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

高品質保証

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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 NIi5d4JEgXSxdH;4bYMhSXO|YYm= NUPqPXFSPDhiaB?= NEDxVJBFVVOR NUTWWnpQS3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhSkGIMzDj[YxteyCneIDy[ZN{cW6pIFHMT{BHOTF5NFygcZV1[W62IHPv[ZhxemW|c3nu[{BGVUx2IIfpeIghUUN3MDDv[kAxNjZ{IN88US=> NEjnZYIzOTV5MkW4PS=>
BAF3 NIfCV3BEgXSxdH;4bYMhSXO|YYm= MofDOFghcA>? M4\IbWROW09? M2HEdmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KG2xdYPlJGJCTjNiY3XscJMh\XiycnXzd4lv\yCDTFugUFEyQT[PIH31eIFvfCClb3X4dJJme3OrbnegSW1NPCC5aYToJGlEPTBib3[gNk4zKM7:TR?= NILINGIzOTV5MkW4PS=>
BAF3 NYG1TmRnS3m2b4TvfIlkKEG|c3H5 MWO0PEBp MontSG1UVw>? NWDS[JJmS3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhSkGIMzDj[YxteyCneIDy[ZN{cW6pIFXNUFQuSUyNIIfpeIghUUN3MDDv[kAxNjJ6IN88US=> M3rMclIyPTd{NUi5
Kelly Mlm3R5l1d3SxeHnjJGF{e2G7 MUTEUXNQ M2XvW2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGtmdGy7IHPlcIx{KGW6cILld5NqdmdiQVzLJGYyOTd2TDDteZRidnRid3n0bEBKSzVyIH;mJFAvPDJizszN MVKyNVU4OjV6OR?=
SH-SY5Y MVjDfZRwfG:6aXOgRZN{[Xl? NGHBS25FVVOR NH\4ZZNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUUC2VWUXZJINmdGy|IHX4dJJme3OrbnegRWxMKEZzMUe0UEBufXSjboSge4l1cCCLQ{WwJI9nKDBwNUOg{txO NXXkfWJKOjF3N{K1PFk>
SMS-KCN M3LTbmN6fG:2b4jpZ{BCe3OjeR?= NHrpfZZFVVOR M2XXfmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNOWy2NQ16gZ4VtdHNiZYjwdoV{e2mwZzDBUGshWjF{N{XRJI12fGGwdDD3bZRpKEmFNUCgc4YhOC57MTFOwG0> NESzT2MzOTV5MkW4PS=>
BAF3 MYnDfZRwfG:6aXOgRZN{[Xl? NUXQT|Y3PDhiaB?= MXzEUXNQ NUS4cHE3S3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhSkGIMzDj[YxteyCneIDy[ZN{cW6pIGTlcE1CVEtid3n0bEBKSzVyIH;mJFAvOTlizszN NFfqd4szOTV5MkW4PS=>
3T3 M4H5c2Z2dmO2aX;uJGF{e2G7 NH7xXowyKGh? NETBOVRFVVOR MnvITY5pcWKrdHnvckBw\iCUT16gZZN{\XO|ZXSgZZMh\3Kxd4ToJIZi[3Sxcj3pcoR2[2WmIHH1eI9xcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEig{txO NV\HU3J{OjF6MUK0NVQ>
3T3-E M2HCbGZ2dmO2aX;uJGF{e2G7 MY[xJIg> NH\BbZJFVVOR M{D1W2lvcGmkaYTpc44hd2ZiVFnFNkBie3Onc4Pl[EBoem:5dHig[oFkfG:{LXnu[JVk\WRiYYX0c5Bpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC52NEig{txO NYfZO3FXOjF6MUK0NVQ>
A549 NUW2fowzU2mwYYPlJGF{e2G7 NXSzfYJxOSCq NYjLcHI6TE2VTx?= MWrJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KGNvTVXUJItqdmG|ZTDlfJBz\XO|ZXSgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDIS2YucW6mdXPl[EBifXSxcHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCwMlAxQCEQvF2= M37POVIyQDF{NEG0
