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 MVvDfZRwfG:6aXOgRZN{[Xl? NF7Cc3I1QCCq M2f0R2ROW09? NFPqcmdEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBDSUZ|IHPlcIx{KGW6cILld5NqdmdiQVzLJGYyOTd2TDDteZRidnRiY3;lfJBz\XO|aX7nJGVOVDRid3n0bEBKSzVyIH;mJFAvPjJizszN M1PFV|IyPTd{NUi5
BAF3 NH\6TphEgXSxdH;4bYMhSXO|YYm= M322U|Q5KGh? NYeyTWZYTE2VTx?= M{jXNmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KG2xdYPlJGJCTjNiY3XscJMh\XiycnXzd4lv\yCDTFugUFEyQT[PIH31eIFvfCClb3X4dJJme3OrbnegSW1NPCC5aYToJGlEPTBib3[gNk4zKM7:TR?= Mn\uNlE2PzJ3OEm=
BAF3 NXHle3NJS3m2b4TvfIlkKEG|c3H5 MUm0PEBp NGjiOpZFVVOR NV;TZpVoS3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhSkGIMzDj[YxteyCneIDy[ZN{cW6pIFXNUFQuSUyNIIfpeIghUUN3MDDv[kAxNjJ6IN88US=> NWLHfHBQOjF3N{K1PFk>
Kelly NHTaNJREgXSxdH;4bYMhSXO|YYm= NXS4RlJYTE2VTx?= MVrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDL[YxtgSClZXzsd{BmgHC{ZYPzbY5oKEGOSzDGNVE4PExibYX0ZY51KHerdHigTWM2OCCxZjCwMlQzKM7:TR?= MX:yNVU4OjV6OR?=
SH-SY5Y M3;wcGN6fG:2b4jpZ{BCe3OjeR?= NXvBd5BMTE2VTx?= NHfnVmFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUUC2VWUXZJINmdGy|IHX4dJJme3OrbnegRWxMKEZzMUe0UEBufXSjboSge4l1cCCLQ{WwJI9nKDBwNUOg{txO NF;0U5YzOTV5MkW4PS=>
SMS-KCN MkDyR5l1d3SxeHnjJGF{e2G7 M{DMWmROW09? M2W4e2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNOWy2NQ16gZ4VtdHNiZYjwdoV{e2mwZzDBUGshWjF{N{XRJI12fGGwdDD3bZRpKEmFNUCgc4YhOC57MTFOwG0> NEDWdWQzOTV5MkW4PS=>
BAF3 M{\LcGN6fG:2b4jpZ{BCe3OjeR?= NVGyXXlxPDhiaB?= MlrnSG1UVw>? NVixdWZUS3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhSkGIMzDj[YxteyCneIDy[ZN{cW6pIGTlcE1CVEtid3n0bEBKSzVyIH;mJFAvOTlizszN M3zXT|IyPTd{NUi5
3T3 MormSpVv[3Srb36gRZN{[Xl? MYSxJIg> MnHBSG1UVw>? NGjXN4JKdmirYnn0bY9vKG:oIGLPUkBie3Onc4Pl[EBieyCpcn;3eIgh\mGldH;yMYlv\HWlZXSgZZV1d3Cqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMD6wPEDPxE1? M1jYXlIyQDF{NEG0
3T3-E MlX4SpVv[3Srb36gRZN{[Xl? MVmxJIg> MULEUXNQ MXvJcohq[mm2aX;uJI9nKFSLRUKgZZN{\XO|ZXSg[5Jwf3SqIH\hZ5Rwei2rbnT1Z4VlKGG3dH;wbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFAvPDR6IN88US=> NXG2TFhGOjF6MUK0NVQ>
A549 Ml3lT4lv[XOnIFHzd4F6 NH;yO24yKGh? NVrIc2J{TE2VTx?= M3rtfmlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiYz3NSXQhc2mwYYPlJIV5eHKnc4Pl[EBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGhITi2rbnT1Z4VlKGG3dH;wbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFAvODB6IN88US=> MormNlE5OTJ2MUS=
