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

高品質保証

文献中の引用(68)

カスタマーフィードバック(11)

MSDS

製品説明

  • Compare c-Met Inhibitors
    c-Met製品生物活性の比較
  • 研究分野
  • Combination Therapy
    併用療法
  • Crizotinib (PF-02341066)のメカニズム

製品の説明

生物活性

製品説明 Crizotinib (PF-02341066)は一種の有効なc-MetとALK阻害剤で、細胞試験でIC50値が11 nMと24 nMです。
ターゲット c-Met ALK
IC50 11 nM 24 nM [1]
In vitro試験 PF-2341066 displays similar potency against c-Met phosphorylation in mIMCD3 mouse or MDCK canine epithelial cells with IC50 of 5 nM and 20 nM, respectivly. PF-2341066 shows improved or similar activity against NIH3T3 cells engineered to express c-Met ATP-binding site mutants V1092I or H1094R or the P-loop mutant M1250T with IC50 of 19 nM, 2 nM and 15 nM, respectively, compared with NIH3T3 cells expressing wild-type receptor with IC50 of 13 nM. In contrast, a marked shift in potency of PF-2341066 is observed against cells engineered to express c-Met activation loop mutants Y1230C and Y1235D with IC50 of 127 nM and 92 nM, respectively, compared with wild-type receptor. PF-2341066 also potently prevents the phosphorylation of c-Met in NCI-H69 and HOP92 cells, with IC50 of 13 nM and 16 nM, respectively, which express the endogenous c-Met variants R988C and T1010I, respectively. PF-2341066 is >1,000-fold selective for the VEGFR2 and PDGFRβ RTKs, >250-fold selective for IRK and Lck, and ∼40- to 60-fold selective for Tie2, TrkA, and TrkB, all compared with c-Met. PF-2341066 is 20- to 30-fold selective for RON and Axl RTKs. In contrast, PF-2341066 shows a near-equivalent IC50 of 24 nM against the nucleophosmin (NPM)-anaplastic lymphoma kinase (ALK) oncogenic fusion variant of the ALK RTK expressed by the KARPAS299 human anaplastic large cell lymphoma (ALCL) cell line. PF-2341066 inhibits c-Met–dependent neoplastic phenotypes of cancer cells and angiogenic phenotypes of endothelial cells. PF-2341066 suppresses human GTL-16 gastric carcinoma cell growth with IC50 of 9.7 nM. PF-2341066 induces apoptosis in GTL-16 cells with IC50 of 8.4 nM. PF-2341066 inhibits HGF-stimulated human NCI-H441 lung carcinoma cell migration and invasion with IC50 of 11 nM and 6.1 nM, respectively. PF-2341066 inhibits MDCK cell scattering with IC50 of 16 nM. PF-2341066 prevents HGF-stimulated c-Met phosphorylation, cell survival, and Matrigel invasion with IC50 of 11 nM, 14 nM and 35 nM, respectively. In addition, PF-2341066 prevents serum-stimulated HMVEC branching tubulogenesis (formation of vascular tubes) in fibrin gels. [1] PF-2341066 also potently inhibits NPM-ALK phosphorylation in Karpas299 or SU-DHL-1 ALCL cells with an IC50 of 24 nM. PF-2341066 potently prevents cell proliferation, which is associated with G(1)-S-phase cell cycle arrest and induction of apoptosis in ALK-positive ALCL cells with IC50 of 30 nM, but not ALK-negative lymphoma cells. [2] Besides, PF-2341066 prevents osteosarcoma behavior associated with primary tumor growth (i.e., proliferation and survival) as well as metastasis (eg, invasion and clonogenicity). [3]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