BAF3-BCL M3PYWmZ2dmO2aX;uJGF{e2G7 NGPtSXQyKGh? M{K5XGROW09? M3T4RWlvcGmkaYTpc44hd2ZiQVLMJIF{e2W|c3XkJIF{KGe{b4f0bEBn[WO2b4KtbY5lfWOnZDDheZRweGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iBzLkG1PUDPxE1? MWmyNVgyOjRzNB?=
HEK293 MU\GeY5kfGmxbjDBd5NigQ>? NUDPTnVJOSCq NIDROpRFVVOR NYDDNJB5UW6qaXLpeIlwdiCxZjDBXGwh[XO|ZYPz[YQh[XNiZ4Lve5RpKG[jY4Tvdk1qdmS3Y3XkJIF2fG:yaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIECuNlk1KM7:TR?= MXGyNVgyOjRzNB?=
HEK293 NFPnNXNHfW6ldHnvckBCe3OjeR?= MY[xJIg> NXf0bIpJTE2VTx?= M3;WN2lvcGmkaYTpc44hd2ZiSWKgZZN{\XO|ZXSgZZMh\3Kxd4ToJIZi[3Sxcj3pcoR2[2WmIHH1eI9xcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDJwOEi3JO69VQ>? M4nabFIyQDF{NEG0
Jurkat NEfPc3JHfW6ldHnvckBCe3OjeR?= NXnodohDOSCq NUXEUpp{TE2VTx?= MknVTY5pcWKrdHnvckBw\iCOQ1ugZZN{\XO|ZXSgZZMh\3Kxd4ToJIZi[3Sxcj3pcoR2[2WmIHH1eI9xcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDJwN{SxJO69VQ>? NFvjeWszOThzMkSxOC=>
KARPAS299 Mn74T4lv[XOnIFHzd4F6 M2rQRlEhcA>? NGX5WFVFVVOR M1jnNmlvcGmkaYTpc44hd2ZiQVzLJIF{e2W|c3XkJIF{KGe{b4f0bEBn[WO2b4KtbY5lfWOnZDDheZRweGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCyJO69VQ>? NUfjUINxOjF6MUK0NVQ>
PAE NXP3dHhFTnWwY4Tpc44hSXO|YYm= Mm\pNUBp MmHuSG1UVw>? NGTlPFZKdmirYnn0bY9vKG:oIGTST2Ih[XO|ZYPz[YQh[XNiZ4Lve5RpKG[jY4Tvdk1qdmS3Y3XkJIF2fG:yaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIECuN|k6KM7:TR?= NF;6V3EzOThzMkSxOC=>
BAF3 MkO0SpVv[3Srb36gRZN{[Xl? Ml32Nk0{KGR? NVjLTVZNTE2VTx?= NV60fopsUW6qaXLpeIlwdiCxZjDUSWwu\nW|ZXSgbY5{fWyrbjDy[YNmeHSxcjDlfJBz\XO|ZXSge4l1cCCLQ{WwJI9nKDFwNkSzJO69VQ>? NGrJNVYzOzd2MkK1Ni=>
KARPAS299 MlTPR5l1d3SxeHnjJGF{e2G7 MYeyMVMh\A>? MXnEUXNQ Mlm2TWM2OD1yLkC2OFIh|ryP NIe0O4UzOzd2MkK1Ni=>
EBC1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWq3NkBp NVXmXZB{TE2VTx?= Ml70TWM2OD1yLkCyN{DPxE1? M2fiZ|I{QTl|M{K4
HCT116 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYSwOINKPzJiaB?= NInpNWpFVVOR MVfJR|UxRTF2LkiyJO69VQ>? NES1T|kzOzl7M{OyPC=>
MCF7 Ml[5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknuO|IhcA>? MmHWSG1UVw>? M1zYOGlEPTB;OT61PEDPxE1? NEPT[HUzOzl7M{OyPC=>
MDA-MB-231 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYe3NkBp MmruSG1UVw>? NYjPXVR4UUN3ME2xNE45KM7:TR?= NFXmeJQzOzl7M{OyPC=>
MKN45 M{f4[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkP2O|IhcA>? MVTEUXNQ NF20S|NKSzVyPUCuNFE{KM7:TR?= NUHsV|VGOjN7OUOzNlg>
NCI-H441 NVWycphbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX:3NkBp MlrvSG1UVw>? MlvxTWM2OD1zNz6yOUDPxE1? MYeyN|k6OzN{OB?=
