{[Xl? NGLsRmEyKGh? M3zIRmROW09? NGDLXG5KdmirYnn0bY9vKG:oIGTJSVIh[XO|ZYPz[YQh\3Kxd4ToJIZi[3Sxcj3pcoR2[2WmIHH1eI9xcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwNES4JO69VQ>? MmrFNlE5OTJ2MUS=
A549 M37JSmtqdmG|ZTDBd5NigQ>? MYqxJIg> M3TmNmROW09? MWDJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KGNvTVXUJItqdmG|ZTDlfJBz\XO|ZXSgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDIS2YucW6mdXPl[EBifXSxcHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCwMlAxQCEQvF2= MmTCNlE5OTJ2MUS=
BAF3-BCL MnfkSpVv[3Srb36gRZN{[Xl? M3ixWVEhcA>? MVHEUXNQ MX3Jcohq[mm2aX;uJI9nKEGETDDhd5Nme3OnZDDhd{Boem:5dHig[oFkfG:{LXnu[JVk\WRiYYX0c5Bpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOS5zNUmg{txO Mlv2NlE5OTJ2MUS=
HEK293 NIrmTYlHfW6ldHnvckBCe3OjeR?= Mn23NUBp MV3EUXNQ MlHXTY5pcWKrdHnvckBw\iCDWFygZZN{\XO|ZXSgZZMh\3Kxd4ToJIZi[3Sxcj3pcoR2[2WmIHH1eI9xcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMkm0JO69VQ>? NYrFXmFSOjF6MUK0NVQ>
HEK293 MXTGeY5kfGmxbjDBd5NigQ>? NX;LZ2dSOSCq M362[GROW09? NGjMdllKdmirYnn0bY9vKG:oIFnSJIF{e2W|c3XkJIF{KGe{b4f0bEBn[WO2b4KtbY5lfWOnZDDheZRweGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iB{Lki4O{DPxE1? NYPGOFhYOjF6MUK0NVQ>
Jurkat MXrGeY5kfGmxbjDBd5NigQ>? MV:xJIg> NGrpTmVFVVOR M{e5PWlvcGmkaYTpc44hd2ZiTFPLJIF{e2W|c3XkJIF{KGe{b4f0bEBn[WO2b4KtbY5lfWOnZDDheZRweGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iB{Lke0NUDPxE1? NXP6dnZpOjF6MUK0NVQ>
KARPAS299 NHrO[mtMcW6jc3WgRZN{[Xl? NUXnWlhPOSCq NXrEOZViTE2VTx?= MV7Jcohq[mm2aX;uJI9nKEGOSzDhd5Nme3OnZDDhd{Boem:5dHig[oFkfG:{LXnu[JVk\WRiYYX0c5Bpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5yMjFOwG0> Mn;VNlE5OTJ2MUS=
PAE NE\JXZBHfW6ldHnvckBCe3OjeR?= MVuxJIg> MX3EUXNQ M1nVZ2lvcGmkaYTpc44hd2ZiVGLLRkBie3Onc4Pl[EBieyCpcn;3eIgh\mGldH;yMYlv\HWlZXSgZZV1d3Cqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMD6zPVkh|ryP MUGyNVgyOjRzNB?=
BAF3 MkW2SpVv[3Srb36gRZN{[Xl? MYWyMVMh\A>? MWHEUXNQ MWLJcohq[mm2aX;uJI9nKFSHTD3meZNm\CCrboP1cIlvKHKnY3XweI9zKGW6cILld5Nm\CC5aYToJGlEPTBib3[gNU43PDNizszN MVmyN|c1OjJ3Mh?=
KARPAS299 NEKyTpJEgXSxdH;4bYMhSXO|YYm= MkPUNk0{KGR? M{PGOmROW09? NXzw[2t5UUN3ME2wMlA3PDJizszN MVOyN|c1OjJ3Mh?=
EBC1 M2nvV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVi3NkBp NV;ubHdCTE2VTx?= MmjDTWM2OD1yLkCyN{DPxE1? NEj1T4kzOzl7M{OyPC=>
HCT116 NUnqXpRsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnj0O|IhcA>? NGDlfJdFVVOR MlzjTWM2OD1zND64NkDPxE1? NVnIXVFCOjN7OUOzNlg>
