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 M{TsbWN6fG:2b4jpZ{BCe3OjeR?= Ml3GOFghcA>? MVTEUXNQ NWrVT5RzS3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhSkGIMzDj[YxteyCneIDy[ZN{cW6pIFHMT{BHOTF5NFygcZV1[W62IHPv[ZhxemW|c3nu[{BGVUx2IIfpeIghUUN3MDDv[kAxNjZ{IN88US=> M336TVIyPTd{NUi5
BAF3 NXTNSIpDS3m2b4TvfIlkKEG|c3H5 MVi0PEBp NVzSUpR3TE2VTx?= M2rUbGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KG2xdYPlJGJCTjNiY3XscJMh\XiycnXzd4lv\yCDTFugUFEyQT[PIH31eIFvfCClb3X4dJJme3OrbnegSW1NPCC5aYToJGlEPTBib3[gNk4zKM7:TR?= NUn4V4N2OjF3N{K1PFk>
BAF3 NV62Zm5ZS3m2b4TvfIlkKEG|c3H5 NEHSN4E1QCCq NYrlfGc2TE2VTx?= MorvR5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgRmFHOyClZXzsd{BmgHC{ZYPzbY5oKEWPTEStRWxMKHerdHigTWM2OCCxZjCwMlI5KM7:TR?= M3\4UlIyPTd{NUi5
Kelly NH[3eG5EgXSxdH;4bYMhSXO|YYm= NWr1S3ptTE2VTx?= MWTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDL[YxtgSClZXzsd{BmgHC{ZYPzbY5oKEGOSzDGNVE4PExibYX0ZY51KHerdHigTWM2OCCxZjCwMlQzKM7:TR?= M4DhUVIyPTd{NUi5
SH-SY5Y M{izcGN6fG:2b4jpZ{BCe3OjeR?= MWTEUXNQ NETTT|lEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUUC2VWUXZJINmdGy|IHX4dJJme3OrbnegRWxMKEZzMUe0UEBufXSjboSge4l1cCCLQ{WwJI9nKDBwNUOg{txO M2PvVVIyPTd{NUi5
SMS-KCN MkTzR5l1d3SxeHnjJGF{e2G7 NFrDem1FVVOR M{XkU2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNOWy2NQ16gZ4VtdHNiZYjwdoV{e2mwZzDBUGshWjF{N{XRJI12fGGwdDD3bZRpKEmFNUCgc4YhOC57MTFOwG0> M1vIOFIyPTd{NUi5
BAF3 NEXLO5VEgXSxdH;4bYMhSXO|YYm= NU\ye4hSPDhiaB?= MWrEUXNQ NYntfmoxS3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhSkGIMzDj[YxteyCneIDy[ZN{cW6pIGTlcE1CVEtid3n0bEBKSzVyIH;mJFAvOTlizszN NYTDUZQyOjF3N{K1PFk>
3T3 MnzlSpVv[3Srb36gRZN{[Xl? NEnVS4cyKGh? NGDNXWRFVVOR MVzJcohq[mm2aX;uJI9nKFKRTjDhd5Nme3OnZDDhd{Boem:5dHig[oFkfG:{LXnu[JVk\WRiYYX0c5Bpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5yODFOwG0> MmraNlE5OTJ2MUS=
3T3-E NX3nXFNbTnWwY4Tpc44hSXO|YYm= NYrIOFc5OSCq NGjQN|JFVVOR MVXJcohq[mm2aX;uJI9nKFSLRUKgZZN{\XO|ZXSg[5Jwf3SqIH\hZ5Rwei2rbnT1Z4VlKGG3dH;wbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFAvPDR6IN88US=> NYmwcoZ3OjF6MUK0NVQ>
A549 M2PuT2tqdmG|ZTDBd5NigQ>? MkTCNUBp MmHHSG1UVw>? NHTBWmZKdmirYnn0bY9vKG:oIHj1cYFvKHKnY3;tZolv[W62IHOtUWVVKGurbnHz[UBmgHC{ZYPz[YQh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBJT0ZvaX7keYNm\CCjdYTvdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjByODFOwG0> MlXONlE5OTJ2MUS=
