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

高品質保証

文献中の引用(64)

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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 MmqxR5l1d3SxeHnjJGF{e2G7 M3y4eVQ5KGh? M3v1fWROW09? M2naTWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KG2xdYPlJGJCTjNiY3XscJMh\XiycnXzd4lv\yCDTFugSlEyPzSOIH31eIFvfCClb3X4dJJme3OrbnegSW1NPCC5aYToJGlEPTBib3[gNE43OiEQvF2= NYXvb5FOOjF3N{K1PFk>
BAF3 MoHBR5l1d3SxeHnjJGF{e2G7 MmiwOFghcA>? NE\FeXZFVVOR MnLnR5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgRmFHOyClZXzsd{BmgHC{ZYPzbY5oKEGOSzDMNVE6Pk1ibYX0ZY51KGOxZYjwdoV{e2mwZzDFUWw1KHerdHigTWM2OCCxZjCyMlIh|ryP MonONlE2PzJ3OEm=
BAF3 NX;ofIdoS3m2b4TvfIlkKEG|c3H5 NGjFeYc1QCCq M2rHUmROW09? NILCSXZEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBDSUZ|IHPlcIx{KGW6cILld5NqdmdiRV3MOE1CVEtid3n0bEBKSzVyIH;mJFAvOjhizszN NHzmcmgzOTV5MkW4PS=>
Kelly MV7DfZRwfG:6aXOgRZN{[Xl? NUf0NlJXTE2VTx?= M2LVfmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGtmdGy7IHPlcIx{KGW6cILld5NqdmdiQVzLJGYyOTd2TDDteZRidnRid3n0bEBKSzVyIH;mJFAvPDJizszN NYTE[llQOjF3N{K1PFk>
SH-SY5Y Mn23R5l1d3SxeHnjJGF{e2G7 MVHEUXNQ MnTWR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2guW1l3WTDj[YxteyCneIDy[ZN{cW6pIFHMT{BHOTF5NFygcZV1[W62IIfpeIghUUN3MDDv[kAxNjV|IN88US=> MV6yNVU4OjV6OR?=
SMS-KCN NUnRboR1S3m2b4TvfIlkKEG|c3H5 Mme1SG1UVw>? NYftOoZSS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW02VLVvDUkBk\WyuczDlfJBz\XO|aX7nJGFNUyCUMUK3OXEhdXW2YX70JJdqfGhiSVO1NEBw\iByLkmxJO69VQ>? M2HIO|IyPTd{NUi5
BAF3 NWjvNY9VS3m2b4TvfIlkKEG|c3H5 MWG0PEBp MUPEUXNQ NXT5O|dES3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhSkGIMzDj[YxteyCneIDy[ZN{cW6pIGTlcE1CVEtid3n0bEBKSzVyIH;mJFAvOTlizszN NYjNcWNGOjF3N{K1PFk>
3T3 MmH2SpVv[3Srb36gRZN{[Xl? NEHZdXQyKGh? M1;ZZ2ROW09? MkW1TY5pcWKrdHnvckBw\iCUT16gZZN{\XO|ZXSgZZMh\3Kxd4ToJIZi[3Sxcj3pcoR2[2WmIHH1eI9xcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEig{txO NHuydZUzOThzMkSxOC=>
3T3-E NViySHVKTnWwY4Tpc44hSXO|YYm= NXLFOnB{OSCq M4[xPGROW09? NYLBfZoxUW6qaXLpeIlwdiCxZjDUTWUzKGG|c3Xzd4VlKGe{b4f0bEBn[WO2b4KtbY5lfWOnZDDheZRweGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkS0PEDPxE1? NGrnd5IzOThzMkSxOC=>
A549 M{fkWmtqdmG|ZTDBd5NigQ>? Mn34NUBp NXXtSJkyTE2VTx?= MoX5TY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCClLV3FWEBscW6jc3Wg[ZhxemW|c3XkJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gTGdHNWmwZIXj[YQh[XW2b4Doc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNE4xODhizszN NUPYW3AyOjF6MUK0NVQ>