NCI-H661 NWfkZlZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1q5WVczKGh? MnvGSG1UVw>? MWPJR|UxRTFzLkS3JO69VQ>? NEfKNIUzOzl7M{OyPC=>
SK-MEL-28 M4LjWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\sUVczKGh? MlrFSG1UVw>? NFn2fXpKSzVyPUGwMlk4KM7:TR?= NHjPUWwzOzl7M{OyPC=>
SKOV3 MmjGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTYWoE4OiCq MUHEUXNQ MoKyTWM2OD1zMj64OUDPxE1? NIi5PXUzOzl7M{OyPC=>
SNU5 NFzoc3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFOzfXA4OiCq NHvXZYdFVVOR NF;NU21KSzVyPUCuNFE3KM7:TR?= MojpNlM6QTN|Mki=
NCI-H2228 NXHFZZI4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYK3NkBp MVzEUXNQ MUDJcohq[mm2aX;uJI9nKEGOSz3meZNqd25iZILpeoVvKGOnbHygdJJwdGmoZYLheIlwdiC5aYToJGlEPTBib3[gNE4yOThizszN Ml7JNlQ1OzJ7MEm=
NCI-H3122 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVW3NkBp MmHvSG1UVw>? NETnOGRKdmirYnn0bY9vKG:oIFHMT{1nfXOrb36g[JJqfmWwIHPlcIwheHKxbHnm[ZJifGmxbjD3bZRpKEmFNUCgc4YhOC5zMEig{txO NHn6XIYzPDR|MkmwPS=>
NCI-H3122 NEixR|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\0WGs4OiCq NVj5[lFHTE2VTx?= MXzJcohq[mm2aX;uJI9nKEGOSz3meZNqd25iZILpeoVvKGOnbHygdJJwdGmoZYLheIlwdiCrbjDoeY1idiCQQ1mtTFMyOjJiY3XscJMhcGG{Yn;ybY5oKEGOSzDHNVI3QUFibYX0ZY51KHerdHigTWM2OCCxZjCwMlYzOyEQvF2= Mne5NlQ1OzJ7MEm=
NCI-H3122 M2rYSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUH2fVNWPzJiaB?= NXXONWdMTE2VTx?= NITVOJRKdmirYnn0bY9vKG:oIFHMT{1nfXOrb36g[JJqfmWwIHPlcIwheHKxbHnm[ZJifGmxbjDpckBpfW2jbjDOR2kuUDNzMkKgZ4VtdHNiaHHyZo9zcW6pIFHMT{BNOTF7Nl2gcZV1[W62IIfpeIghUUN3MDDv[kAxNjh|ODFOwG0> MnjiNlQ1OzJ7MEm=
NIH-3T3 M2HU[mtqdmG|ZTDBd5NigQ>? MYexJIg> M{HkemROW09? MnKyTY5pcWKrdHnvckBw\iCqdX3hckB4cWymIIT5dIUhTU2OND3meZNm\CCDTFug[ZhxemW|c3XkJIF{e2W|c3XkJIF{KHCqb4PwbI9zgWyjdHXkJGFNUyCuZY\lcEB4cXSqIFnDOVAhd2ZiMD6wPEDPxE1? NIHiVXUzPDR|MkmwPS=>
NIH-3T3 NVfV[WV2U2mwYYPlJGF{e2G7 NYXuXmRvOSCq M3jvbmROW09? MV;Jcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIFexNlY6SSCvdYThcpQh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IIDoc5NxcG9vQVzLJIxmfmWuIIfpeIghUUN3MDDv[kAxNjZyNTFOwG0> MVmyOFQ{OjlyOR?=
NIH-3T3 Ml7ZT4lv[XOnIFHzd4F6 NX30cYdXOSCq M2nucWROW09? NF:zT2lKdmirYnn0bY9vKG:oIHj1cYFvKEWPTESt[pV{\WRiQVzLJHMyOjB4WTDteZRidnRiZYjwdoV{e2WmIHHzd4V{e2WmIHHzJJBpd3OyaH:tRWxMKGyndnXsJJdqfGhiSVO1NEBw\iByLk[yOkDPxE1? Ml;BNlQ1OzJ7MEm=
NIH-3T3 MnnNT4lv[XOnIFHzd4F6 MYKxJIg> NY[2ZWZETE2VTx?= NGfUfmdKdmirYnn0bY9vKG:oIHj1cYFvKEWPTESt[pV{\WRiQVzLJGwyOTl4TTDteZRidnRiZYjwdoV{e2WmIHHzd4V{e2WmIHHzJJBpd3OyaH:tRWxMKGyndnXsJJdqfGhiSVO1NEBw\iByLki0N{DPxE1? NVzYPI94OjR2M{K5NFk>