BAF3-BCL M{jBemZ2dmO2aX;uJGF{e2G7 Mn3VNUBp Ml6wSG1UVw>? M13LR2lvcGmkaYTpc44hd2ZiQVLMJIF{e2W|c3XkJIF{KGe{b4f0bEBn[WO2b4KtbY5lfWOnZDDheZRweGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iBzLkG1PUDPxE1? NUixdYFTOjF6MUK0NVQ>
HEK293 MljwSpVv[3Srb36gRZN{[Xl? M3Sx[lEhcA>? M1TCd2ROW09? MUfJcohq[mm2aX;uJI9nKEG[TDDhd5Nme3OnZDDhd{Boem:5dHig[oFkfG:{LXnu[JVk\WRiYYX0c5Bpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5{OUSg{txO M3zrSVIyQDF{NEG0
HEK293 NVTGdnFVTnWwY4Tpc44hSXO|YYm= M1zENlEhcA>? MVvEUXNQ NFu5bo9KdmirYnn0bY9vKG:oIFnSJIF{e2W|c3XkJIF{KGe{b4f0bEBn[WO2b4KtbY5lfWOnZDDheZRweGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iB{Lki4O{DPxE1? NH3rO2MzOThzMkSxOC=>
Jurkat MljpSpVv[3Srb36gRZN{[Xl? M2Lvb|EhcA>? MUDEUXNQ Mo\VTY5pcWKrdHnvckBw\iCOQ1ugZZN{\XO|ZXSgZZMh\3Kxd4ToJIZi[3Sxcj3pcoR2[2WmIHH1eI9xcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDJwN{SxJO69VQ>? M3\CdlIyQDF{NEG0
KARPAS299 M2DBcWtqdmG|ZTDBd5NigQ>? M{XtbVEhcA>? MYfEUXNQ NV7kcHM6UW6qaXLpeIlwdiCxZjDBUGsh[XO|ZYPz[YQh[XNiZ4Lve5RpKG[jY4Tvdk1qdmS3Y3XkJIF2fG:yaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIECuNFIh|ryP NVXGdZUzOjF6MUK0NVQ>
PAE MVvGeY5kfGmxbjDBd5NigQ>? NYP1dWtKOSCq M2DJRWROW09? NEDnXJJKdmirYnn0bY9vKG:oIGTST2Ih[XO|ZYPz[YQh[XNiZ4Lve5RpKG[jY4Tvdk1qdmS3Y3XkJIF2fG:yaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIECuN|k6KM7:TR?= NFzaOlIzOThzMkSxOC=>
BAF3 NVWyOpN[TnWwY4Tpc44hSXO|YYm= M1vmNlIuOyCm NU\zTHBFTE2VTx?= MmjZTY5pcWKrdHnvckBw\iCWRVyt[pV{\WRiaX7zeYxqdiC{ZXPldJRweiCneIDy[ZN{\WRid3n0bEBKSzVyIH;mJFEvPjR|IN88US=> NFuzd2gzOzd2MkK1Ni=>
KARPAS299 M3LLNGN6fG:2b4jpZ{BCe3OjeR?= Mlj5Nk0{KGR? MnLGSG1UVw>? Ml\6TWM2OD1yLkC2OFIh|ryP NHjBOo8zOzd2MkK1Ni=>
EBC1 NVvafIZyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYi3NkBp NF7hZXlFVVOR NFTEW2pKSzVyPUCuNFI{KM7:TR?= MmfkNlM6QTN|Mki=
HCT116 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHaO|IhcA>? MWLEUXNQ Mn3LTWM2OD1zND64NkDPxE1? M3HiOFI{QTl|M{K4
MCF7 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXO3NkBp NETkSY5FVVOR M1\QbGlEPTB;OT61PEDPxE1? NGPNWoczOzl7M{OyPC=>
MDA-MB-231 M{HjdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXi3NkBp NUTW[lF5TE2VTx?= NUCzO4UzUUN3ME2xNE45KM7:TR?= NXX6XJlKOjN7OUOzNlg>
MKN45 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYG3NkBp MYLEUXNQ MljRTWM2OD1yLkCxN{DPxE1? M3q1blI{QTl|M{K4
NCI-H441 NIrZblZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXDcmhpPzJiaB?= Mlr4SG1UVw>? M2\lc2lEPTB;MUeuNlUh|ryP MWWyN|k6OzN{OB?=