MCF7 NEnTfIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVn0R5psPzJiaB?= NF\ZfGdFVVOR NEPEU2JKSzVyPUmuOVgh|ryP NGDoSZIzOzl7M{OyPC=>
MDA-MB-231 NIrqOphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\JO|IhcA>? MkPhSG1UVw>? NInRZpFKSzVyPUGwMlgh|ryP NGfGW4QzOzl7M{OyPC=>
MKN45 NXvkTXFoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE[2S4E4OiCq NEHYVphFVVOR MXHJR|UxRTBwMEGzJO69VQ>? Mlf0NlM6QTN|Mki=
NCI-H441 NEGwXZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW[3NkBp M2fx[2ROW09? MWrJR|UxRTF5LkK1JO69VQ>? MX2yN|k6OzN{OB?=
NCI-H661 NH3QVZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYG3NkBp M{XsV2ROW09? NVnDfJE5UUN3ME2xNU41PyEQvF2= NH\rS|UzOzl7M{OyPC=>
SK-MEL-28 MnzNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13pXVczKGh? NXfEe5RnTE2VTx?= M2[wU2lEPTB;MUCuPVch|ryP MX6yN|k6OzN{OB?=
SKOV3 NEP2bW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvRSFNrPzJiaB?= NH22d2pFVVOR MlrkTWM2OD1zMj64OUDPxE1? Mlz0NlM6QTN|Mki=
SNU5 MlHVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV63NkBp M2D3W2ROW09? MXvJR|UxRTBwMEG2JO69VQ>? NUHQWZpiOjN7OUOzNlg>
NCI-H2228 NVjDN29IT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXG3NkBp NGP2OVBFVVOR NGr1TGFKdmirYnn0bY9vKG:oIFHMT{1nfXOrb36g[JJqfmWwIHPlcIwheHKxbHnm[ZJifGmxbjD3bZRpKEmFNUCgc4YhOC5zMUig{txO NIfrXGozPDR|MkmwPS=>
NCI-H3122 MkXqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWC3PZo3PzJiaB?= NHyxdoZFVVOR NGTwUm9KdmirYnn0bY9vKG:oIFHMT{1nfXOrb36g[JJqfmWwIHPlcIwheHKxbHnm[ZJifGmxbjD3bZRpKEmFNUCgc4YhOC5zMEig{txO NFLjR2szPDR|MkmwPS=>
NCI-H3122 Ml6xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHr2T3g4OiCq MlSySG1UVw>? MYjJcohq[mm2aX;uJI9nKEGOSz3meZNqd25iZILpeoVvKGOnbHygdJJwdGmoZYLheIlwdiCrbjDoeY1idiCQQ1mtTFMyOjJiY3XscJMhcGG{Yn;ybY5oKEGOSzDHNVI3QUFibYX0ZY51KHerdHigTWM2OCCxZjCwMlYzOyEQvF2= M3[4[lI1PDN{OUC5
NCI-H3122 M1z5TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTpbHlYPzJiaB?= MWDEUXNQ NUDEOJN3UW6qaXLpeIlwdiCxZjDBUGsu\nW|aX;uJIRzcX[nbjDj[YxtKHC{b3zp[oVz[XSrb36gbY4hcHWvYX6gUmNKNUh|MUKyJINmdGy|IHjhdoJwemmwZzDBUGshVDFzOU\NJI12fGGwdDD3bZRpKEmFNUCgc4YhOC56M{ig{txO NGniTmgzPDR|MkmwPS=>
NIH-3T3 NUTsb29lU2mwYYPlJGF{e2G7 M37OUVEhcA>? M1rJ[mROW09? M3Xu[2lvcGmkaYTpc44hd2ZiaIXtZY4hf2muZDD0fZBmKEWPTESt[pV{\WRiQVzLJIV5eHKnc4Pl[EBie3Onc4Pl[EBieyCyaH;zdIhwenmuYYTl[EBCVEtibHX2[Ywhf2m2aDDJR|UxKG:oIECuNFgh|ryP M{XIUVI1PDN{OUC5