BAF3-BCL NEjvN21HfW6ldHnvckBCe3OjeR?= M2LycFEhcA>? M2jDN2ROW09? NF;zbGhKdmirYnn0bY9vKG:oIFHCUEBie3Onc4Pl[EBieyCpcn;3eIgh\mGldH;yMYlv\HWlZXSgZZV1d3Cqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMT6xOVkh|ryP M1fVWVIyQDF{NEG0
HEK293 MofLSpVv[3Srb36gRZN{[Xl? MXuxJIg> NVy0bYdlTE2VTx?= NIrve2ZKdmirYnn0bY9vKG:oIFHYUEBie3Onc4Pl[EBieyCpcn;3eIgh\mGldH;yMYlv\HWlZXSgZZV1d3Cqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMD6yPVQh|ryP NHn1Z2UzOThzMkSxOC=>
HEK293 NF;qZ5BHfW6ldHnvckBCe3OjeR?= MVWxJIg> NFi3[m5FVVOR NWrlRYxwUW6qaXLpeIlwdiCxZjDJVkBie3Onc4Pl[EBieyCpcn;3eIgh\mGldH;yMYlv\HWlZXSgZZV1d3Cqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMj64PFch|ryP M2PCOVIyQDF{NEG0
Jurkat MlHESpVv[3Srb36gRZN{[Xl? M4TGN|EhcA>? MlLOSG1UVw>? M{f6TGlvcGmkaYTpc44hd2ZiTFPLJIF{e2W|c3XkJIF{KGe{b4f0bEBn[WO2b4KtbY5lfWOnZDDheZRweGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iB{Lke0NUDPxE1? M1LGeFIyQDF{NEG0
KARPAS299 NGjFTYdMcW6jc3WgRZN{[Xl? M{Ht[FEhcA>? MnLrSG1UVw>? M4rSZmlvcGmkaYTpc44hd2ZiQVzLJIF{e2W|c3XkJIF{KGe{b4f0bEBn[WO2b4KtbY5lfWOnZDDheZRweGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCyJO69VQ>? NEHHNJAzOThzMkSxOC=>
PAE M3L1WWZ2dmO2aX;uJGF{e2G7 M1zQR|EhcA>? NELhV4xFVVOR NHXtV2xKdmirYnn0bY9vKG:oIGTST2Ih[XO|ZYPz[YQh[XNiZ4Lve5RpKG[jY4Tvdk1qdmS3Y3XkJIF2fG:yaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIECuN|k6KM7:TR?= M2HiNVIyQDF{NEG0
BAF3 MUjGeY5kfGmxbjDBd5NigQ>? M4\hNVIuOyCm M1jySmROW09? MnzTTY5pcWKrdHnvckBw\iCWRVyt[pV{\WRiaX7zeYxqdiC{ZXPldJRweiCneIDy[ZN{\WRid3n0bEBKSzVyIH;mJFEvPjR|IN88US=> MojtNlM4PDJ{NUK=
KARPAS299 M4e2cGN6fG:2b4jpZ{BCe3OjeR?= MknONk0{KGR? M{fwdGROW09? MofZTWM2OD1yLkC2OFIh|ryP NVe3[ZV6OjN5NEKyOVI>
EBC1 M1vqdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\tNJE4OiCq MXrEUXNQ NHjPdXVKSzVyPUCuNFI{KM7:TR?= Ml3LNlM6QTN|Mki=
HCT116 NYS1U5NJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYi3NkBp M3PoR2ROW09? M2DMXWlEPTB;MUSuPFIh|ryP NEjBd2YzOzl7M{OyPC=>
MCF7 M1zoN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnDO|IhcA>? MX7EUXNQ M2f2TmlEPTB;OT61PEDPxE1? MnW1NlM6QTN|Mki=
MDA-MB-231 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3SwRVczKGh? NFL3UnVFVVOR Ml;CTWM2OD1zMD64JO69VQ>? NEfYO2EzOzl7M{OyPC=>
MKN45 NGe4UY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWe5WXNzPzJiaB?= NGLRcllFVVOR MojWTWM2OD1yLkCxN{DPxE1? NGmxVpEzOzl7M{OyPC=>