BAF3 MlHBR5l1d3SxeHnjJGF{e2G7 M{XRc|Q5KGh? MoXRSG1UVw>? MYTDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDCRWY{KGOnbHzzJIV5eHKnc4PpcochSUyNIF[xNVc1VCCvdYThcpQh[2:neIDy[ZN{cW6pIFXNUFQhf2m2aDDJR|UxKG:oIECuOlIh|ryP MlyzNlE2PzJ3OEm=
BAF3 M1PJRWN6fG:2b4jpZ{BCe3OjeR?= M13jUFQ5KGh? MkPDSG1UVw>? NV\vS4pDS3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhSkGIMzDj[YxteyCneIDy[ZN{cW6pIFHMT{BNOTF7Nl2gcZV1[W62IHPv[ZhxemW|c3nu[{BGVUx2IIfpeIghUUN3MDDv[kAzNjJizszN MXWyNVU4OjV6OR?=
BAF3 NH\1[YZEgXSxdH;4bYMhSXO|YYm= MVK0PEBp MnjRSG1UVw>? NEXFVHFEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBDSUZ|IHPlcIx{KGW6cILld5NqdmdiRV3MOE1CVEtid3n0bEBKSzVyIH;mJFAvOjhizszN NWfUe4tnOjF3N{K1PFk>
Kelly MVnDfZRwfG:6aXOgRZN{[Xl? MmXiSG1UVw>? NXn4[olJS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hU2WubImgZ4VtdHNiZYjwdoV{e2mwZzDBUGshTjFzN{TMJI12fGGwdDD3bZRpKEmFNUCgc4YhOC52MjFOwG0> MkPTNlE2PzJ3OEm=
SH-SY5Y MU\DfZRwfG:6aXOgRZN{[Xl? MVnEUXNQ MWnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTTE1UYTW\IHPlcIx{KGW6cILld5NqdmdiQVzLJGYyOTd2TDDteZRidnRid3n0bEBKSzVyIH;mJFAvPTNizszN NXzTUphyOjF3N{K1PFk>
SMS-KCN MUjDfZRwfG:6aXOgRZN{[Xl? M{ntcmROW09? M3vwdWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNOWy2NQ16gZ4VtdHNiZYjwdoV{e2mwZzDBUGshWjF{N{XRJI12fGGwdDD3bZRpKEmFNUCgc4YhOC57MTFOwG0> NEjNU|QzOTV5MkW4PS=>
BAF3 MYLDfZRwfG:6aXOgRZN{[Xl? NYjTWZlJPDhiaB?= MV3EUXNQ M{fhbGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KG2xdYPlJGJCTjNiY3XscJMh\XiycnXzd4lv\yCWZXytRWxMKHerdHigTWM2OCCxZjCwMlE6KM7:TR?= MYmyNVU4OjV6OR?=
3T3 NHGzN2RHfW6ldHnvckBCe3OjeR?= NY[3[2Q4OSCq MnS5SG1UVw>? Mlj2TY5pcWKrdHnvckBw\iCUT16gZZN{\XO|ZXSgZZMh\3Kxd4ToJIZi[3Sxcj3pcoR2[2WmIHH1eI9xcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEig{txO MkC0NlE5OTJ2MUS=
3T3-E M4fpeGZ2dmO2aX;uJGF{e2G7 NXToNG02OSCq NUjpcIlGTE2VTx?= NWXPd21GUW6qaXLpeIlwdiCxZjDUTWUzKGG|c3Xzd4VlKGe{b4f0bEBn[WO2b4KtbY5lfWOnZDDheZRweGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkS0PEDPxE1? M4L3UlIyQDF{NEG0
A549 MWPLbY5ie2ViQYPzZZk> NEfvXGQyKGh? Ml\zSG1UVw>? MmrRTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCClLV3FWEBscW6jc3Wg[ZhxemW|c3XkJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gTGdHNWmwZIXj[YQh[XW2b4Doc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNE4xODhizszN NVm0b4xMOjF6MUK0NVQ>
BAF3-BCL NGPueW5HfW6ldHnvckBCe3OjeR?= NVXUXoh1OSCq MW\EUXNQ NV3TRWZTUW6qaXLpeIlwdiCxZjDBRmwh[XO|ZYPz[YQh[XNiZ4Lve5RpKG[jY4Tvdk1qdmS3Y3XkJIF2fG:yaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIEGuNVU6KM7:TR?= MWCyNVgyOjRzNB?=
HEK293 NYm0b2ZCTnWwY4Tpc44hSXO|YYm= NIfYRlkyKGh? MUjEUXNQ MXzJcohq[mm2aX;uJI9nKEG[TDDhd5Nme3OnZDDhd{Boem:5dHig[oFkfG:{LXnu[JVk\WRiYYX0c5Bpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5{OUSg{txO MmTXNlE5OTJ2MUS=