NIH-3T3 MULLbY5ie2ViQYPzZZk> NEPwVHAyKGh? NETU[nFFVVOR NXviNFhtUW6qaXLpeIlwdiCxZjDoeY1idiCHTVy0MYZ2e2WmIFHMT{BIOTJ4OVGgcZV1[W62IHX4dJJme3OnZDDhd5Nme3OnZDDhd{BxcG:|cHjvMWFNUyCuZY\lcEB4cXSqIFnDOVAhd2ZiMD62NFUh|ryP MknlNlQ1OzJ7MEm=
NIH-3T3 M{K5V2tqdmG|ZTDBd5NigQ>? NFjuT5EyKGh? Mln2SG1UVw>? MX\Jcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIGOxNlA3YSCvdYThcpQh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IIDoc5NxcG9vQVzLJIxmfmWuIIfpeIghUUN3MDDv[kAxNjZ{NjFOwG0> NFfBOHAzPDR|MkmwPS=>
NIH-3T3 MVrLbY5ie2ViQYPzZZk> NXnaSWt[OSCq M3jab2ROW09? MmHaTY5pcWKrdHnvckBw\iCqdX3hckBGVUx2LX\1d4VlKEGOSzDMNVE6Pk1ibYX0ZY51KGW6cILld5Nm\CCjc4Pld5Nm\CCjczDwbI9{eGixLVHMT{Bt\X[nbDD3bZRpKEmFNUCgc4YhOC56NEOg{txO NXu2PVA5OjR2M{K5NFk>
NIH-3T3 NEPHe5lMcW6jc3WgRZN{[Xl? MX2xJIg> NI[wfJhFVVOR MkHUTY5pcWKrdHnvckBw\iCqdX3hckBGVUx2LX\1d4VlKEGOSzDMNVE2OlJibYX0ZY51KGW6cILld5Nm\CCjc4Pld5Nm\CCjczDwbI9{eGixLVHMT{Bt\X[nbDD3bZRpKEmFNUCgc4YhOS5yMk[g{txO NInNT|AzPDR|MkmwPS=>
BAF3 M2[wWGZ2dmO2aX;uJGF{e2G7 MoP4O|IhcA>? NHS2R5BFVVOR NXLnXotIUW6qaXLpeIlwdiCxZjDOVG0wSUyNIITyZY5{\mWldHXkJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36ge4l1cCCLQ{WwJI9nKDBwMEWxJO69VQ>? MVeyOFQ3QDZ|Mh?=
BAF3 MX3DfZRwfG:6aXOgRZN{[Xl? NXL2SGhkPzJiaB?= NFXiNZZFVVOR NIXBbnNKSzVyPUCuPVgh|ryP NWDycm5LOjR2Nki2N|I>
NIH-3T3 NWTYSlhqU2mwYYPlJGF{e2G7 NYnOfmVsOSCq MoC4TY5pcWKrdHnvckBw\iCqdX3hckBGVUx2LX\1d4VlKEGOSzDGNVE4PExibYX0ZY51KGW6cILld5Nm\CCjc4Pld5Nm\CCjczDwbI9{eGixLVHMT{Bt\X[nbDD3bZRpKEmFNUCgc4YhOC5zNkWg{txO M{eyNVI1QDF7MUG2
NIH-3T3 MW\LbY5ie2ViQYPzZZk> NWLYZoc{OSCq M2rEcWlvcGmkaYTpc44hd2ZiaIXtZY4hTU2OND3meZNm\CCDTFugR|EyPT[\IH31eIFvfCCneIDy[ZN{\WRiYYPz[ZN{\WRiYYOgdIhwe3Cqbz3BUGshdGW4ZXyge4l1cCCLQ{WwJI9nKDBwNEe4JO69VQ>? M3\1PVI1QDF7MUG2
NIH-3T3 MVjLbY5ie2ViQYPzZZk> Ml7aNUBp MYHJcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIFexNlAzWiCvdYThcpQh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IIDoc5NxcG9vQVzLJIxmfmWuIIfpeIghUUN3MDDv[kAyNjF2ODFOwG0> NWf1ZpVkOjR6MUmxNVY>
NIH-3T3 NETN[oVMcW6jc3WgRZN{[Xl? MmK3NUBp M{e0XGlvcGmkaYTpc44hd2ZiaIXtZY4hTU2OND3meZNm\CCDTFugNVE2OVSrboOgcZV1[W62IHX4dJJme3OnZDDhd5Nme3OnZDDhd{BxcG:|cHjvMWFNUyCuZY\lcEB4cXSqIFnDOVAhd2ZiMz6wN|kh|ryP M2SzeFI1QDF7MUG2
KARPAS299 M1nGcmtqdmG|ZTDBd5NigQ>? Ml;jPVAhdWmw NUP1XZJqTE2VTx?= M1nGN2lvcGmkaYTpc44hd2ZiTmDNMYZ2e2WmIFHMT{BxcG:|cHjvdplt[XSrb36g[ZhxemW|c3XkJJdqfGhiSVO1NEBw\iByLkGxJO69VQ>? NEnyZ2szPDlyMEe1NC=>