NCI-H441 M{W0Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vy[VczKGh? Mli2SG1UVw>? NUOzO2REUUN3ME2xO{4zPSEQvF2= MVmyN|k6OzN{OB?=
NCI-H661 NYL2WnFzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGT0U4M4OiCq MX\EUXNQ Mn;xTWM2OD1zMT60O{DPxE1? NWn3eW5XOjN7OUOzNlg>
SK-MEL-28 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;0S2ZVPzJiaB?= MnLrSG1UVw>? NHfVUlRKSzVyPUGwMlk4KM7:TR?= MWeyN|k6OzN{OB?=
SKOV3 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLxRmE5PzJiaB?= M1OxUGROW09? NIO4fJpKSzVyPUGyMlg2KM7:TR?= NWTBeVVmOjN7OUOzNlg>
SNU5 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TtOlczKGh? NWG1c4JwTE2VTx?= MkLaTWM2OD1yLkCxOkDPxE1? MlToNlM6QTN|Mki=
NCI-H2228 NFPvTXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHvT5A4OiCq MYLEUXNQ M2TpbGlvcGmkaYTpc44hd2ZiQVzLMYZ2e2mxbjDkdol3\W5iY3XscEBxem:uaX\ldoF1cW:wIIfpeIghUUN3MDDv[kAxNjFzODFOwG0> NI[yW48zPDR|MkmwPS=>
NCI-H3122 M1K5XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLrO|IhcA>? MoiwSG1UVw>? MVPJcohq[mm2aX;uJI9nKEGOSz3meZNqd25iZILpeoVvKGOnbHygdJJwdGmoZYLheIlwdiC5aYToJGlEPTBib3[gNE4yODhizszN MnvCNlQ1OzJ7MEm=
NCI-H3122 MmDXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\PRlVHPzJiaB?= MoHuSG1UVw>? NEPHeHhKdmirYnn0bY9vKG:oIFHMT{1nfXOrb36g[JJqfmWwIHPlcIwheHKxbHnm[ZJifGmxbjDpckBpfW2jbjDOR2kuUDNzMkKgZ4VtdHNiaHHyZo9zcW6pIFHMT{BIOTJ4OVGgcZV1[W62IIfpeIghUUN3MDDv[kAxNjZ{MzFOwG0> M1mybVI1PDN{OUC5
NCI-H3122 MnPwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{X3ZVczKGh? MVjEUXNQ NG\WNlBKdmirYnn0bY9vKG:oIFHMT{1nfXOrb36g[JJqfmWwIHPlcIwheHKxbHnm[ZJifGmxbjDpckBpfW2jbjDOR2kuUDNzMkKgZ4VtdHNiaHHyZo9zcW6pIFHMT{BNOTF7Nl2gcZV1[W62IIfpeIghUUN3MDDv[kAxNjh|ODFOwG0> NIfLWlYzPDR|MkmwPS=>
NIH-3T3 NUXQ[VIyU2mwYYPlJGF{e2G7 NVTsOXBnOSCq MmDNSG1UVw>? NFzsfVNKdmirYnn0bY9vKG:oIHj1cYFvKHerbHSgeJlx\SCHTVy0MYZ2e2WmIFHMT{BmgHC{ZYPz[YQh[XO|ZYPz[YQh[XNicHjvd5Bpd3K7bHH0[YQhSUyNIHzleoVtKHerdHigTWM2OCCxZjCwMlA5KM7:TR?= M37CcFI1PDN{OUC5
NIH-3T3 MXvLbY5ie2ViQYPzZZk> M{DR[lEhcA>? NYfoNms5TE2VTx?= M4C3dmlvcGmkaYTpc44hd2ZiaIXtZY4hTU2OND3meZNm\CCDTFugS|EzPjmDIH31eIFvfCCneIDy[ZN{\WRiYYPz[ZN{\WRiYYOgdIhwe3Cqbz3BUGshdGW4ZXyge4l1cCCLQ{WwJI9nKDBwNkC1JO69VQ>? NHzQcI8zPDR|MkmwPS=>
NIH-3T3 MojBT4lv[XOnIFHzd4F6 MUGxJIg> MormSG1UVw>? M3TPZ2lvcGmkaYTpc44hd2ZiaIXtZY4hTU2OND3meZNm\CCDTFugV|EzOD[\IH31eIFvfCCneIDy[ZN{\WRiYYPz[ZN{\WRiYYOgdIhwe3Cqbz3BUGshdGW4ZXyge4l1cCCLQ{WwJI9nKDBwNkK2JO69VQ>? NY[wOpRwOjR2M{K5NFk>