HEK293 NUWyR5FWTnWwY4Tpc44hSXO|YYm= NUTETYtzOSCq M2LacmROW09? M1\ubGlvcGmkaYTpc44hd2ZiSWKgZZN{\XO|ZXSgZZMh\3Kxd4ToJIZi[3Sxcj3pcoR2[2WmIHH1eI9xcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDJwOEi3JO69VQ>? MlTkNlE5OTJ2MUS=
Jurkat NF;iUJJHfW6ldHnvckBCe3OjeR?= MoHINUBp M2XIWGROW09? MX3Jcohq[mm2aX;uJI9nKEyFSzDhd5Nme3OnZDDhd{Boem:5dHig[oFkfG:{LXnu[JVk\WRiYYX0c5Bpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOi55NEGg{txO Mn3oNlE5OTJ2MUS=
KARPAS299 MontT4lv[XOnIFHzd4F6 MUWxJIg> M3PScGROW09? NFvONJpKdmirYnn0bY9vKG:oIFHMT{Bie3Onc4Pl[EBieyCpcn;3eIgh\mGldH;yMYlv\HWlZXSgZZV1d3Cqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMD6wNkDPxE1? NH\LfWozOThzMkSxOC=>
PAE NHfWXlFHfW6ldHnvckBCe3OjeR?= NWjzWYFtOSCq M3TVbWROW09? M4LRPGlvcGmkaYTpc44hd2ZiVGLLRkBie3Onc4Pl[EBieyCpcn;3eIgh\mGldH;yMYlv\HWlZXSgZZV1d3Cqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMD6zPVkh|ryP NYjaOnl3OjF6MUK0NVQ>
BAF3 Mle0SpVv[3Srb36gRZN{[Xl? NEPkc2EzNTNiZB?= MkC2SG1UVw>? MmDFTY5pcWKrdHnvckBw\iCWRVyt[pV{\WRiaX7zeYxqdiC{ZXPldJRweiCneIDy[ZN{\WRid3n0bEBKSzVyIH;mJFEvPjR|IN88US=> NUXVVZh7OjN5NEKyOVI>
KARPAS299 MnvNR5l1d3SxeHnjJGF{e2G7 M3jlflIuOyCm M4my[2ROW09? MYrJR|UxRTBwME[0NkDPxE1? MXWyN|c1OjJ3Mh?=
EBC1 MlfVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYW3NkBp NXrzWG5mTE2VTx?= NWnKe2lUUUN3ME2wMlAzOyEQvF2= Ml3HNlM6QTN|Mki=
HCT116 M{nQR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTFVFM4OiCq NX7ZSotFTE2VTx?= M4SwOmlEPTB;MUSuPFIh|ryP MnnsNlM6QTN|Mki=
MCF7 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFKwcVQ4OiCq MX\EUXNQ MY\JR|UxRTlwNUig{txO NGrpTYgzOzl7M{OyPC=>
MDA-MB-231 M1;Tc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWS3NkBp NH7ybINFVVOR MYrJR|UxRTFyLkig{txO NXXQSXZ7OjN7OUOzNlg>
MKN45 MmTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH73NZk4OiCq NInRVm9FVVOR NEPFdXdKSzVyPUCuNFE{KM7:TR?= MW[yN|k6OzN{OB?=
NCI-H441 NWf3[|c2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXf5[oJ[PzJiaB?= M3nSVWROW09? NUD4eHFnUUN3ME2xO{4zPSEQvF2= MX:yN|k6OzN{OB?=
NCI-H661 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUSxXIdkPzJiaB?= MWXEUXNQ MlfCTWM2OD1zMT60O{DPxE1? Ml\PNlM6QTN|Mki=
SK-MEL-28 MoToS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPwPIM4OiCq NYe0coFTTE2VTx?= NYTpdG9oUUN3ME2xNE46PyEQvF2= NITEeIkzOzl7M{OyPC=>
SKOV3 NV;4T3ptT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3kO|IhcA>? NEPGN|ZFVVOR M4X4b2lEPTB;MUKuPFUh|ryP MmTVNlM6QTN|Mki=
SNU5 M1WyNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVi3NkBp M{TSV2ROW09? NYXmS4Z[UUN3ME2wMlAyPiEQvF2= NYrCXVZ6OjN7OUOzNlg>
NCI-H2228 NEXLVG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHmzTY04OiCq NU\rUnFRTE2VTx?= NYDQdXZTUW6qaXLpeIlwdiCxZjDBUGsu\nW|aX;uJIRzcX[nbjDj[YxtKHC{b3zp[oVz[XSrb36ge4l1cCCLQ{WwJI9nKDBwMUG4JO69VQ>? NHrUXlYzPDR|MkmwPS=>