BAF3-BCL MXrGeY5kfGmxbjDBd5NigQ>? MnXUNUBp NIP5dVFFVVOR M{nmWmlvcGmkaYTpc44hd2ZiQVLMJIF{e2W|c3XkJIF{KGe{b4f0bEBn[WO2b4KtbY5lfWOnZDDheZRweGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iBzLkG1PUDPxE1? NXfnOJRmOjF6MUK0NVQ>
HEK293 NEXCUlZHfW6ldHnvckBCe3OjeR?= NHKwcZMyKGh? NGXvPVhFVVOR MnfqTY5pcWKrdHnvckBw\iCDWFygZZN{\XO|ZXSgZZMh\3Kxd4ToJIZi[3Sxcj3pcoR2[2WmIHH1eI9xcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMkm0JO69VQ>? MUeyNVgyOjRzNB?=
HEK293 NUHhbHJZTnWwY4Tpc44hSXO|YYm= NVvzenlnOSCq NU\WV2VWTE2VTx?= NFPXVJJKdmirYnn0bY9vKG:oIFnSJIF{e2W|c3XkJIF{KGe{b4f0bEBn[WO2b4KtbY5lfWOnZDDheZRweGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iB{Lki4O{DPxE1? Mmf3NlE5OTJ2MUS=
Jurkat NWC4co0xTnWwY4Tpc44hSXO|YYm= Mni3NUBp NEHTOmFFVVOR MkfSTY5pcWKrdHnvckBw\iCOQ1ugZZN{\XO|ZXSgZZMh\3Kxd4ToJIZi[3Sxcj3pcoR2[2WmIHH1eI9xcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDJwN{SxJO69VQ>? MnvYNlE5OTJ2MUS=
KARPAS299 MXzLbY5ie2ViQYPzZZk> NYHnOY1OOSCq MoPqSG1UVw>? MoLmTY5pcWKrdHnvckBw\iCDTFugZZN{\XO|ZXSgZZMh\3Kxd4ToJIZi[3Sxcj3pcoR2[2WmIHH1eI9xcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEKg{txO MYOyNVgyOjRzNB?=
PAE M3ThTWZ2dmO2aX;uJGF{e2G7 MXKxJIg> MYjEUXNQ NHLUNY1KdmirYnn0bY9vKG:oIGTST2Ih[XO|ZYPz[YQh[XNiZ4Lve5RpKG[jY4Tvdk1qdmS3Y3XkJIF2fG:yaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIECuN|k6KM7:TR?= MXKyNVgyOjRzNB?=
BAF3 NWDWTVhtTnWwY4Tpc44hSXO|YYm= MoL6Nk0{KGR? M4DYd2ROW09? NGnTV3NKdmirYnn0bY9vKG:oIGTFUE1nfXOnZDDpcpN2dGmwIILlZ4VxfG:{IHX4dJJme3OnZDD3bZRpKEmFNUCgc4YhOS54NEOg{txO NIqz[m8zOzd2MkK1Ni=>
KARPAS299 NX3mSmJjS3m2b4TvfIlkKEG|c3H5 MXKyMVMh\A>? MXHEUXNQ NH7FUI5KSzVyPUCuNFY1OiEQvF2= M{XTSVI{PzR{MkWy
EBC1 Mkm2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEn5[HA4OiCq MXPEUXNQ M2rqOmlEPTB;MD6wNlMh|ryP NHHUTmEzOzl7M{OyPC=>
HCT116 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XueFczKGh? M4\0RmROW09? M3XjcGlEPTB;MUSuPFIh|ryP MoXVNlM6QTN|Mki=
MCF7 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUe3NkBp NYrNU|lWTE2VTx?= NGrsVGZKSzVyPUmuOVgh|ryP MV:yN|k6OzN{OB?=
MDA-MB-231 MnXFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnQO|IhcA>? NHnRV2NFVVOR NVfjXHM6UUN3ME2xNE45KM7:TR?= Mmr3NlM6QTN|Mki=
MKN45 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmG2O|IhcA>? M1nP[2ROW09? NHvjflNKSzVyPUCuNFE{KM7:TR?= NUTrZVY3OjN7OUOzNlg>