NIH-3T3 NVrrTnJKU2mwYYPlJGF{e2G7 MV6xJIg> NILkZVZFVVOR MVzJcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIFyxNVk3VSCvdYThcpQh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IIDoc5NxcG9vQVzLJIxmfmWuIIfpeIghUUN3MDDv[kAxNjh2MzFOwG0> MX:yOFQ{OjlyOR?=
NIH-3T3 MkjsT4lv[XOnIFHzd4F6 MYixJIg> MkPYSG1UVw>? NY\0VHo1UW6qaXLpeIlwdiCxZjDoeY1idiCHTVy0MYZ2e2WmIFHMT{BNOTF3MmKgcZV1[W62IHX4dJJme3OnZDDhd5Nme3OnZDDhd{BxcG:|cHjvMWFNUyCuZY\lcEB4cXSqIFnDOVAhd2ZiMT6wNlYh|ryP NW\0fFVJOjR2M{K5NFk>
BAF3 MlHzSpVv[3Srb36gRZN{[Xl? Mk\FO|IhcA>? MmnXSG1UVw>? NH63bndKdmirYnn0bY9vKG:oIF7QUU9CVEtidILhcpNn\WO2ZXSgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjD3bZRpKEmFNUCgc4YhOC5yNUGg{txO NV;zdZZEOjR2Nki2N|I>
BAF3 M1;0WWN6fG:2b4jpZ{BCe3OjeR?= NYC1fIdnPzJiaB?= MUnEUXNQ MVPJR|UxRTBwOUig{txO MkXCNlQ1Pjh4M{K=
NIH-3T3 MXLLbY5ie2ViQYPzZZk> NGDoOHoyKGh? MUjJcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIF[xNVc1VCCvdYThcpQh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IIDoc5NxcG9vQVzLJIxmfmWuIIfpeIghUUN3MDDv[kAxNjF4NTFOwG0> MWGyOFgyQTFzNh?=
NIH-3T3 MkPlT4lv[XOnIFHzd4F6 NHf6UXkyKGh? MX3Jcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIFOxNVU3YSCvdYThcpQh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IIDoc5NxcG9vQVzLJIxmfmWuIIfpeIghUUN3MDDv[kAxNjR5ODFOwG0> Mn7WNlQ5OTlzMU[=
NIH-3T3 NW\0fZIzU2mwYYPlJGF{e2G7 MVuxJIg> M3\mXGlvcGmkaYTpc44hd2ZiaIXtZY4hTU2OND3meZNm\CCDTFugS|EzODKUIH31eIFvfCCneIDy[ZN{\WRiYYPz[ZN{\WRiYYOgdIhwe3Cqbz3BUGshdGW4ZXyge4l1cCCLQ{WwJI9nKDFwMUS4JO69VQ>? MX[yOFgyQTFzNh?=
NIH-3T3 M2XFPGtqdmG|ZTDBd5NigQ>? MoTaNUBp M{PQSmlvcGmkaYTpc44hd2ZiaIXtZY4hTU2OND3meZNm\CCDTFugNVE2OVSrboOgcZV1[W62IHX4dJJme3OnZDDhd5Nme3OnZDDhd{BxcG:|cHjvMWFNUyCuZY\lcEB4cXSqIFnDOVAhd2ZiMz6wN|kh|ryP NWO4fXV[OjR6MUmxNVY>
KARPAS299 MlTBT4lv[XOnIFHzd4F6 NHfxOFk6OCCvaX6= NFLLZ5pFVVOR NH[2WlZKdmirYnn0bY9vKG:oIF7QUU1nfXOnZDDBUGsheGixc4Doc5J6dGG2aX;uJIV5eHKnc4Pl[EB4cXSqIFnDOVAhd2ZiMD6xNUDPxE1? NV3oe5ZsOjR7MEC3OVA>
MKN 45 MnO4T4lv[XOnIFHzd4F6 MmLsNUBp M1mzfGROW09? NYXQdJZ3UW6qaXLpeIlwdiCxZjDjMW1mfCCyaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIECuNFIh|ryP MWSyOFkxODd3MB?=
A549 MkTYR5l1d3SxeHnjJGF{e2G7 Mk[4OFghcA>? NXfqRppjTE2VTx?= NUj6N5o3UUN3MDDv[kA1NjB6NDFOwG0> NV7KR4I2OjR7MEC4N|A>
NCI-H1975 NIHKb4dEgXSxdH;4bYMhSXO|YYm= NWnwb2c1PDhiaB?= NVLDZpI{TE2VTx?= M4XqfGlEPTBib3[gO{42PTFizszN MkXPNlQ6ODB6M{C=
NCI-H1993 M1TjPWN6fG:2b4jpZ{BCe3OjeR?= MVG0PEBp MkjjSG1UVw>? Mn;yTWM2OCCxZjCwMlA3OSEQvF2= NEW5[GczPDlyMEizNC=>