NCI-H661 Ml;FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVG3NkBp MXTEUXNQ NIfhRmZKSzVyPUGxMlQ4KM7:TR?= NH[5XnUzOzl7M{OyPC=>
SK-MEL-28 MlzoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPrO|IhcA>? NXHNepVLTE2VTx?= MXrJR|UxRTFyLkm3JO69VQ>? M4fRSlI{QTl|M{K4
SKOV3 NVHE[YZxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{X0RVczKGh? MkfnSG1UVw>? MonXTWM2OD1zMj64OUDPxE1? MVmyN|k6OzN{OB?=
SNU5 Mly4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vwflczKGh? NYDF[3dlTE2VTx?= NVXvVoNEUUN3ME2wMlAyPiEQvF2= MljWNlM6QTN|Mki=
NCI-H2228 MoO2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX:3NkBp MnX0SG1UVw>? M1PqUGlvcGmkaYTpc44hd2ZiQVzLMYZ2e2mxbjDkdol3\W5iY3XscEBxem:uaX\ldoF1cW:wIIfpeIghUUN3MDDv[kAxNjFzODFOwG0> MVOyOFQ{OjlyOR?=
NCI-H3122 NWLSc2ZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEe4NGE4OiCq Mo\sSG1UVw>? M4rDO2lvcGmkaYTpc44hd2ZiQVzLMYZ2e2mxbjDkdol3\W5iY3XscEBxem:uaX\ldoF1cW:wIIfpeIghUUN3MDDv[kAxNjFyODFOwG0> MnPPNlQ1OzJ7MEm=
NCI-H3122 NEHqcW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoftO|IhcA>? MX;EUXNQ M{nK[WlvcGmkaYTpc44hd2ZiQVzLMYZ2e2mxbjDkdol3\W5iY3XscEBxem:uaX\ldoF1cW:wIHnuJIh2dWGwIF7DTU1JOzF{MjDj[YxteyCqYYLic5JqdmdiQVzLJGcyOjZ7QTDteZRidnRid3n0bEBKSzVyIH;mJFAvPjJ|IN88US=> MoDvNlQ1OzJ7MEm=
NCI-H3122 M{Kzcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDsW5M4OiCq NUfLfHQ2TE2VTx?= NFfyVYRKdmirYnn0bY9vKG:oIFHMT{1nfXOrb36g[JJqfmWwIHPlcIwheHKxbHnm[ZJifGmxbjDpckBpfW2jbjDOR2kuUDNzMkKgZ4VtdHNiaHHyZo9zcW6pIFHMT{BNOTF7Nl2gcZV1[W62IIfpeIghUUN3MDDv[kAxNjh|ODFOwG0> MmTCNlQ1OzJ7MEm=
NIH-3T3 M1m5NmtqdmG|ZTDBd5NigQ>? M4X3dVEhcA>? M1XD[GROW09? M4PKdWlvcGmkaYTpc44hd2ZiaIXtZY4hf2muZDD0fZBmKEWPTESt[pV{\WRiQVzLJIV5eHKnc4Pl[EBie3Onc4Pl[EBieyCyaH;zdIhwenmuYYTl[EBCVEtibHX2[Ywhf2m2aDDJR|UxKG:oIECuNFgh|ryP Moi2NlQ1OzJ7MEm=
NIH-3T3 M165VmtqdmG|ZTDBd5NigQ>? M4PlXVEhcA>? NUjIWmF[TE2VTx?= M3z1XWlvcGmkaYTpc44hd2ZiaIXtZY4hTU2OND3meZNm\CCDTFugS|EzPjmDIH31eIFvfCCneIDy[ZN{\WRiYYPz[ZN{\WRiYYOgdIhwe3Cqbz3BUGshdGW4ZXyge4l1cCCLQ{WwJI9nKDBwNkC1JO69VQ>? NXvxbHlEOjR2M{K5NFk>
NIH-3T3 MYjLbY5ie2ViQYPzZZk> MoPnNUBp NGPyZVNFVVOR MUjJcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIGOxNlA3YSCvdYThcpQh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IIDoc5NxcG9vQVzLJIxmfmWuIIfpeIghUUN3MDDv[kAxNjZ{NjFOwG0> MYmyOFQ{OjlyOR?=