NCI-H441 NF;RcXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXOVmd[PzJiaB?= MWLEUXNQ M2LvTGlEPTB;MUeuNlUh|ryP Mlq3NlM6QTN|Mki=
NCI-H661 NX34ZWZQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzHcohXPzJiaB?= MVPEUXNQ NVWzdZNSUUN3ME2xNU41PyEQvF2= NGfzN2UzOzl7M{OyPC=>
SK-MEL-28 NHTFR|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1vUSFczKGh? NV7qdY5lTE2VTx?= NF3HbWJKSzVyPUGwMlk4KM7:TR?= MV6yN|k6OzN{OB?=
SKOV3 NYfrZ2pDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXq3NkBp MojNSG1UVw>? NEXxe3NKSzVyPUGyMlg2KM7:TR?= MkPhNlM6QTN|Mki=
SNU5 NFLTWIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWO3NkBp MXTEUXNQ NW\idodiUUN3ME2wMlAyPiEQvF2= MmfLNlM6QTN|Mki=
NCI-H2228 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;xO|IhcA>? M37NT2ROW09? MXvJcohq[mm2aX;uJI9nKEGOSz3meZNqd25iZILpeoVvKGOnbHygdJJwdGmoZYLheIlwdiC5aYToJGlEPTBib3[gNE4yOThizszN NF3qPWUzPDR|MkmwPS=>
NCI-H3122 M2\ie2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M16yfFczKGh? M1qzcWROW09? M1LwdmlvcGmkaYTpc44hd2ZiQVzLMYZ2e2mxbjDkdol3\W5iY3XscEBxem:uaX\ldoF1cW:wIIfpeIghUUN3MDDv[kAxNjFyODFOwG0> NIrNVXQzPDR|MkmwPS=>
NCI-H3122 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rhdFczKGh? NXXVfo12TE2VTx?= M1PTTGlvcGmkaYTpc44hd2ZiQVzLMYZ2e2mxbjDkdol3\W5iY3XscEBxem:uaX\ldoF1cW:wIHnuJIh2dWGwIF7DTU1JOzF{MjDj[YxteyCqYYLic5JqdmdiQVzLJGcyOjZ7QTDteZRidnRid3n0bEBKSzVyIH;mJFAvPjJ|IN88US=> NECyNmgzPDR|MkmwPS=>
NCI-H3122 NV;iXYM6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjZO|IhcA>? M3nDO2ROW09? NGDBVXRKdmirYnn0bY9vKG:oIFHMT{1nfXOrb36g[JJqfmWwIHPlcIwheHKxbHnm[ZJifGmxbjDpckBpfW2jbjDOR2kuUDNzMkKgZ4VtdHNiaHHyZo9zcW6pIFHMT{BNOTF7Nl2gcZV1[W62IIfpeIghUUN3MDDv[kAxNjh|ODFOwG0> MV:yOFQ{OjlyOR?=
NIH-3T3 M17zcWtqdmG|ZTDBd5NigQ>? M2P3d|EhcA>? MkHpSG1UVw>? NETrTGhKdmirYnn0bY9vKG:oIHj1cYFvKHerbHSgeJlx\SCHTVy0MYZ2e2WmIFHMT{BmgHC{ZYPz[YQh[XO|ZYPz[YQh[XNicHjvd5Bpd3K7bHH0[YQhSUyNIHzleoVtKHerdHigTWM2OCCxZjCwMlA5KM7:TR?= MUiyOFQ{OjlyOR?=
NIH-3T3 NInGd4hMcW6jc3WgRZN{[Xl? NV;yZmJZOSCq NUHPboRVTE2VTx?= M3rsfWlvcGmkaYTpc44hd2ZiaIXtZY4hTU2OND3meZNm\CCDTFugS|EzPjmDIH31eIFvfCCneIDy[ZN{\WRiYYPz[ZN{\WRiYYOgdIhwe3Cqbz3BUGshdGW4ZXyge4l1cCCLQ{WwJI9nKDBwNkC1JO69VQ>? M1ywVVI1PDN{OUC5
NIH-3T3 MXLLbY5ie2ViQYPzZZk> Ml[1NUBp Mnq3SG1UVw>? Ml3UTY5pcWKrdHnvckBw\iCqdX3hckBGVUx2LX\1d4VlKEGOSzDTNVIxPllibYX0ZY51KGW6cILld5Nm\CCjc4Pld5Nm\CCjczDwbI9{eGixLVHMT{Bt\X[nbDD3bZRpKEmFNUCgc4YhOC54Mk[g{txO MWOyOFQ{OjlyOR?=