NIH-3T3 MmfLT4lv[XOnIFHzd4F6 M3[4XVEhcA>? NWXxTGo3TE2VTx?= MYrJcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIFyxNVUzWiCvdYThcpQh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IIDoc5NxcG9vQVzLJIxmfmWuIIfpeIghUUN3MDDv[kAyNjB{NjFOwG0> MWOyOFQ{OjlyOR?=
BAF3 M3jsXmZ2dmO2aX;uJGF{e2G7 NHHBVoE4OiCq NYX1XmFlTE2VTx?= NGXmV3ZKdmirYnn0bY9vKG:oIF7QUU9CVEtidILhcpNn\WO2ZXSgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjD3bZRpKEmFNUCgc4YhOC5yNUGg{txO M3n0eVI1PDZ6NkOy
BAF3 NETmdVBEgXSxdH;4bYMhSXO|YYm= NU\RWY1KPzJiaB?= NULpW4FPTE2VTx?= NGexeoxKSzVyPUCuPVgh|ryP MYCyOFQ3QDZ|Mh?=
NIH-3T3 MX3LbY5ie2ViQYPzZZk> MVexJIg> NUfnSHhYUW6qaXLpeIlwdiCxZjDoeY1idiCHTVy0MYZ2e2WmIFHMT{BHOTF5NFygcZV1[W62IHX4dJJme3OnZDDhd5Nme3OnZDDhd{BxcG:|cHjvMWFNUyCuZY\lcEB4cXSqIFnDOVAhd2ZiMD6xOlUh|ryP M2DkNlI1QDF7MUG2
NIH-3T3 MlvBT4lv[XOnIFHzd4F6 M2HUU|EhcA>? MljKTY5pcWKrdHnvckBw\iCqdX3hckBGVUx2LX\1d4VlKEGOSzDDNVE2PllibYX0ZY51KGW6cILld5Nm\CCjc4Pld5Nm\CCjczDwbI9{eGixLVHMT{Bt\X[nbDD3bZRpKEmFNUCgc4YhOC52N{ig{txO MXqyOFgyQTFzNh?=
NIH-3T3 NGq3XWJMcW6jc3WgRZN{[Xl? M2rtRVEhcA>? M{[xS2lvcGmkaYTpc44hd2ZiaIXtZY4hTU2OND3meZNm\CCDTFugS|EzODKUIH31eIFvfCCneIDy[ZN{\WRiYYPz[ZN{\WRiYYOgdIhwe3Cqbz3BUGshdGW4ZXyge4l1cCCLQ{WwJI9nKDFwMUS4JO69VQ>? M{fVZ|I1QDF7MUG2
NIH-3T3 M3LNO2tqdmG|ZTDBd5NigQ>? M1\GeFEhcA>? MW\Jcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIEGxOVFVcW6|IH31eIFvfCCneIDy[ZN{\WRiYYPz[ZN{\WRiYYOgdIhwe3Cqbz3BUGshdGW4ZXyge4l1cCCLQ{WwJI9nKDNwMEO5JO69VQ>? MWOyOFgyQTFzNh?=
KARPAS299 NFHE[ZZMcW6jc3WgRZN{[Xl? M4PhN|kxKG2rbh?= NYf4O5RHTE2VTx?= NXXEfIM4UW6qaXLpeIlwdiCxZjDOVG0u\nW|ZXSgRWxMKHCqb4PwbI9zgWyjdHnvckBmgHC{ZYPz[YQhf2m2aDDJR|UxKG:oIECuNVEh|ryP MljvNlQ6ODB5NUC=
MKN 45 M1fVcWtqdmG|ZTDBd5NigQ>? MnzQNUBp MmTMSG1UVw>? MofBTY5pcWKrdHnvckBw\iClLV3leEBxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEKg{txO NGTEUVkzPDlyMEe1NC=>
A549 MnLhR5l1d3SxeHnjJGF{e2G7 NF;lNoM1QCCq NW\0cpg{TE2VTx?= M4fp[mlEPTBib3[gOE4xQDRizszN NUjNcJJUOjR7MEC4N|A>
NCI-H1975 MVnDfZRwfG:6aXOgRZN{[Xl? M4W1W|Q5KGh? NIXVbG9FVVOR MoK2TWM2OCCxZjC3MlU2OSEQvF2= MUWyOFkxODh|MB?=
NCI-H1993 M2qzNmN6fG:2b4jpZ{BCe3OjeR?= MVO0PEBp M3\W[mROW09? NFvOdm1KSzVyIH;mJFAvODZzIN88US=> MUGyOFkxODh|MB?=
NCI-H1993 NYrJ[2hmSXCxdH;zbZMhSXO|YYm= M4HSeVEh|ryP MX[yOEBp MW\EUXNQ M2rqN4Rw\XNibn;0JIlv\HWlZTDhdI9xfG:|aYO= MYmyOFkxODh|MB?=
NIH-3T3 NGTqXmREgXSxdH;4bYMhSXO|YYm= MoXLOFghcA>? NILEcFBFVVOR MkTQTWM2OCCxZjCwMlM3PCEQvF2= M4P1dVI1QTByOEOw
EBC1 Mk\CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnv3O|IhcA>? NWfiWVBjTE2VTx?= MVfJR|UxKG:oIECuNFA3QSEQvF2= MorJNlQ6ODB6M{G=