NCI-H3122 NELxUGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonuO|IhcA>? MV7EUXNQ NV7YSopXUW6qaXLpeIlwdiCxZjDBUGsu\nW|aX;uJIRzcX[nbjDj[YxtKHC{b3zp[oVz[XSrb36ge4l1cCCLQ{WwJI9nKDBwMUC4JO69VQ>? NHG4UYwzPDR|MkmwPS=>
NCI-H3122 NYLnUmgxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LD[lczKGh? NHrPR|FFVVOR MWDJcohq[mm2aX;uJI9nKEGOSz3meZNqd25iZILpeoVvKGOnbHygdJJwdGmoZYLheIlwdiCrbjDoeY1idiCQQ1mtTFMyOjJiY3XscJMhcGG{Yn;ybY5oKEGOSzDHNVI3QUFibYX0ZY51KHerdHigTWM2OCCxZjCwMlYzOyEQvF2= NI\xd3EzPDR|MkmwPS=>
NCI-H3122 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PyWlczKGh? MWfEUXNQ Mmi1TY5pcWKrdHnvckBw\iCDTFut[pV{cW:wIHTybZZmdiClZXzsJJBzd2yrZnXyZZRqd25iaX6gbJVu[W5iTlPJMWg{OTJ{IHPlcIx{KGijcnLvdolv\yCDTFugUFEyQT[PIH31eIFvfCC5aYToJGlEPTBib3[gNE45OzhizszN NHr4RZMzPDR|MkmwPS=>
NIH-3T3 MmP6T4lv[XOnIFHzd4F6 MYCxJIg> M3rtfmROW09? NXS0TlZ{UW6qaXLpeIlwdiCxZjDoeY1idiC5aXzkJJR6eGViRV3MOE1nfXOnZDDBUGsh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IIDoc5NxcG:{eXzheIVlKEGOSzDs[ZZmdCC5aYToJGlEPTBib3[gNE4xQCEQvF2= MnW3NlQ1OzJ7MEm=
NIH-3T3 M2m1fGtqdmG|ZTDBd5NigQ>? M2TlZVEhcA>? MmXOSG1UVw>? NHu0c|NKdmirYnn0bY9vKG:oIHj1cYFvKEWPTESt[pV{\WRiQVzLJGcyOjZ7QTDteZRidnRiZYjwdoV{e2WmIHHzd4V{e2WmIHHzJJBpd3OyaH:tRWxMKGyndnXsJJdqfGhiSVO1NEBw\iByLk[wOUDPxE1? NUHKepQ4OjR2M{K5NFk>
NIH-3T3 NH;rbHRMcW6jc3WgRZN{[Xl? MUixJIg> NY[xW|d[TE2VTx?= MWLJcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIGOxNlA3YSCvdYThcpQh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IIDoc5NxcG9vQVzLJIxmfmWuIIfpeIghUUN3MDDv[kAxNjZ{NjFOwG0> NY\QT3ozOjR2M{K5NFk>
NIH-3T3 MWrLbY5ie2ViQYPzZZk> NXHzOZl[OSCq MoexSG1UVw>? MVTJcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIFyxNVk3VSCvdYThcpQh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IIDoc5NxcG9vQVzLJIxmfmWuIIfpeIghUUN3MDDv[kAxNjh2MzFOwG0> MnrhNlQ1OzJ7MEm=
NIH-3T3 MlPsT4lv[XOnIFHzd4F6 MXexJIg> MW\EUXNQ MWPJcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIFyxNVUzWiCvdYThcpQh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IIDoc5NxcG9vQVzLJIxmfmWuIIfpeIghUUN3MDDv[kAyNjB{NjFOwG0> MWCyOFQ{OjlyOR?=
BAF3 M3T0bWZ2dmO2aX;uJGF{e2G7 NV\hTYFpPzJiaB?= Mk\VSG1UVw>? M3\PVmlvcGmkaYTpc44hd2ZiTmDNM2FNUyC2cnHud4Zm[3SnZDDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIIfpeIghUUN3MDDv[kAxNjB3MTFOwG0> NEXBW|MzPDR4OE[zNi=>
BAF3 MmrBR5l1d3SxeHnjJGF{e2G7 NFXxVHY4OiCq NGjvZYJFVVOR NGrne25KSzVyPUCuPVgh|ryP MlzaNlQ1Pjh4M{K=
NIH-3T3 MXLLbY5ie2ViQYPzZZk> MnXnNUBp NFns[o9KdmirYnn0bY9vKG:oIHj1cYFvKEWPTESt[pV{\WRiQVzLJGYyOTd2TDDteZRidnRiZYjwdoV{e2WmIHHzd4V{e2WmIHHzJJBpd3OyaH:tRWxMKGyndnXsJJdqfGhiSVO1NEBw\iByLkG2OUDPxE1? M13pNFI1QDF7MUG2
NIH-3T3 NUKxNWVbU2mwYYPlJGF{e2G7 Mn7BNUBp MX;Jcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIFOxNVU3YSCvdYThcpQh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IIDoc5NxcG9vQVzLJIxmfmWuIIfpeIghUUN3MDDv[kAxNjR5ODFOwG0> MnfjNlQ5OTlzMU[=
NIH-3T3 NYjzZXkyU2mwYYPlJGF{e2G7 Mn7WNUBp NYTMeYUyUW6qaXLpeIlwdiCxZjDoeY1idiCHTVy0MYZ2e2WmIFHMT{BIOTJyMmKgcZV1[W62IHX4dJJme3OnZDDhd5Nme3OnZDDhd{BxcG:|cHjvMWFNUyCuZY\lcEB4cXSqIFnDOVAhd2ZiMT6xOFgh|ryP NEXXbokzPDhzOUGxOi=>