NIH-3T3 M3T2bGtqdmG|ZTDBd5NigQ>? MnTINUBp MXvEUXNQ M2TaN2lvcGmkaYTpc44hd2ZiaIXtZY4hTU2OND3meZNm\CCDTFugUFEyQT[PIH31eIFvfCCneIDy[ZN{\WRiYYPz[ZN{\WRiYYOgdIhwe3Cqbz3BUGshdGW4ZXyge4l1cCCLQ{WwJI9nKDBwOESzJO69VQ>? NED5ZZQzPDR|MkmwPS=>
NIH-3T3 MVTLbY5ie2ViQYPzZZk> NX\uU3J4OSCq NF7hcXhFVVOR M2i2cGlvcGmkaYTpc44hd2ZiaIXtZY4hTU2OND3meZNm\CCDTFugUFEyPTKUIH31eIFvfCCneIDy[ZN{\WRiYYPz[ZN{\WRiYYOgdIhwe3Cqbz3BUGshdGW4ZXyge4l1cCCLQ{WwJI9nKDFwMEK2JO69VQ>? Mom4NlQ1OzJ7MEm=
BAF3 Mo\TSpVv[3Srb36gRZN{[Xl? NXf2U3NrPzJiaB?= M2P3fGROW09? M3njbmlvcGmkaYTpc44hd2ZiTmDNM2FNUyC2cnHud4Zm[3SnZDDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIIfpeIghUUN3MDDv[kAxNjB3MTFOwG0> NW[3fZRqOjR2Nki2N|I>
BAF3 MVTDfZRwfG:6aXOgRZN{[Xl? M1HVflczKGh? M3T4WWROW09? MXXJR|UxRTBwOUig{txO M1L2dFI1PDZ6NkOy
NIH-3T3 MmrtT4lv[XOnIFHzd4F6 MWCxJIg> NHT1TphKdmirYnn0bY9vKG:oIHj1cYFvKEWPTESt[pV{\WRiQVzLJGYyOTd2TDDteZRidnRiZYjwdoV{e2WmIHHzd4V{e2WmIHHzJJBpd3OyaH:tRWxMKGyndnXsJJdqfGhiSVO1NEBw\iByLkG2OUDPxE1? Mm\UNlQ5OTlzMU[=
NIH-3T3 M3fQXWtqdmG|ZTDBd5NigQ>? MlHhNUBp M4LMWWlvcGmkaYTpc44hd2ZiaIXtZY4hTU2OND3meZNm\CCDTFugR|EyPT[\IH31eIFvfCCneIDy[ZN{\WRiYYPz[ZN{\WRiYYOgdIhwe3Cqbz3BUGshdGW4ZXyge4l1cCCLQ{WwJI9nKDBwNEe4JO69VQ>? NYrtSVZtOjR6MUmxNVY>
NIH-3T3 Ml\3T4lv[XOnIFHzd4F6 NHL4S5cyKGh? NGL6eJRKdmirYnn0bY9vKG:oIHj1cYFvKEWPTESt[pV{\WRiQVzLJGcyOjB{UjDteZRidnRiZYjwdoV{e2WmIHHzd4V{e2WmIHHzJJBpd3OyaH:tRWxMKGyndnXsJJdqfGhiSVO1NEBw\iBzLkG0PEDPxE1? MmraNlQ5OTlzMU[=
NIH-3T3 NIXHN3pMcW6jc3WgRZN{[Xl? MWSxJIg> MmS3TY5pcWKrdHnvckBw\iCqdX3hckBGVUx2LX\1d4VlKEGOSzCxNVUyXGmwczDteZRidnRiZYjwdoV{e2WmIHHzd4V{e2WmIHHzJJBpd3OyaH:tRWxMKGyndnXsJJdqfGhiSVO1NEBw\iB|LkCzPUDPxE1? M1;HT|I1QDF7MUG2
KARPAS299 NIDzcHJMcW6jc3WgRZN{[Xl? NGPhZ2k6OCCvaX6= MknVSG1UVw>? MVvJcohq[mm2aX;uJI9nKE6STT3meZNm\CCDTFugdIhwe3Cqb4L5cIF1cW:wIHX4dJJme3OnZDD3bZRpKEmFNUCgc4YhOC5zMTFOwG0> M3ryNVI1QTByN{Ww
MKN 45 MofuT4lv[XOnIFHzd4F6 NX7tVmdOOSCq M{[4NGROW09? M1PWNGlvcGmkaYTpc44hd2ZiYz3N[ZQheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCyJO69VQ>? NHmyVoEzPDlyMEe1NC=>
A549 M2T6W2N6fG:2b4jpZ{BCe3OjeR?= NXThZZlLPDhiaB?= MlLZSG1UVw>? M{fL[WlEPTBib3[gOE4xQDRizszN MnnTNlQ6ODB6M{C=
NCI-H1975 NWLyZZFqS3m2b4TvfIlkKEG|c3H5 Mn3tOFghcA>? MmLESG1UVw>? M4rhO2lEPTBib3[gO{42PTFizszN NXrlXWpbOjR7MEC4N|A>
NCI-H1993 M2XLcmN6fG:2b4jpZ{BCe3OjeR?= NHTlZlg1QCCq M1HQTGROW09? NYXEeFJtUUN3MDDv[kAxNjB4MTFOwG0> NEfqdYgzPDlyMEizNC=>