KARPAS299 M4ricmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWW3NkBp MWnEUXNQ MnLKTWM2OCCxZjCwMlIh|ryP NXn2ZWN2OjR7MEC4N|E>
NB1 MmD1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTlzLkm4JI5O NEnXeWtUSU6JRWK=
NCI-SNU-5 M4XNUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjlZpdSUUN3ME2xNFUvPzVibl2= NYrqUHNlW0GQR1XS
SR NVHhOIp[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfxdmVKSzVyPUGyOk4{OSCwTR?= NHizTYxUSU6JRWK=
SF539 MoCwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnvTWM2OD1{MESuNlQhdk1? NH6weINUSU6JRWK=
SU-DHL-1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF21O5lKSzVyPUOzOk45OiCwTR?= NHPSXVBUSU6JRWK=
SCC-3 NWi5RXA3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\6WZh6UUN3ME2zOVYvPzZibl2= MXzTRW5ITVJ?
DEL MoCzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfYdINGUUN3ME2zOlkvQSCwTR?= NXzDWVBRW0GQR1XS
CTV-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTV7Nj60PEBvVQ>? MniyV2FPT0WU
EM-2 NFPwPVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn6yTWM2OD14MEGuN|Qhdk1? M3;xfXNCVkeHUh?=
MHH-CALL-2 NFnGfnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLCVlRMUUN3ME22PFIvPTdibl2= MYnTRW5ITVJ?
KM12 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XSNGlEPTB;N{C2Mlkhdk1? NU[4NG1VW0GQR1XS
KINGS-1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\iTYRKSzVyPUe0PU44PSCwTR?= MX3TRW5ITVJ?
MEG-01 Mo\6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTh3Nz62OkBvVQ>? Mn\MV2FPT0WU
BV-173 MkPDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XPWWlEPTB;MT6wOVk6PyEQvF2= MVfTRW5ITVJ?
LAMA-84 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHT2S2VKSzVyPUGuN|gzQDJizszN M4rGcXNCVkeHUh?=
KARPAS-299 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3njPWlEPTB;MT60NFg3OSEQvF2= NFLuPFJUSU6JRWK=
K-562 NGrNfFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTFwN{KyOlkh|ryP NYnvSY5bW0GQR1XS
SK-LMS-1 NHq4PHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zvcmlEPTB;MT63Olg3PyEQvF2= M{jsfnNCVkeHUh?=
MOLT-16 MkXiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFWzOmdKSzVyPUGuPVU2PzVizszN M3zGUHNCVkeHUh?=
CMK NV\zN2NMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\iTWM2OD1zLkm2NVU6KM7:TR?= M1y2T3NCVkeHUh?=
ST486 NWDDVmQ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTpTWM2OD1{LkSzNFc{KM7:TR?= M3v3TXNCVkeHUh?=
CI-1 MoC1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3u4TmlEPTB;Mj60PVY2QSEQvF2= NXLp[VBqW0GQR1XS
KP-N-RT-BM-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHVTWM2OD1{LkewNVIzKM7:TR?= MVzTRW5ITVJ?