NIH-3T3 NIHYd3VMcW6jc3WgRZN{[Xl? NVPSSoZFOSCq M{Th[GROW09? NVHYdYxkUW6qaXLpeIlwdiCxZjDoeY1idiCHTVy0MYZ2e2WmIFHMT{BNOTF7Nl2gcZV1[W62IHX4dJJme3OnZDDhd5Nme3OnZDDhd{BxcG:|cHjvMWFNUyCuZY\lcEB4cXSqIFnDOVAhd2ZiMD64OFMh|ryP NULaWIF2OjR2M{K5NFk>
NIH-3T3 NYnLU49TU2mwYYPlJGF{e2G7 MUWxJIg> NIrxNoVFVVOR MXzJcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIFyxNVUzWiCvdYThcpQh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IIDoc5NxcG9vQVzLJIxmfmWuIIfpeIghUUN3MDDv[kAyNjB{NjFOwG0> M2TrfFI1PDN{OUC5
BAF3 MVHGeY5kfGmxbjDBd5NigQ>? NWXWPI9DPzJiaB?= NYjycmFkTE2VTx?= NInY[lZKdmirYnn0bY9vKG:oIF7QUU9CVEtidILhcpNn\WO2ZXSgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjD3bZRpKEmFNUCgc4YhOC5yNUGg{txO NXHF[Fh[OjR2Nki2N|I>
BAF3 M4ewTWN6fG:2b4jpZ{BCe3OjeR?= MmP6O|IhcA>? NYj4ZYR4TE2VTx?= M1HxO2lEPTB;MD65PEDPxE1? MW[yOFQ3QDZ|Mh?=
NIH-3T3 Mk\zT4lv[XOnIFHzd4F6 MUWxJIg> M1PTcGlvcGmkaYTpc44hd2ZiaIXtZY4hTU2OND3meZNm\CCDTFugSlEyPzSOIH31eIFvfCCneIDy[ZN{\WRiYYPz[ZN{\WRiYYOgdIhwe3Cqbz3BUGshdGW4ZXyge4l1cCCLQ{WwJI9nKDBwMU[1JO69VQ>? NVGwXWRNOjR6MUmxNVY>
NIH-3T3 M2XI[2tqdmG|ZTDBd5NigQ>? NVXKPJRzOSCq MWfJcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIFOxNVU3YSCvdYThcpQh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IIDoc5NxcG9vQVzLJIxmfmWuIIfpeIghUUN3MDDv[kAxNjR5ODFOwG0> Mnn0NlQ5OTlzMU[=
NIH-3T3 MnW2T4lv[XOnIFHzd4F6 Mk\YNUBp MV\Jcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIFexNlAzWiCvdYThcpQh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IIDoc5NxcG9vQVzLJIxmfmWuIIfpeIghUUN3MDDv[kAyNjF2ODFOwG0> MUWyOFgyQTFzNh?=
NIH-3T3 M3HMSGtqdmG|ZTDBd5NigQ>? MVmxJIg> MX\Jcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIEGxOVFVcW6|IH31eIFvfCCneIDy[ZN{\WRiYYPz[ZN{\WRiYYOgdIhwe3Cqbz3BUGshdGW4ZXyge4l1cCCLQ{WwJI9nKDNwMEO5JO69VQ>? NUHNRplwOjR6MUmxNVY>
KARPAS299 MXHLbY5ie2ViQYPzZZk> MYC5NEBucW5? M133cmROW09? NYnaXXQzUW6qaXLpeIlwdiCxZjDOVG0u\nW|ZXSgRWxMKHCqb4PwbI9zgWyjdHnvckBmgHC{ZYPz[YQhf2m2aDDJR|UxKG:oIECuNVEh|ryP M{Hmd|I1QTByN{Ww
MKN 45 MkHBT4lv[XOnIFHzd4F6 M3j6R|EhcA>? MUDEUXNQ MVrJcohq[mm2aX;uJI9nKGNvTXX0JJBpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5yMjFOwG0> MoXjNlQ6ODB5NUC=
A549 MoDRR5l1d3SxeHnjJGF{e2G7 M2HQPVQ5KGh? NEG5bXVFVVOR NX\hS5cyUUN3MDDv[kA1NjB6NDFOwG0> MWGyOFkxODh|MB?=
NCI-H1975 NV;peop5S3m2b4TvfIlkKEG|c3H5 NXLk[WpjPDhiaB?= NIX3c3ZFVVOR MV;JR|UxKG:oIEeuOVUyKM7:TR?= NWHzNZJsOjR7MEC4N|A>
NCI-H1993 MUnDfZRwfG:6aXOgRZN{[Xl? NXP4bVdXPDhiaB?= NXPHSI1JTE2VTx?= MkHMTWM2OCCxZjCwMlA3OSEQvF2= NUeyW49QOjR7MEC4N|A>