NCI-H1993 NF;4N2VCeG:2b4Ppd{BCe3OjeR?= MV:xJO69VQ>? NF\xZ|czPCCq M4fQNmROW09? M4jNU4Rw\XNibn;0JIlv\HWlZTDhdI9xfG:|aYO= MoH0NlQ6ODB6M{C=
NIH-3T3 MUHDfZRwfG:6aXOgRZN{[Xl? MnOwOFghcA>? M1vQVGROW09? M4riNWlEPTBib3[gNE4{PjRizszN NG\qXmEzPDlyMEizNC=>
EBC1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjLe2p7PzJiaB?= NHHTTolFVVOR NFfKVIZKSzVyIH;mJFAvODB4OTFOwG0> M{nBRlI1QTByOEOx
KARPAS299 Mn7JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVniU3BZPzJiaB?= MnvDSG1UVw>? NF;YWnNKSzVyIH;mJFAvOiEQvF2= M{XuelI1QTByOEOx
NB1 MnPZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlH1TWM2OD17MT65PEBvVQ>? M2DSWXNCVkeHUh?=
NCI-SNU-5 NGfvSJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULDWZJNUUN3ME2xNFUvPzVibl2= MWTTRW5ITVJ?
SR NF\oRZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fZV2lEPTB;MUK2MlMyKG6P MoDkV2FPT0WU
SF539 M4rabmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLIbmdEUUN3ME2yNFQvOjRibl2= MXnTRW5ITVJ?
SU-DHL-1 M1;QZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XWbmlEPTB;M{O2MlgzKG6P MkPzV2FPT0WU
SCC-3 NIHFRYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITpUXFKSzVyPUO1Ok44PiCwTR?= MWDTRW5ITVJ?
DEL NWD3PGxuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTN4OT65JI5O NVf3fmcyW0GQR1XS
CTV-1 NFrPVmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXsfI9KSzVyPUW5Ok41QCCwTR?= NIC5T2NUSU6JRWK=
EM-2 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRTZyMT6zOEBvVQ>? NIjvS3hUSU6JRWK=
MHH-CALL-2 NXLkTpp[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTZ6Mj61O{BvVQ>? MlvDV2FPT0WU
KM12 NUHafIpnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTdyNj65JI5O NXXJVYw6W0GQR1XS
KINGS-1 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnviTWM2OD15NEmuO|Uhdk1? NHXQUoJUSU6JRWK=
MEG-01 NHn5dlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfkWVA5UUN3ME24OVcvPjZibl2= NUj3V5ZjW0GQR1XS
BV-173 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPw[pFqUUN3ME2xMlA2QTl5IN88US=> NYixTnh7W0GQR1XS
LAMA-84 NWHnXld6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfkTWM2OD1zLkO4NlgzKM7:TR?= MlTpV2FPT0WU
KARPAS-299 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIf4dHRKSzVyPUGuOFA5PjFizszN MmOwV2FPT0WU
K-562 MmG3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTFwN{KyOlkh|ryP M1fPO3NCVkeHUh?=
SK-LMS-1 NFK5eFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTFwN{[4Olch|ryP MWTTRW5ITVJ?