NCI-H1993 NYXhd45oSXCxdH;zbZMhSXO|YYm= MY[xJO69VQ>? NEDOWFUzPCCq NXTZO5BWTE2VTx?= MojX[I9meyCwb4SgbY5lfWOnIHHwc5B1d3Orcx?= NVu4N5hDOjR7MEC4N|A>
NIH-3T3 NILpOlVEgXSxdH;4bYMhSXO|YYm= MnLtOFghcA>? M2nYZWROW09? MYHJR|UxKG:oIECuN|Y1KM7:TR?= MnrINlQ6ODB6M{C=
EBC1 MkLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDrenY4OiCq NXjP[XdzTE2VTx?= MXrJR|UxKG:oIECuNFA3QSEQvF2= NUfvNINrOjR7MEC4N|E>
KARPAS299 M2XGbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\6O|IhcA>? MnewSG1UVw>? Ml\xTWM2OCCxZjCwMlIh|ryP Mor6NlQ6ODB6M{G=
NB1 NFP6c4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PwXWlEPTB;OUGuPVghdk1? NFXxPXRUSU6JRWK=
NCI-SNU-5 M2DxV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfKTWM2OD1zMEWuO|Uhdk1? NWDneZNjW0GQR1XS
SR MmjYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTF{Nj6zNUBvVQ>? NFu5NYJUSU6JRWK=
SF539 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmf2TWM2OD1{MESuNlQhdk1? MX3TRW5ITVJ?
SU-DHL-1 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEW4dVBKSzVyPUOzOk45OiCwTR?= M1;rOXNCVkeHUh?=
SCC-3 Mlf2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTN3Nj63OkBvVQ>? NVTheohbW0GQR1XS
DEL MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXLXpVKSzVyPUO2PU46KG6P Ml\HV2FPT0WU
CTV-1 M1\OUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTV7Nj60PEBvVQ>? Mn;FV2FPT0WU
EM-2 NX[xdpdET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7VWXZiUUN3ME22NFEvOzRibl2= NGrWVpNUSU6JRWK=
MHH-CALL-2 MoDBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPvTGJzUUN3ME22PFIvPTdibl2= MYDTRW5ITVJ?
KM12 MlvLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\oXGlEPTB;N{C2Mlkhdk1? MWXTRW5ITVJ?
KINGS-1 NH3hOZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTd2OT63OUBvVQ>? M{DoOnNCVkeHUh?=
MEG-01 M4nUUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTh3Nz62OkBvVQ>? MoToV2FPT0WU
BV-173 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLkTWM2OD1zLkC1PVk4KM7:TR?= M4\5V3NCVkeHUh?=
LAMA-84 NEPjcJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPZd5JGUUN3ME2xMlM5Ojh{IN88US=> MV\TRW5ITVJ?
KARPAS-299 MmfZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTKTWM2OD1zLkSwPFYyKM7:TR?= NGfJNVlUSU6JRWK=
K-562 NFqzfXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2i3RmlEPTB;MT63NlI3QSEQvF2= M3z5e3NCVkeHUh?=
SK-LMS-1 M335Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvkd3JKSzVyPUGuO|Y5PjdizszN M3rITHNCVkeHUh?=
MOLT-16 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTsTWM2OD1zLkm1OVc2KM7:TR?= MWXTRW5ITVJ?