MKN 45 NIDZb|lMcW6jc3WgRZN{[Xl? NHvGbWwyKGh? NF\icnpFVVOR MlfLTY5pcWKrdHnvckBw\iClLV3leEBxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEKg{txO MnnnNlQ6ODB5NUC=
A549 NFrLfY5EgXSxdH;4bYMhSXO|YYm= NHTHU3c1QCCq NE\xcotFVVOR MmjBTWM2OCCxZjC0MlA5PCEQvF2= NHXpfYMzPDlyMEizNC=>
NCI-H1975 MVHDfZRwfG:6aXOgRZN{[Xl? M3jHW|Q5KGh? NHq3RotFVVOR MkPzTWM2OCCxZjC3MlU2OSEQvF2= M1Xa[|I1QTByOEOw
NCI-H1993 MoH5R5l1d3SxeHnjJGF{e2G7 NEfOZ2M1QCCq NEX1U2pFVVOR MkOwTWM2OCCxZjCwMlA3OSEQvF2= NIrWTYUzPDlyMEizNC=>
NCI-H1993 M3H3W2Fxd3Sxc3nzJGF{e2G7 NW\vfIFWOSEQvF2= MYiyOEBp M2nSPWROW09? NW[zc|lm\G:nczDuc5QhcW6mdXPlJIFxd3C2b4Ppdy=> NH;udnQzPDlyMEizNC=>
NIH-3T3 Mmr3R5l1d3SxeHnjJGF{e2G7 M4H0SFQ5KGh? MUDEUXNQ MWDJR|UxKG:oIECuN|Y1KM7:TR?= NIXVUowzPDlyMEizNC=>
EBC1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWO3NkBp NGTuW2JFVVOR NGHxZ3NKSzVyIH;mJFAvODB4OTFOwG0> MnfmNlQ6ODB6M{G=
KARPAS299 MkHyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF32eVQ4OiCq NGnifpFFVVOR NELEfGlKSzVyIH;mJFAvOiEQvF2= NFLpcHQzPDlyMEizNS=>
NB1 Ml\LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\KdGlEPTB;OUGuPVghdk1? Ml[xV2FPT0WU
NCI-SNU-5 Mn:4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTFyNT63OUBvVQ>? MWXTRW5ITVJ?
SR NIPtRXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MorMTWM2OD1zMk[uN|Ehdk1? Ml;5V2FPT0WU
SF539 MmHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHSTWM2OD1{MESuNlQhdk1? MUDTRW5ITVJ?
SU-DHL-1 NHTWTVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTvZVQ3UUN3ME2zN|YvQDJibl2= M2npOnNCVkeHUh?=
SCC-3 NVjhTZFpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHxb|ZKSzVyPUO1Ok44PiCwTR?= MXHTRW5ITVJ?
DEL Mn65S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mle1TWM2OD1|NkmuPUBvVQ>? NGTSW3BUSU6JRWK=
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D-283MED M1[2Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLXTWM2OD12OD6zOVQzKM7:TR?= MnnXV2FPT0WU
NCI-H2126 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo[5TWM2OD12OD64OFc3KM7:TR?= MYjTRW5ITVJ?
NCI-SNU-16 M4ToXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTR7LkKxOFMh|ryP MnvKV2FPT0WU
CESS MlOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXtTJBKSzVyPUS5MlUxQDhizszN MX;TRW5ITVJ?
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... 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)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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