MOLT-16 M1HjV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLXTWM2OD1zLkm1OVc2KM7:TR?= MmnnV2FPT0WU
CMK MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3hOoJKSzVyPUGuPVYyPTlizszN NUniToRZW0GQR1XS
ST486 M{DzbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmj3TWM2OD1{LkSzNFc{KM7:TR?= M1G2XnNCVkeHUh?=
CI-1 NVLLO2hKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHEbYlKSzVyPUKuOFk3PTlizszN M1HqOHNCVkeHUh?=
KP-N-RT-BM-1 M4\DRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGf5SVlKSzVyPUKuO|AyOjJizszN NXO2SpRxW0GQR1XS
ALL-PO M3rIdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLjTWM2OD1|LkG4NlA4KM7:TR?= NV\hWnBYW0GQR1XS
KS-1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jCb2lEPTB;Mz6yNVIzPSEQvF2= NYG0V4Y1W0GQR1XS
Becker NVv6eYFnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjVd3c5UUN3ME20MlI{QTNizszN NHTRPWdUSU6JRWK=
GDM-1 M1L1cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfDO3lGUUN3ME20MlI1PjF5IN88US=> MWHTRW5ITVJ?
BC-1 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\ae|BKSzVyPUSuOFkzPzdizszN NIDnPWZUSU6JRWK=
NB14 M4Xtcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LNWGlEPTB;ND64N|UzPCEQvF2= NVPMfWhPW0GQR1XS
NOS-1 NVvTeG42T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTVwM{O4O|Qh|ryP MVXTRW5ITVJ?
MZ1-PC NVPKUVJET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zCTGlEPTB;NT64NlE2OSEQvF2= MWjTRW5ITVJ?
A498 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUe1RngxUUN3ME22MlA5PDd|IN88US=> MnHDV2FPT0WU
EW-16 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULaPZNDUUN3ME22MlM4Pzd|IN88US=> NHHEU|NUSU6JRWK=
NALM-6 Mor2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTZwNkizPFch|ryP NX\uO3M2W0GQR1XS
EB-3 NFO1OG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3X5[2lEPTB;Nz6wO|I{OyEQvF2= MWnTRW5ITVJ?
697 MlvYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPGTWM2OD17LkK0N|I6KM7:TR?= NFHVRmpUSU6JRWK=
Ramos-2G6-4C10 M{LPcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTlwNUm4OFIh|ryP NEmxV49USU6JRWK=
KNS-81-FD NHzPfWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2i2RmlEPTB;OT62PVY2OyEQvF2= NWCweod1W0GQR1XS
HUTU-80 Mn3VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4L5XWlEPTB;OT63OFY1OiEQvF2= MV3TRW5ITVJ?
LS-411N M1;PV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTkeWpKSzVyPUGwMlA2PjdizszN NYXjV2lHW0GQR1XS
RPMI-8402 M2HkZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fk[GlEPTB;MUCuNVE3KM7:TR?= MnnEV2FPT0WU
KU812 NVe4SnpHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXkTWM2OD1zMD6yPVkyKM7:TR?= NFzPW5dUSU6JRWK=
EW-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTFyLkS0NlUh|ryP MU\TRW5ITVJ?
HC-1 NVTrRog1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTQTWM2OD1zMD60PFQ1KM7:TR?= NHK4VW1USU6JRWK=
NB69 Mmm0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTFyLkWwOFMh|ryP NEjieVBUSU6JRWK=
MFH-ino MmjZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHRWm44UUN3ME2xNE45OzB|IN88US=> NISzR3hUSU6JRWK=
CCRF-CEM MkO2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInmdnVKSzVyPUGxMlU6PyEQvF2= MVvTRW5ITVJ?
SK-N-DZ NVHtdJdHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTF{LkC0N|Yh|ryP NEHGSVBUSU6JRWK=
NCI-H720 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3XWpdKSzVyPUGyMlE4ODVizszN MVPTRW5ITVJ?
HCC1187 NIXhWVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DPdmlEPTB;MUKuNlA1OSEQvF2= NWfDfWhsW0GQR1XS
IST-SL2 NUnJXXRLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTF{LkS4O|Ih|ryP NV3D[opXW0GQR1XS
KE-37 M4HtVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHWTWM2OD1zMj63PVY3KM7:TR?= MUfTRW5ITVJ?