NIH-3T3 MX7LbY5ie2ViQYPzZZk> MnnZNUBp NGfoO4lKdmirYnn0bY9vKG:oIHj1cYFvKEWPTESt[pV{\WRiQVzLJFEyPTGWaX7zJI12fGGwdDDlfJBz\XO|ZXSgZZN{\XO|ZXSgZZMheGixc4Doc{1CVEtibHX2[Ywhf2m2aDDJR|UxKG:oIEOuNFM6KM7:TR?= MojPNlQ5OTlzMU[=
KARPAS299 MXfLbY5ie2ViQYPzZZk> MVK5NEBucW5? MmL3SG1UVw>? M{\qeGlvcGmkaYTpc44hd2ZiTmDNMYZ2e2WmIFHMT{BxcG:|cHjvdplt[XSrb36g[ZhxemW|c3XkJJdqfGhiSVO1NEBw\iByLkGxJO69VQ>? M121UVI1QTByN{Ww
MKN 45 NXPJW5A4U2mwYYPlJGF{e2G7 M1XlPFEhcA>? NXPCbHpSTE2VTx?= Ml;qTY5pcWKrdHnvckBw\iClLV3leEBxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEKg{txO MVSyOFkxODd3MB?=
A549 MkfzR5l1d3SxeHnjJGF{e2G7 MY[0PEBp MV3EUXNQ MmHrTWM2OCCxZjC0MlA5PCEQvF2= M4\DZVI1QTByOEOw
NCI-H1975 NG\RSlJEgXSxdH;4bYMhSXO|YYm= M4XHWlQ5KGh? NWK5bFhVTE2VTx?= NUH4XlBiUUN3MDDv[kA4NjV3MTFOwG0> NUf6TJR{OjR7MEC4N|A>
NCI-H1993 NYe4fVBbS3m2b4TvfIlkKEG|c3H5 M1\tRlQ5KGh? NWXvVZZUTE2VTx?= NX;PPIxMUUN3MDDv[kAxNjB4MTFOwG0> NHK4elkzPDlyMEizNC=>
NCI-H1993 MmTSRZBwfG:|aYOgRZN{[Xl? NGLyXWsyKM7:TR?= M2DCOlI1KGh? MormSG1UVw>? NH\GNmRld2W|IH7veEBqdmS3Y3WgZZBweHSxc3nz MlXDNlQ6ODB6M{C=
NIH-3T3 MnSxR5l1d3SxeHnjJGF{e2G7 NFjoeZo1QCCq Mmj2SG1UVw>? NXv5cYRFUUN3MDDv[kAxNjN4NDFOwG0> MXuyOFkxODh|MB?=
EBC1 M3HONmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYG3NkBp MoTFSG1UVw>? NVX5dnRxUUN3MDDv[kAxNjByNkmg{txO MlTJNlQ6ODB6M{G=
KARPAS299 NWjOXppVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXe3NkBp NWfuU2p[TE2VTx?= MlLETWM2OCCxZjCwMlIh|ryP M13hOVI1QTByOEOx
NB1 NYDEVG9zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\KTWM2OD17MT65PEBvVQ>? Mo\iV2FPT0WU
NCI-SNU-5 M161VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PhOGlEPTB;MUC1Mlc2KG6P NXvPZpJCW0GQR1XS
SR NXzwbotXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnHOVVKUUN3ME2xNlYvOzFibl2= NIrEW4lUSU6JRWK=
SF539 MmXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTJyND6yOEBvVQ>? NELwZpBUSU6JRWK=
SU-DHL-1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHSxNHdKSzVyPUOzOk45OiCwTR?= MXTTRW5ITVJ?
SCC-3 MmHyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1naemlEPTB;M{W2Mlc3KG6P MnOxV2FPT0WU
DEL NX[2PZlLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn30TWM2OD1|NkmuPUBvVQ>? MnHZV2FPT0WU
CTV-1 MnToS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPLTWM2OD13OU[uOFghdk1? NHHQWIRUSU6JRWK=
EM-2 NXu5[HlsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmi1TWM2OD14MEGuN|Qhdk1? NHLjb|NUSU6JRWK=
MHH-CALL-2 M{LubGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPqWVVKSzVyPU[4Nk42PyCwTR?= Mn20V2FPT0WU
KM12 M13XT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{f1b2lEPTB;N{C2Mlkhdk1? M2X2RnNCVkeHUh?=
KINGS-1 M1j0SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\vb2lEPTB;N{S5Mlc2KG6P M3TTeHNCVkeHUh?=
MEG-01 NFzJc|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnKwTWM2OD16NUeuOlYhdk1? MVXTRW5ITVJ?