ALL-PO NVHhN5AxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTNwMUiyNFch|ryP MX3TRW5ITVJ?
KS-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTNwMkGyNlUh|ryP MmjEV2FPT0WU
Becker NVTNXZZvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTRwMkO5N{DPxE1? MnniV2FPT0WU
GDM-1 M1jZWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rMVmlEPTB;ND6yOFYyPyEQvF2= NY\oTnc1W0GQR1XS
BC-1 NFrTdm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\uR5hHUUN3ME20MlQ6Ojd5IN88US=> M{TzNHNCVkeHUh?=
NB14 M3W2Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHP0dotKSzVyPUSuPFM2OjRizszN NIjPSGNUSU6JRWK=
NOS-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXq4[JN2UUN3ME21MlM{QDd2IN88US=> MmnIV2FPT0WU
MZ1-PC M2\mdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHP0O4pKSzVyPUWuPFIyPTFizszN MkDGV2FPT0WU
A498 NVTFU4pZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTZwMEi0O|Mh|ryP MXTTRW5ITVJ?
EW-16 M2eyR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTZwM{e3O|Mh|ryP MW\TRW5ITVJ?
NALM-6 Mn3qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3zdGdKSzVyPU[uOlg{QDdizszN NHLwN3FUSU6JRWK=
EB-3 M4TKeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjyU5RKSzVyPUeuNFczOzNizszN NUXh[Iw6W0GQR1XS
697 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTlwMkSzNlkh|ryP NGn0fVJUSU6JRWK=
Ramos-2G6-4C10 Mo[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPtTWM2OD17LkW5PFQzKM7:TR?= MX;TRW5ITVJ?
KNS-81-FD MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVS3dpl4UUN3ME25MlY6PjV|IN88US=> NXq0[HI4W0GQR1XS
HUTU-80 M2W5[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPEdIs{UUN3ME25Mlc1PjR{IN88US=> M{\ySnNCVkeHUh?=
LS-411N M33nUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3uxOWlEPTB;MUCuNFU3PyEQvF2= NHn5XnJUSU6JRWK=
RPMI-8402 Mkf3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoexTWM2OD1zMD6xNVYh|ryP M3e2XnNCVkeHUh?=
KU812 M{fRTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XmZ2lEPTB;MUCuNlk6OSEQvF2= M2e5THNCVkeHUh?=
EW-1 Ml3pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYr5VllsUUN3ME2xNE41PDJ3IN88US=> MoWyV2FPT0WU
HC-1 MnnBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2G4VGlEPTB;MUCuOFg1PCEQvF2= MVjTRW5ITVJ?
NB69 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\wd45KUUN3ME2xNE42ODR|IN88US=> MV\TRW5ITVJ?
MFH-ino MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HhcWlEPTB;MUCuPFMxOyEQvF2= NFnsbZZUSU6JRWK=
CCRF-CEM NFPMdoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFniS5RKSzVyPUGxMlU6PyEQvF2= M17ETXNCVkeHUh?=
SK-N-DZ MlXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTF{LkC0N|Yh|ryP MXvTRW5ITVJ?
NCI-H720 NHH4b3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vsOmlEPTB;MUKuNVcxPSEQvF2= MYHTRW5ITVJ?
HCC1187 NY[1WmQ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mof1TWM2OD1zMj6yNFQyKM7:TR?= NVLxdJVDW0GQR1XS
IST-SL2 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTF{LkS4O|Ih|ryP MXjTRW5ITVJ?
KE-37 NGHGXo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHu4WopKSzVyPUGyMlc6PjZizszN NUXjWHB2W0GQR1XS
HCC1599 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3ySoQ4UUN3ME2xNk46ODZ7IN88US=> M2fmZXNCVkeHUh?=
A4-Fuk MknSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jQPWlEPTB;MUKuPVU5PiEQvF2= NGTFR4pUSU6JRWK=
NKM-1 M3:xfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfWfXZKSzVyPUGzMlI6OjVizszN MWrTRW5ITVJ?