CMK MnKyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXv3Ro57UUN3ME2xMlk3OTV7IN88US=> NVjFXVd7W0GQR1XS
ST486 NGHiUmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTJwNEOwO|Mh|ryP NWjnW5ZVW0GQR1XS
CI-1 M3naOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLJTWM2OD1{LkS5OlU6KM7:TR?= MknsV2FPT0WU
KP-N-RT-BM-1 M2Xnd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTJwN{CxNlIh|ryP MVLTRW5ITVJ?
ALL-PO NWrYN49nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\U[4lKSzVyPUOuNVgzODdizszN NUfVVWt4W0GQR1XS
KS-1 NHvYfHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDBTWM2OD1|LkKxNlI2KM7:TR?= NYTtSZVNW0GQR1XS
Becker MkP2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LFTmlEPTB;ND6yN|k{KM7:TR?= M1T4bHNCVkeHUh?=
GDM-1 MnLKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnZTWM2OD12LkK0OlE4KM7:TR?= M1H1W3NCVkeHUh?=
BC-1 NIqx[YlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTWTlc1UUN3ME20MlQ6Ojd5IN88US=> NEW2SYNUSU6JRWK=
NB14 NF3SV4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjZd5VKSzVyPUSuPFM2OjRizszN NX7rNXg2W0GQR1XS
NOS-1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrtemJKSzVyPUWuN|M5PzRizszN MX3TRW5ITVJ?
MZ1-PC M3PGb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HWXWlEPTB;NT64NlE2OSEQvF2= M{LvZnNCVkeHUh?=
A498 NFvROZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4Pz[WlEPTB;Nj6wPFQ4OyEQvF2= M2jiU3NCVkeHUh?=
EW-16 NXvFd49{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTZwM{e3O|Mh|ryP M{foPXNCVkeHUh?=
NALM-6 M{LKW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrrTWM2OD14Lk[4N|g4KM7:TR?= NVn4bWY6W0GQR1XS
EB-3 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\aTXdKSzVyPUeuNFczOzNizszN MUXTRW5ITVJ?
697 NW\heZptT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVK3U2h4UUN3ME25MlI1OzJ7IN88US=> NGjh[3BUSU6JRWK=
Ramos-2G6-4C10 NX7GRlB1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HwPWlEPTB;OT61PVg1OiEQvF2= MVzTRW5ITVJ?
KNS-81-FD M4\PSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjrU3YyUUN3ME25MlY6PjV|IN88US=> M3PqNnNCVkeHUh?=
HUTU-80 M{DYRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXi1SJNVUUN3ME25Mlc1PjR{IN88US=> MVzTRW5ITVJ?
LS-411N NUfVb4JUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTFyLkC1Olch|ryP MWXTRW5ITVJ?
RPMI-8402 NV;5XYtVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjOOJNKSzVyPUGwMlEyPiEQvF2= NInOe|RUSU6JRWK=
KU812 M3vSV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTITWM2OD1zMD6yPVkyKM7:TR?= NWLWT4dUW0GQR1XS
EW-1 MoLFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfTTWM2OD1zMD60OFI2KM7:TR?= MorDV2FPT0WU
HC-1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;sNGlEPTB;MUCuOFg1PCEQvF2= MVnTRW5ITVJ?
NB69 NVHYT4lIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjJTGNoUUN3ME2xNE42ODR|IN88US=> Mln2V2FPT0WU
MFH-ino NVi5b4NKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTFyLkizNFMh|ryP NX7JXItHW0GQR1XS
CCRF-CEM MmHSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTFzLkW5O{DPxE1? MYnTRW5ITVJ?
SK-N-DZ NHK4bmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvCTWM2OD1zMj6wOFM3KM7:TR?= M1G1dXNCVkeHUh?=
NCI-H720 M3mz[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTF{LkG3NFUh|ryP NXy0RW16W0GQR1XS
HCC1187 M1LuXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnNdFd4UUN3ME2xNk4zODRzIN88US=> M1XifnNCVkeHUh?=
IST-SL2 NIG3b3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLzPIdKSzVyPUGyMlQ5PzJizszN MYnTRW5ITVJ?
KE-37 NXTwNVVbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTF{Lke5OlYh|ryP MXHTRW5ITVJ?
HCC1599 MmO2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo[yTWM2OD1zMj65NFY6KM7:TR?= MV;TRW5ITVJ?