BV-173 MlLRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTFwMEW5PVch|ryP M2DWTnNCVkeHUh?=
LAMA-84 NFiyVGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTFwM{iyPFIh|ryP NX;Xe45GW0GQR1XS
KARPAS-299 NY\D[mh3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmf1TWM2OD1zLkSwPFYyKM7:TR?= MUDTRW5ITVJ?
K-562 M2HURWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTFwN{KyOlkh|ryP M{n2U3NCVkeHUh?=
SK-LMS-1 M1X1NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnzeVBKSzVyPUGuO|Y5PjdizszN NU\QXmJwW0GQR1XS
MOLT-16 NHfIOJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHsTWM2OD1zLkm1OVc2KM7:TR?= MWrTRW5ITVJ?
CMK M3rwbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;SeppDUUN3ME2xMlk3OTV7IN88US=> MWHTRW5ITVJ?
ST486 MnizS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTJwNEOwO|Mh|ryP NIK2W2dUSU6JRWK=
CI-1 NEfTdWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDPbnk{UUN3ME2yMlQ6PjV7IN88US=> NFvlU3RUSU6JRWK=
KP-N-RT-BM-1 M2j4NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXle29KSzVyPUKuO|AyOjJizszN M372SHNCVkeHUh?=
ALL-PO M4jxcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vkemlEPTB;Mz6xPFIxPyEQvF2= MlTHV2FPT0WU
KS-1 NHf2WnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4H6NmlEPTB;Mz6yNVIzPSEQvF2= MnnMV2FPT0WU
Becker Mo\wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{L6cWlEPTB;ND6yN|k{KM7:TR?= NEXNbWJUSU6JRWK=
GDM-1 M4XCc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXvTWM2OD12LkK0OlE4KM7:TR?= NHP6THhUSU6JRWK=
BC-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHqzN2xKSzVyPUSuOFkzPzdizszN NG\IbJJUSU6JRWK=
NB14 M{PsRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTRwOEO1NlQh|ryP Ml7vV2FPT0WU
NOS-1 NXLZOGxQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4O0PGlEPTB;NT6zN|g4PCEQvF2= MXrTRW5ITVJ?
MZ1-PC MkPrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTVwOEKxOVEh|ryP MYHTRW5ITVJ?
A498 M{TPOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\wO2lEPTB;Nj6wPFQ4OyEQvF2= M3HMc3NCVkeHUh?=
EW-16 M3npWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFuweoxKSzVyPU[uN|c4PzNizszN MYrTRW5ITVJ?
NALM-6 M2fLOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljYTWM2OD14Lk[4N|g4KM7:TR?= NELUbFJUSU6JRWK=
EB-3 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnsZXM{UUN3ME23MlA4OjN|IN88US=> M1PPN3NCVkeHUh?=
697 NXXSOo1kT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HQe2lEPTB;OT6yOFMzQSEQvF2= NXv3bFF5W0GQR1XS
Ramos-2G6-4C10 NXG5eVR2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTlwNUm4OFIh|ryP NGezZYpUSU6JRWK=
KNS-81-FD M{jkdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zUbGlEPTB;OT62PVY2OyEQvF2= M4TI[nNCVkeHUh?=
HUTU-80 M4i0WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYO5dXFmUUN3ME25Mlc1PjR{IN88US=> NV;PeJY3W0GQR1XS
LS-411N M3:3bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDsUWdGUUN3ME2xNE4xPTZ5IN88US=> M1nsb3NCVkeHUh?=
RPMI-8402 M1flNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTFyLkGxOkDPxE1? M4\PdHNCVkeHUh?=
KU812 MoW4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnPTGZRUUN3ME2xNE4zQTlzIN88US=> M{LTTHNCVkeHUh?=
EW-1 M{i4Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\UTWM2OD1zMD60OFI2KM7:TR?= MV\TRW5ITVJ?
HC-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NICwfWdKSzVyPUGwMlQ5PDRizszN NYfGNXU4W0GQR1XS
NB69 M1ezTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHr4[pVKSzVyPUGwMlUxPDNizszN MWHTRW5ITVJ?
MFH-ino MmnBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4m3emlEPTB;MUCuPFMxOyEQvF2= NGDnd25USU6JRWK=
CCRF-CEM M4K2d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7uXFFLUUN3ME2xNU42QTdizszN MkiwV2FPT0WU
SK-N-DZ Mk\DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXldWR{UUN3ME2xNk4xPDN4IN88US=> MYTTRW5ITVJ?