NCI-H1993 NYDxPZdkSXCxdH;zbZMhSXO|YYm= Ml;lNUDPxE1? MY[yOEBp NGLUNXdFVVOR Monj[I9meyCwb4SgbY5lfWOnIHHwc5B1d3Orcx?= MWCyOFkxODh|MB?=
NIH-3T3 M2rNTmN6fG:2b4jpZ{BCe3OjeR?= MmXXOFghcA>? MnHySG1UVw>? MmTaTWM2OCCxZjCwMlM3PCEQvF2= NHvub|MzPDlyMEizNC=>
EBC1 M1fsOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\uO|IhcA>? MlfISG1UVw>? Mo\MTWM2OCCxZjCwMlAxPjlizszN NHfxRpAzPDlyMEizNS=>
KARPAS299 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHSS4k4OiCq MXnEUXNQ M1;U[WlEPTBib3[gNE4zKM7:TR?= M1jJ[|I1QTByOEOx
NB1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTlzLkm4JI5O NEHiNWlUSU6JRWK=
NCI-SNU-5 NF3rNVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXP5eo9uUUN3ME2xNFUvPzVibl2= NFe5UIFUSU6JRWK=
SR NHrM[JZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvRU3RKSzVyPUGyOk4{OSCwTR?= NXvXOVNqW0GQR1XS
SF539 M4HlSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTJyND6yOEBvVQ>? NXXRc5Y5W0GQR1XS
SU-DHL-1 M{nzOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGq3fJRKSzVyPUOzOk45OiCwTR?= NHi3OoJUSU6JRWK=
SCC-3 NGP2cZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\ReYlKSzVyPUO1Ok44PiCwTR?= MYnTRW5ITVJ?
DEL Mom0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPyV4hKSzVyPUO2PU46KG6P MXPTRW5ITVJ?
CTV-1 NXS1bplLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXDU5JJUUN3ME21PVYvPDhibl2= MUnTRW5ITVJ?
EM-2 NXP3TVl4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIe1PJRKSzVyPU[wNU4{PCCwTR?= Ml\IV2FPT0WU
MHH-CALL-2 M1SxSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTZ6Mj61O{BvVQ>? MljOV2FPT0WU
KM12 NHzp[49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXQcHhKSzVyPUewOk46KG6P NWe4dIE2W0GQR1XS
KINGS-1 NIjHW4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nHbGlEPTB;N{S5Mlc2KG6P Mk\IV2FPT0WU
MEG-01 M1XzUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIrscIpKSzVyPUi1O{43PiCwTR?= M2jrVHNCVkeHUh?=
BV-173 NVXoXYN6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7vTWM2OD1zLkC1PVk4KM7:TR?= NEjoO2hUSU6JRWK=
LAMA-84 NWLjboVUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXtS4hKSzVyPUGuN|gzQDJizszN MXvTRW5ITVJ?
KARPAS-299 NHHVeHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;tNWRKSzVyPUGuOFA5PjFizszN M17OdXNCVkeHUh?=
K-562 M{XYXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVOxRmpsUUN3ME2xMlczOjZ7IN88US=> NFzXUJFUSU6JRWK=
SK-LMS-1 MmraS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnBcYhvUUN3ME2xMlc3QDZ5IN88US=> MXLTRW5ITVJ?