HCC1599 NGfESIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTLZZJKSzVyPUGyMlkxPjlizszN M1nzR3NCVkeHUh?=
A4-Fuk NXG5TIZLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjCfWpKSzVyPUGyMlk2QDZizszN NHPScFlUSU6JRWK=
NKM-1 MmrOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrJfo5iUUN3ME2xN{4zQTJ3IN88US=> M3;ZfnNCVkeHUh?=
BE-13 MmKwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTi[W5KSzVyPUGzMlc6QDlizszN NEHXUVBUSU6JRWK=
MV-4-11 NEPqNW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3:wUWlEPTB;MUSuNFMzPCEQvF2= NXz3Sok4W0GQR1XS
OPM-2 MkfFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnxTWM2OD1zND60NFg2KM7:TR?= NWrrN3JoW0GQR1XS
KARPAS-422 NWfJUpV2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPYTWM2OD1zND61NVI3KM7:TR?= MXfTRW5ITVJ?
RPMI-8226 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\mN2h[UUN3ME2xOE45QTF3IN88US=> NYLKSohEW0GQR1XS
KARPAS-45 M1e1eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;4TWM2OD1zNT63O|E3KM7:TR?= MVnTRW5ITVJ?
SK-PN-DW M17Kd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{[yNmlEPTB;MUWuPFY{OSEQvF2= NFjlR5lUSU6JRWK=
LC-2 M33hfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTF4LkG1NFYh|ryP NInaZ|FUSU6JRWK=
NCI-H1648 Ml7HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfsTWM2OD1zNj6yOVQh|ryP MmnGV2FPT0WU
RL95-2 NH25fYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnZPFg4UUN3ME2xOk4{QTd6IN88US=> NWWwOFNVW0GQR1XS
KNS-42 NHjkZXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnIdG1EUUN3ME2xOk44Ojd2IN88US=> M2TrXXNCVkeHUh?=
RPMI-6666 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnuRotbUUN3ME2xOk46OjFzIN88US=> NWPuepVHW0GQR1XS
SIG-M5 MnvHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jtUWlEPTB;MUeuNVkxOyEQvF2= NVHLRVdEW0GQR1XS
VA-ES-BJ M3TPcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\JN41KSzVyPUG3Mlc1PTFizszN MWjTRW5ITVJ?
MONO-MAC-6 NILHdVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTF5LkmzNVIh|ryP MYDTRW5ITVJ?
LAN-6 NWTZNZhtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITKdI5KSzVyPUG4Mlc2PTdizszN M13POHNCVkeHUh?=
A388 MkTaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoO3TWM2OD1zOT6zNFU6KM7:TR?= NGfBXYtUSU6JRWK=
SK-NEP-1 Mo\lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTJyLkKxN|Ih|ryP MYfTRW5ITVJ?
TE-10 NVjCXYkxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTJyLkWyNlEh|ryP NEfxNW5USU6JRWK=
HL-60 Ml22S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nGWWlEPTB;MkCuPVA6QSEQvF2= NHHlTpFUSU6JRWK=
MC116 Mn7tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mof5TWM2OD1{MT63NlIyKM7:TR?= M4f2bXNCVkeHUh?=
SW962 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXlTWM2OD1{MT63PVE2KM7:TR?= NGTRcWtUSU6JRWK=
NOMO-1 NHP2WJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTJ{Lk[1OlQh|ryP NGjHN3hUSU6JRWK=
CTB-1 MnTIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnzTWM2OD1{Mj64OlcyKM7:TR?= NHnXeWRUSU6JRWK=
MRK-nu-1 NF20c21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjQTWM2OD1{Mj65NFc1KM7:TR?= M1TvRXNCVkeHUh?=
GR-ST Mmq3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTJ|Lke2JO69VQ>? NUG3PIR3W0GQR1XS
HH MnrtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWj2VWJtUUN3ME2yOE4xODNizszN MVXTRW5ITVJ?
NCI-H1963 M4HMdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFn3bHpKSzVyPUK0MlA4QDJizszN MUTTRW5ITVJ?