NCI-H720 MlroS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTF{LkG3NFUh|ryP Mk\kV2FPT0WU
HCC1187 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYD3OoJtUUN3ME2xNk4zODRzIN88US=> NV\pXJdQW0GQR1XS
IST-SL2 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3KUYdsUUN3ME2xNk41QDd{IN88US=> NXPuRnBXW0GQR1XS
KE-37 MonRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTF{Lke5OlYh|ryP NFTTS4xUSU6JRWK=
HCC1599 Mn;zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nQXmlEPTB;MUKuPVA3QSEQvF2= M{PFXXNCVkeHUh?=
A4-Fuk NW\ITnZXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mki4TWM2OD1zMj65OVg3KM7:TR?= NH\2PY5USU6JRWK=
NKM-1 NVfBWIc4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfjUGR4UUN3ME2xN{4zQTJ3IN88US=> MX7TRW5ITVJ?
BE-13 M1W1PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTF|Lke5PFkh|ryP M{PCT3NCVkeHUh?=
MV-4-11 NUmxPYNCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnGxTWM2OD1zND6wN|I1KM7:TR?= MXTTRW5ITVJ?
OPM-2 M{PCOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjLTWM2OD1zND60NFg2KM7:TR?= MWnTRW5ITVJ?
KARPAS-422 Ml\1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTF2LkWxNlYh|ryP MnzlV2FPT0WU
RPMI-8226 NFuxbI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LnT2lEPTB;MUSuPFkyPSEQvF2= NIr5e3FUSU6JRWK=
KARPAS-45 MofmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PPUWlEPTB;MUWuO|cyPiEQvF2= MkPMV2FPT0WU
SK-PN-DW MofVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mne0TWM2OD1zNT64OlMyKM7:TR?= M{C1NHNCVkeHUh?=
LC-2 NWe5d4tZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTF4LkG1NFYh|ryP NGfKT3dUSU6JRWK=
NCI-H1648 NYWyN5lqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TY[WlEPTB;MU[uNlU1KM7:TR?= M{nCc3NCVkeHUh?=
RL95-2 NXXLcmZiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;tUmlEPTB;MU[uN|k4QCEQvF2= MYrTRW5ITVJ?
KNS-42 M3PL[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rNUGlEPTB;MU[uO|I4PCEQvF2= NV:1XHg1W0GQR1XS
RPMI-6666 M3z6WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3eycmlEPTB;MU[uPVIyOSEQvF2= MkjCV2FPT0WU
SIG-M5 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfSWGpKSzVyPUG3MlE6ODNizszN NGe1PY5USU6JRWK=
VA-ES-BJ Mk\1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXu5SG94UUN3ME2xO{44PDVzIN88US=> NV35PZZlW0GQR1XS
MONO-MAC-6 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvsdmRHUUN3ME2xO{46OzF{IN88US=> NITX[HVUSU6JRWK=
LAN-6 MlHLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrBOYFKSzVyPUG4Mlc2PTdizszN NWH1T5ZlW0GQR1XS
A388 MkXrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\m[mlEPTB;MUmuN|A2QSEQvF2= NYHB[GJEW0GQR1XS
SK-NEP-1 MlKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPjTHZKSzVyPUKwMlIyOzJizszN M2KxT3NCVkeHUh?=
TE-10 NWHl[phZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTJyLkWyNlEh|ryP NHnoOHJUSU6JRWK=
HL-60 NGrLd2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Moj4TWM2OD1{MD65NFk6KM7:TR?= NX;QVINNW0GQR1XS
MC116 NYThdYxpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTs[GVKSzVyPUKxMlczOjFizszN NH2wcZdUSU6JRWK=
SW962 M{KweGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXu5bppxUUN3ME2yNU44QTF3IN88US=> Mmr2V2FPT0WU
NOMO-1 M1;HeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LHXGlEPTB;MkKuOlU3PCEQvF2= NWfM[nBLW0GQR1XS
CTB-1 M4njdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTJ{Lki2O|Eh|ryP MnHyV2FPT0WU
MRK-nu-1 MlmwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTJ{LkmwO|Qh|ryP NWjB[YZDW0GQR1XS
GR-ST NXTnTm1CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fGSWlEPTB;MkOuO|Yh|ryP M1f3PXNCVkeHUh?=
HH NGnTOGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTJ2LkCwN{DPxE1? NHnKZ3BUSU6JRWK=
NCI-H1963 NV76RWhQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTJ2LkC3PFIh|ryP M3jRU3NCVkeHUh?=
QIMR-WIL MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTJ2Lki3O|Ih|ryP MoDHV2FPT0WU
CGTH-W-1 NWLaV5lyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrJTWM2OD1{NT6wO|I{KM7:TR?= NHrne3RUSU6JRWK=
LP-1 NUjueWVST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLUTWM2OD1{NT62OVUyKM7:TR?= NGDyTWlUSU6JRWK=
NCI-H748 NWfl[mpnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTxZYNKSzVyPUK2MlUyOzdizszN MUjTRW5ITVJ?