A4-Fuk NFf0c|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjSZXdKUUN3ME2xNk46PTh4IN88US=> MUnTRW5ITVJ?
NKM-1 M2TnR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTF|LkK5NlUh|ryP MkfvV2FPT0WU
BE-13 MontS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTF|Lke5PFkh|ryP MoLMV2FPT0WU
MV-4-11 NF7Ub3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV24e4ZHUUN3ME2xOE4xOzJ2IN88US=> MYPTRW5ITVJ?
OPM-2 M3LnSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXm5bGc2UUN3ME2xOE41ODh3IN88US=> M4PYTXNCVkeHUh?=
KARPAS-422 NHH4V3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fiN2lEPTB;MUSuOVEzPiEQvF2= NETlZ4VUSU6JRWK=
RPMI-8226 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUT0WYQ{UUN3ME2xOE45QTF3IN88US=> M4n1WHNCVkeHUh?=
KARPAS-45 M4fITWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXVcFlKSzVyPUG1Mlc4OTZizszN MYjTRW5ITVJ?
SK-PN-DW M3TjNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHRN2ZIUUN3ME2xOU45PjNzIN88US=> NX7EWIxMW0GQR1XS
LC-2 M1vEemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTF4LkG1NFYh|ryP MmfsV2FPT0WU
NCI-H1648 M{PpPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLHTWM2OD1zNj6yOVQh|ryP NV3EXlF4W0GQR1XS
RL95-2 M{fmWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTF4LkO5O|gh|ryP MXzTRW5ITVJ?
KNS-42 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnf0TWM2OD1zNj63Nlc1KM7:TR?= NFvLVXNUSU6JRWK=
RPMI-6666 NVzHNWV{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml60TWM2OD1zNj65NlEyKM7:TR?= NFq4V41USU6JRWK=
SIG-M5 M2DNdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVi4WG1{UUN3ME2xO{4yQTB|IN88US=> NH;ObZpUSU6JRWK=
VA-ES-BJ MmezS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV:5fnN5UUN3ME2xO{44PDVzIN88US=> NFrNb3hUSU6JRWK=
MONO-MAC-6 NUDpVFBZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfZUmNOUUN3ME2xO{46OzF{IN88US=> MkPYV2FPT0WU
LAN-6 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4KyNWlEPTB;MUiuO|U2PyEQvF2= NH3rZZJUSU6JRWK=
A388 M{\Pd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTF7LkOwOVkh|ryP MkPMV2FPT0WU
SK-NEP-1 Mn;ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTJyLkKxN|Ih|ryP NGi4b5RUSU6JRWK=
TE-10 NYDKU3RLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmj6TWM2OD1{MD61NlIyKM7:TR?= MYjTRW5ITVJ?
HL-60 M2fnemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTJyLkmwPVkh|ryP MkHxV2FPT0WU
MC116 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFzrVGRKSzVyPUKxMlczOjFizszN MnjaV2FPT0WU
SW962 NGr0[ZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVewTlRxUUN3ME2yNU44QTF3IN88US=> NIjSTYZUSU6JRWK=
NOMO-1 M1jQSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jzXWlEPTB;MkKuOlU3PCEQvF2= NF;FVG5USU6JRWK=
CTB-1 Mn3DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nuZWlEPTB;MkKuPFY4OSEQvF2= M4r4TnNCVkeHUh?=
MRK-nu-1 NF7LSXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfTdWQxUUN3ME2yNk46ODd2IN88US=> MY\TRW5ITVJ?
GR-ST NWDJZVBPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7zTWM2OD1{Mz63OkDPxE1? NHf5XYxUSU6JRWK=
HH MnXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTJ2LkCwN{DPxE1? MXTTRW5ITVJ?
NCI-H1963 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofyTWM2OD1{ND6wO|gzKM7:TR?= MYPTRW5ITVJ?
QIMR-WIL M2T5Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTJ2Lki3O|Ih|ryP MXLTRW5ITVJ?
CGTH-W-1 MmjpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXCfZZRUUN3ME2yOU4xPzJ|IN88US=> NGPJSI9USU6JRWK=
LP-1 NFf2VnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\EZZhRUUN3ME2yOU43PTVzIN88US=> Mn3iV2FPT0WU
NCI-H748 NInydJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXCW|FKSzVyPUK2MlUyOzdizszN MUjTRW5ITVJ?