MOLT-16 M{m2fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7RSndKSzVyPUGuPVU2PzVizszN M4\hSHNCVkeHUh?=
CMK MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XPdGlEPTB;MT65OlE2QSEQvF2= NUn6fJJrW0GQR1XS
ST486 NEPQNG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTJwNEOwO|Mh|ryP NH;PVllUSU6JRWK=
CI-1 NX3jSGs5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHHO5U6UUN3ME2yMlQ6PjV7IN88US=> NWXvOI9IW0GQR1XS
KP-N-RT-BM-1 MnGxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTJwN{CxNlIh|ryP MYHTRW5ITVJ?
ALL-PO MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfUTWM2OD1|LkG4NlA4KM7:TR?= MlTYV2FPT0WU
KS-1 NEPDdlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUS1c2RtUUN3ME2zMlIyOjJ3IN88US=> NE\YUJpUSU6JRWK=
Becker NIf3VIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{myXGlEPTB;ND6yN|k{KM7:TR?= M{fPSXNCVkeHUh?=
GDM-1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHNTWM2OD12LkK0OlE4KM7:TR?= NWX4WFg3W0GQR1XS
BC-1 Mk\MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zqVWlEPTB;ND60PVI4PyEQvF2= NUfQTmNMW0GQR1XS
NB14 NYnzcHZxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPt[XdKSzVyPUSuPFM2OjRizszN NWrSRm95W0GQR1XS
NOS-1 M3T0e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnDTotKSzVyPUWuN|M5PzRizszN MVzTRW5ITVJ?
MZ1-PC M1nnOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTlTWM2OD13LkiyNVUyKM7:TR?= MkH3V2FPT0WU
A498 Ml7CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnkbmpxUUN3ME22MlA5PDd|IN88US=> MlnDV2FPT0WU
EW-16 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3uzSGlEPTB;Nj6zO|c4OyEQvF2= NYTNUVJrW0GQR1XS
NALM-6 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTZwNkizPFch|ryP NWHDUpVGW0GQR1XS
EB-3 NXLnNm1qT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDZTWM2OD15LkC3NlM{KM7:TR?= NXfWPFlHW0GQR1XS
697 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlrTTWM2OD17LkK0N|I6KM7:TR?= NXHMRmh4W0GQR1XS
Ramos-2G6-4C10 M13ocmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTQTWM2OD17LkW5PFQzKM7:TR?= MnvnV2FPT0WU
KNS-81-FD MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXISXF1UUN3ME25MlY6PjV|IN88US=> Mni1V2FPT0WU
HUTU-80 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTlwN{S2OFIh|ryP NWDIWG54W0GQR1XS
LS-411N NUDnPXVQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTFyLkC1Olch|ryP M4Lt[3NCVkeHUh?=
RPMI-8402 NHXYXGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUX2NXRbUUN3ME2xNE4yOTZizszN NX3NbZNjW0GQR1XS
KU812 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRTFyLkK5PVEh|ryP MlroV2FPT0WU
EW-1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVz4PJVJUUN3ME2xNE41PDJ3IN88US=> NHHoVopUSU6JRWK=
HC-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTFyLkS4OFQh|ryP NYX6PJo5W0GQR1XS
NB69 NWrvblZ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nnOWlEPTB;MUCuOVA1OyEQvF2= NFzCPGVUSU6JRWK=
MFH-ino Mnv6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXH3T3FLUUN3ME2xNE45OzB|IN88US=> MmrsV2FPT0WU
CCRF-CEM MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHCTodTUUN3ME2xNU42QTdizszN M1XZbHNCVkeHUh?=
SK-N-DZ Ml3sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvpTWM2OD1zMj6wOFM3KM7:TR?= MnnzV2FPT0WU
NCI-H720 MoHDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTF{LkG3NFUh|ryP MXTTRW5ITVJ?
HCC1187 M{XXcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWryTZpTUUN3ME2xNk4zODRzIN88US=> NFXERoFUSU6JRWK=
IST-SL2 NF3QbFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTF{LkS4O|Ih|ryP NX;OZWU3W0GQR1XS
KE-37 MlOzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDUXm01UUN3ME2xNk44QTZ4IN88US=> MonLV2FPT0WU
HCC1599 MlraS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorsTWM2OD1zMj65NFY6KM7:TR?= MXPTRW5ITVJ?