PF-382 NWS1blFoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTJ5LkKyNlMh|ryP Ml3nV2FPT0WU
ATN-1 NYPET5A4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TqUWlEPTB;MkeuN|c{OiEQvF2= MnmzV2FPT0WU
L-540 NH23fJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHKyWVlKSzVyPUK3MlY1PTlizszN NUTG[3BDW0GQR1XS
LXF-289 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPUTWM2OD1{Nz63OVE6KM7:TR?= MlKxV2FPT0WU
LS-513 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITmVFNKSzVyPUK4MlE5ODdizszN M4TmNXNCVkeHUh?=
NCI-H1581 NFy3cHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TZ[GlEPTB;M{CuN|k4PiEQvF2= NG\YVpdUSU6JRWK=
ES6 MnL1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkH4TWM2OD1|MD62PFk6KM7:TR?= M1;MT3NCVkeHUh?=
SW982 NXTpbHdKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUX5S|NZUUN3ME2zNE45PTZ4IN88US=> Mn3lV2FPT0WU
DOHH-2 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfrTWM2OD1|MT61PFk{KM7:TR?= MmfHV2FPT0WU
DB MmfiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLuSXRjUUN3ME2zN{46PDNzIN88US=> M2LaenNCVkeHUh?=
MPP-89 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF25PIFKSzVyPUO0MlE4PTZizszN NVTOUoI1W0GQR1XS
LB831-BLC MljYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF33cWRKSzVyPUO0MlUyQDRizszN M{DpNXNCVkeHUh?=
NB5 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTN2Lki1N|Uh|ryP MojXV2FPT0WU
GB-1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3r5OGlEPTB;M{WuNFQ3QSEQvF2= NXrQRoxoW0GQR1XS
TE-15 NY\2dW9jT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXZTXVGUUN3ME2zOU4zOjN6IN88US=> M3XmTXNCVkeHUh?=
LC4-1 NVmwZ5dqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfmWHVKSzVyPUO1MlM5PDdizszN MXXTRW5ITVJ?
NCI-H747 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jsdWlEPTB;M{[uNVM3QSEQvF2= M1HubHNCVkeHUh?=
NTERA-S-cl-D1 M2HyRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zXVWlEPTB;M{iuO|M1PyEQvF2= Mof5V2FPT0WU
SK-MM-2 NH7UO|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{ewd2lEPTB;NECuNVE1PiEQvF2= MWfTRW5ITVJ?
TGW MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDFVlE{UUN3ME20NU4xPTZ|IN88US=> NEfkXYlUSU6JRWK=
ONS-76 NXvFSWJET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTR{LkS4PFMh|ryP M1rHcnNCVkeHUh?=
CPC-N NWG5bnZOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2[5NmlEPTB;NEKuPVk4OSEQvF2= M4XyNXNCVkeHUh?=
ES4 MknvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;oUGRKSzVyPUS0MlQyPTNizszN NIDrSXVUSU6JRWK=
Daudi NGn3bFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnScVd[UUN3ME20OU4xQDJ5IN88US=> M3e5VXNCVkeHUh?=
MOLT-4 NY\vRm8xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTR3LkC4OVMh|ryP MkTGV2FPT0WU
HT-144 M3iz[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXlZ2FvUUN3ME20Ok44OjZizszN MWXTRW5ITVJ?
SW872 NWHjO3prT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4Pnd2lEPTB;NEiuNVk{OyEQvF2= NX3BfnI6W0GQR1XS
D-283MED MoqxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULreJNYUUN3ME20PE4{PTR{IN88US=> MmK4V2FPT0WU
NCI-H2126 NYTKZlV5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWSwNIJUUUN3ME20PE45PDd4IN88US=> MVXTRW5ITVJ?
NCI-SNU-16 NX2zUY9XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVmwTJdZUUN3ME20PU4zOTR|IN88US=> MmCxV2FPT0WU
CESS M1fIT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnORZpLUUN3ME20PU42ODh6IN88US=> MVPTRW5ITVJ?
A101D MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTR7Lkm3N|Yh|ryP MUHTRW5ITVJ?

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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 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 9 mg/mL (19.98 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 5% DMSO+30% PEG 300+dd H2O 5mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 3-((R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine

文献中の引用 (68)

Frequently Asked Questions

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

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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