PF-382 NVrBWHpqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnhTYlQUUN3ME2yO{4zOjJ|IN88US=> NVPBVokzW0GQR1XS
ATN-1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnPVmNKSzVyPUK3MlM4OzJizszN Mk\NV2FPT0WU
L-540 NGn2T3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NED3SJBKSzVyPUK3MlY1PTlizszN M{nqNXNCVkeHUh?=
LXF-289 M1XKPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1P5XGlEPTB;MkeuO|UyQSEQvF2= NV32VHNbW0GQR1XS
LS-513 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2H3U2lEPTB;MkiuNVgxPyEQvF2= MnfkV2FPT0WU
NCI-H1581 M2rkXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfSTWM2OD1|MD6zPVc3KM7:TR?= M3XNfnNCVkeHUh?=
ES6 M2fidWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPpTWM2OD1|MD62PFk6KM7:TR?= NVjGXWFbW0GQR1XS
SW982 MlnvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWG1XIpSUUN3ME2zNE45PTZ4IN88US=> M1LFbnNCVkeHUh?=
DOHH-2 NGjFR4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LSW2lEPTB;M{GuOVg6OyEQvF2= M{HKXXNCVkeHUh?=
DB M1\4ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rMW2lEPTB;M{OuPVQ{OSEQvF2= MUTTRW5ITVJ?
MPP-89 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\zbFlKSzVyPUO0MlE4PTZizszN M2fTc3NCVkeHUh?=
LB831-BLC M13IWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nXbGlEPTB;M{SuOVE5PCEQvF2= MVzTRW5ITVJ?
NB5 M1TWTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHMW2hVUUN3ME2zOE45PTN3IN88US=> MYLTRW5ITVJ?
GB-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTN3LkC0Olkh|ryP NV32cJJ2W0GQR1XS
TE-15 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXxTWM2OD1|NT6yNlM5KM7:TR?= MofoV2FPT0WU
LC4-1 NE\4U2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX60NVNWUUN3ME2zOU4{QDR5IN88US=> MWrTRW5ITVJ?
NCI-H747 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTN4LkGzOlkh|ryP MW\TRW5ITVJ?
NTERA-S-cl-D1 NHzsXpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLITWM2OD1|OD63N|Q4KM7:TR?= MXzTRW5ITVJ?
SK-MM-2 MmXhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTRyLkGxOFYh|ryP NF\lTGFUSU6JRWK=
TGW NW\HV2pJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3kdGdZUUN3ME20NU4xPTZ|IN88US=> M1XXRnNCVkeHUh?=
ONS-76 Ml\wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHBfHI2UUN3ME20Nk41QDh|IN88US=> NVjRe5lQW0GQR1XS
CPC-N MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXNW5dKSzVyPUSyMlk6PzFizszN MnrtV2FPT0WU
ES4 NV7sbnhWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fNdGlEPTB;NESuOFE2OyEQvF2= NHHVXW1USU6JRWK=
Daudi MkWxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDMUFJKSzVyPUS1MlA5OjdizszN NGOwVoJUSU6JRWK=
MOLT-4 MkXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjLb5lKSzVyPUS1MlA5PTNizszN NH[xepBUSU6JRWK=
HT-144 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mke1TWM2OD12Nj63NlYh|ryP MlfFV2FPT0WU
SW872 NF\qSmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnjVm5KSzVyPUS4MlE6OzNizszN MmfnV2FPT0WU
D-283MED NFLaNZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnO0TWM2OD12OD6zOVQzKM7:TR?= MVPTRW5ITVJ?
NCI-H2126 NGLDVmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTR6Lki0O|Yh|ryP MWPTRW5ITVJ?
NCI-SNU-16 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTR7LkKxOFMh|ryP MmfaV2FPT0WU
CESS Mo\HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MojjTWM2OD12OT61NFg5KM7:TR?= M2HsT3NCVkeHUh?=
A101D MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HKSWlEPTB;NEmuPVc{PiEQvF2= NIiwe5hUSU6JRWK=

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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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Rating
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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Rating
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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Rating
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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Rating
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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Rating
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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