QIMR-WIL NUnoNlFGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPKTWM2OD1{ND64O|czKM7:TR?= MonBV2FPT0WU
CGTH-W-1 M4XpcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPhXlZKSzVyPUK1MlA4OjNizszN M1jzfnNCVkeHUh?=
LP-1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPLTWM2OD1{NT62OVUyKM7:TR?= NEPJdJBUSU6JRWK=
NCI-H748 MnjGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3ocplKSzVyPUK2MlUyOzdizszN NFvPd2pUSU6JRWK=
PF-382 MkH2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\PVIVKSzVyPUK3MlIzOjNizszN MWHTRW5ITVJ?
ATN-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jsR2lEPTB;MkeuN|c{OiEQvF2= NFHS[2FUSU6JRWK=
L-540 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHoTWM2OD1{Nz62OFU6KM7:TR?= NGLLNG9USU6JRWK=
LXF-289 NEXsOoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{e1dGlEPTB;MkeuO|UyQSEQvF2= NUjmTVdmW0GQR1XS
LS-513 M2\3Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HHOWlEPTB;MkiuNVgxPyEQvF2= NVLPV3dKW0GQR1XS
NCI-H1581 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\PVnJNUUN3ME2zNE4{QTd4IN88US=> MmHoV2FPT0WU
ES6 M2D5Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDpSZpKSzVyPUOwMlY5QTlizszN MkewV2FPT0WU
SW982 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTNyLki1OlYh|ryP M3\KZnNCVkeHUh?=
DOHH-2 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3BTWM2OD1|MT61PFk{KM7:TR?= Mon0V2FPT0WU
DB Mk\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLIcGdKSzVyPUOzMlk1OzFizszN NU[5bHE6W0GQR1XS
MPP-89 NVjUZlVMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;6dGlEPTB;M{SuNVc2PiEQvF2= M3i3fnNCVkeHUh?=
LB831-BLC MmO0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLBSmZpUUN3ME2zOE42OTh2IN88US=> M{\aT3NCVkeHUh?=
NB5 NUHRW4s5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTN2Lki1N|Uh|ryP MmfRV2FPT0WU
GB-1 NI\U[oxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTN3LkC0Olkh|ryP NGDxdZVUSU6JRWK=
TE-15 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjUTWM2OD1|NT6yNlM5KM7:TR?= MVvTRW5ITVJ?
LC4-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlr6TWM2OD1|NT6zPFQ4KM7:TR?= MYrTRW5ITVJ?
NCI-H747 MkHhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTN4LkGzOlkh|ryP MV\TRW5ITVJ?
NTERA-S-cl-D1 MoXWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPYTWM2OD1|OD63N|Q4KM7:TR?= M3jwdHNCVkeHUh?=
SK-MM-2 NHj1enlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\LfGlEPTB;NECuNVE1PiEQvF2= NVHw[ppPW0GQR1XS
TGW M13j[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPCTWM2OD12MT6wOVY{KM7:TR?= MWXTRW5ITVJ?
ONS-76 NF;IPYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rvfGlEPTB;NEKuOFg5OyEQvF2= NUnEU5F6W0GQR1XS
CPC-N MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DpbmlEPTB;NEKuPVk4OSEQvF2= NWLaPIJuW0GQR1XS
ES4 M{ftXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\EN5BzUUN3ME20OE41OTV|IN88US=> Ml25V2FPT0WU
Daudi NUH0XW1TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTR3LkC4Nlch|ryP MUnTRW5ITVJ?
MOLT-4 MoX1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLTTWM2OD12NT6wPFU{KM7:TR?= MXTTRW5ITVJ?
HT-144 M3ntfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVX2ZW5HUUN3ME20Ok44OjZizszN NYDVSJVFW0GQR1XS
SW872 MnXTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTR6LkG5N|Mh|ryP MmnoV2FPT0WU
D-283MED M2rXNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nkTmlEPTB;NEiuN|U1OiEQvF2= NGD2b3JUSU6JRWK=
NCI-H2126 M3;EXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTR6Lki0O|Yh|ryP NFTOcHhUSU6JRWK=
NCI-SNU-16 M1HXfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PWcGlEPTB;NEmuNlE1OyEQvF2= M3rkVnNCVkeHUh?=
CESS MnnBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\5TWM2OD12OT61NFg5KM7:TR?= M1PtR3NCVkeHUh?=
A101D NVTCbpVUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkfPTWM2OD12OT65O|M3KM7:TR?= MX;TRW5ITVJ?

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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)


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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.

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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.

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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.

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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)

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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.

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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.

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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.

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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)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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