A4-Fuk NE\KboZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXQV2JnUUN3ME2xNk46PTh4IN88US=> NXfqfnZFW0GQR1XS
NKM-1 M2m3WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfmWVlKSzVyPUGzMlI6OjVizszN MUjTRW5ITVJ?
BE-13 NVPFXXdvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDxc|htUUN3ME2xN{44QTh7IN88US=> MljvV2FPT0WU
MV-4-11 MmPpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHs[XVXUUN3ME2xOE4xOzJ2IN88US=> MmSxV2FPT0WU
OPM-2 MnrFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDEbY5KSzVyPUG0MlQxQDVizszN M{js[nNCVkeHUh?=
KARPAS-422 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4noc2lEPTB;MUSuOVEzPiEQvF2= NGrKTpBUSU6JRWK=
RPMI-8226 MlewS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTF2Lki5NVUh|ryP M{nle3NCVkeHUh?=
KARPAS-45 MkC0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDvTWM2OD1zNT63O|E3KM7:TR?= NXP2ZYt5W0GQR1XS
SK-PN-DW Ml;NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTF3Lki2N|Eh|ryP MlfGV2FPT0WU
LC-2 M4jlS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHFcG5KSzVyPUG2MlE2ODZizszN MlHqV2FPT0WU
NCI-H1648 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojZTWM2OD1zNj6yOVQh|ryP NIfWXWxUSU6JRWK=
RL95-2 NGLZeJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTF4LkO5O|gh|ryP NXfZOmlNW0GQR1XS
KNS-42 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPLRWtQUUN3ME2xOk44Ojd2IN88US=> MonwV2FPT0WU
RPMI-6666 NFXR[4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTF4LkmyNVEh|ryP M{\BN3NCVkeHUh?=
SIG-M5 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzNTWM2OD1zNz6xPVA{KM7:TR?= NIfsZ3lUSU6JRWK=
VA-ES-BJ M1Hydmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;kbGlEPTB;MUeuO|Q2OSEQvF2= MUTTRW5ITVJ?
MONO-MAC-6 NWDJWmQ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\uV4hKSzVyPUG3Mlk{OTJizszN MULTRW5ITVJ?
LAN-6 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nUUWlEPTB;MUiuO|U2PyEQvF2= MWDTRW5ITVJ?
A388 MkfTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnSTGRjUUN3ME2xPU4{ODV7IN88US=> NX3GSIoyW0GQR1XS
SK-NEP-1 MlnFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYS0VJVZUUN3ME2yNE4zOTN{IN88US=> M1H3bXNCVkeHUh?=
TE-10 NFz5b|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTJyLkWyNlEh|ryP MYjTRW5ITVJ?
HL-60 MnnRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XiNWlEPTB;MkCuPVA6QSEQvF2= MoXuV2FPT0WU
MC116 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1Gyb2lEPTB;MkGuO|IzOSEQvF2= NInBfJNUSU6JRWK=
SW962 NV7Ub49mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnL6TWM2OD1{MT63PVE2KM7:TR?= NFXQPJZUSU6JRWK=
NOMO-1 NGf3W2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrDOHVKSzVyPUKyMlY2PjRizszN MU\TRW5ITVJ?
CTB-1 M4XXRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTJ{Lki2O|Eh|ryP NVLEW2h[W0GQR1XS
MRK-nu-1 MofPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnQc4dJUUN3ME2yNk46ODd2IN88US=> NV;G[mdnW0GQR1XS
GR-ST NXHvWlRFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTJ|Lke2JO69VQ>? MW\TRW5ITVJ?
HH NIT2NphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DUNmlEPTB;MkSuNFA{KM7:TR?= NFnkSVlUSU6JRWK=
NCI-H1963 M4rnXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnjTWM2OD1{ND6wO|gzKM7:TR?= M4HuPHNCVkeHUh?=
QIMR-WIL NVT0[ZNuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoWwTWM2OD1{ND64O|czKM7:TR?= MmXNV2FPT0WU
CGTH-W-1 Mn7RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlz0TWM2OD1{NT6wO|I{KM7:TR?= NVfzXogzW0GQR1XS
LP-1 M{HTV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XD[2lEPTB;MkWuOlU2OSEQvF2= NIDFepZUSU6JRWK=
NCI-H748 NFTTWJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILxPVVKSzVyPUK2MlUyOzdizszN MlzyV2FPT0WU
PF-382 M1\ieWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTJ5LkKyNlMh|ryP NX[0fFdHW0GQR1XS
ATN-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWX4XGlMUUN3ME2yO{4{PzN{IN88US=> MVzTRW5ITVJ?
L-540 MmfIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDXPVhMUUN3ME2yO{43PDV7IN88US=> M1v2R3NCVkeHUh?=
LXF-289 M2qwO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvvTWM2OD1{Nz63OVE6KM7:TR?= M2jRdXNCVkeHUh?=
LS-513 M{f6eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTJ6LkG4NFch|ryP MoDrV2FPT0WU
NCI-H1581 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrycIxFUUN3ME2zNE4{QTd4IN88US=> NXvIUFhqW0GQR1XS
ES6 MmHpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;NTWM2OD1|MD62PFk6KM7:TR?= MUTTRW5ITVJ?
SW982 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7YTWM2OD1|MD64OVY3KM7:TR?= M2TKNHNCVkeHUh?=
DOHH-2 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYf2THY3UUN3ME2zNU42QDl|IN88US=> M1W0OHNCVkeHUh?=
DB MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUjJR|UxRTN|Lkm0N|Eh|ryP NEnrUGhUSU6JRWK=
MPP-89 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mny1TWM2OD1|ND6xO|U3KM7:TR?= M2\zPHNCVkeHUh?=
LB831-BLC M3:1[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDJc|FKSzVyPUO0MlUyQDRizszN NGT5Z2VUSU6JRWK=
NB5 M2XWU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTN2Lki1N|Uh|ryP M3mzeXNCVkeHUh?=
GB-1 M1HURWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XmR2lEPTB;M{WuNFQ3QSEQvF2= NXy3OHZZW0GQR1XS
TE-15 NEfEUJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLlTWM2OD1|NT6yNlM5KM7:TR?= M{LBbXNCVkeHUh?=
LC4-1 NHvITHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGj1bopKSzVyPUO1MlM5PDdizszN NX;SRVBHW0GQR1XS
NCI-H747 MnvaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7lTWM2OD1|Nj6xN|Y6KM7:TR?= M1;oPHNCVkeHUh?=
NTERA-S-cl-D1 M4\V[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHCTIdKSzVyPUO4Mlc{PDdizszN MUjTRW5ITVJ?
SK-MM-2 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M36yWmlEPTB;NECuNVE1PiEQvF2= MVfTRW5ITVJ?
TGW NEKzU3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTRzLkC1OlMh|ryP NHrsRZBUSU6JRWK=
ONS-76 NHe2WWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPvNHhKSzVyPUSyMlQ5QDNizszN MWHTRW5ITVJ?
CPC-N M1zUb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlqyTWM2OD12Mj65PVcyKM7:TR?= MWLTRW5ITVJ?
ES4 Mm\OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPWTWM2OD12ND60NVU{KM7:TR?= M2fEZnNCVkeHUh?=
Daudi MkPzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\zPGlEPTB;NEWuNFgzPyEQvF2= NI\SdVlUSU6JRWK=
MOLT-4 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4j6S2lEPTB;NEWuNFg2OyEQvF2= NYn4RohUW0GQR1XS
HT-144 NHjtNGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\SXXkyUUN3ME20Ok44OjZizszN M3vvOnNCVkeHUh?=
SW872 M1fXe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTmTWM2OD12OD6xPVM{KM7:TR?= M1ntdXNCVkeHUh?=
D-283MED MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTR6LkO1OFIh|ryP NXKwcml6W0GQR1XS
NCI-H2126 NULtS2dIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInKNoZKSzVyPUS4Mlg1PzZizszN NHLHdYxUSU6JRWK=
NCI-SNU-16 NWm2WokzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvZe5p3UUN3ME20PU4zOTR|IN88US=> NXP1Z2Y6W0GQR1XS
CESS MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTR7LkWwPFgh|ryP NF\vTmJUSU6JRWK=
A101D Ml\rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELTSGVKSzVyPUS5Mlk4OzZizszN 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

文献中の引用 (65)

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