BE-13 NVftcI55T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlviTWM2OD1zMz63PVg6KM7:TR?= NFrwfXdUSU6JRWK=
MV-4-11 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonkTWM2OD1zND6wN|I1KM7:TR?= MoT6V2FPT0WU
OPM-2 NGrEelVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2W1OmlEPTB;MUSuOFA5PSEQvF2= NWXEfXBMW0GQR1XS
KARPAS-422 M2\ofWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHyzdXNKSzVyPUG0MlUyOjZizszN MUfTRW5ITVJ?
RPMI-8226 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XkfWlEPTB;MUSuPFkyPSEQvF2= MkfXV2FPT0WU
KARPAS-45 MmruS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfWPZVCUUN3ME2xOU44PzF4IN88US=> M4LhXnNCVkeHUh?=
SK-PN-DW NI\TbJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NISxUFRKSzVyPUG1Mlg3OzFizszN MmXzV2FPT0WU
LC-2 MoDKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fk[WlEPTB;MU[uNVUxPiEQvF2= NXrxT25NW0GQR1XS
NCI-H1648 M4rHNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkS1TWM2OD1zNj6yOVQh|ryP MnP6V2FPT0WU
RL95-2 MoSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjOTWM2OD1zNj6zPVc5KM7:TR?= M3y0OnNCVkeHUh?=
KNS-42 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEWxOWVKSzVyPUG2MlczPzRizszN MXHTRW5ITVJ?
RPMI-6666 Mn7xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vIbmlEPTB;MU[uPVIyOSEQvF2= NX7WRnBKW0GQR1XS
SIG-M5 M1qxUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXObohKSzVyPUG3MlE6ODNizszN MoP4V2FPT0WU
VA-ES-BJ MmPoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTF5Lke0OVEh|ryP NXLPdVZtW0GQR1XS
MONO-MAC-6 M3Xqdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrPTWM2OD1zNz65N|EzKM7:TR?= NXXwXm5CW0GQR1XS
LAN-6 NF\iNnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\PRXNzUUN3ME2xPE44PTV5IN88US=> NISyU4xUSU6JRWK=
A388 M{PmeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTF7LkOwOVkh|ryP NF2yU2xUSU6JRWK=
SK-NEP-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTJyLkKxN|Ih|ryP NXXzVG1GW0GQR1XS
TE-10 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTJyLkWyNlEh|ryP NU\CTmNsW0GQR1XS
HL-60 MlXVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7uTWM2OD1{MD65NFk6KM7:TR?= NHLjSnJUSU6JRWK=
MC116 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrTWVlKSzVyPUKxMlczOjFizszN MVzTRW5ITVJ?
SW962 MljvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTOe2R6UUN3ME2yNU44QTF3IN88US=> MYHTRW5ITVJ?
NOMO-1 NVW0UXJWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{L5R2lEPTB;MkKuOlU3PCEQvF2= Ml7sV2FPT0WU
CTB-1 M1TNOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XGfmlEPTB;MkKuPFY4OSEQvF2= NUD2VHAxW0GQR1XS
MRK-nu-1 MnrFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTJ{LkmwO|Qh|ryP M3\qVHNCVkeHUh?=
GR-ST M2XjN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDF[2tKSzVyPUKzMlc3KM7:TR?= NF7VdHdUSU6JRWK=
HH NInKPGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFq0ZYdKSzVyPUK0MlAxOyEQvF2= M3XWXHNCVkeHUh?=
NCI-H1963 NFiwTGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHx[VBKSzVyPUK0MlA4QDJizszN M17qcnNCVkeHUh?=
QIMR-WIL NUnHc2VHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1T0T2lEPTB;MkSuPFc4OiEQvF2= NVHqWopmW0GQR1XS
CGTH-W-1 NYLhT442T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTJ3LkC3NlMh|ryP NXP4RnhFW0GQR1XS
LP-1 NX;KTIprT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYn3cItmUUN3ME2yOU43PTVzIN88US=> NVrPTVA3W0GQR1XS
NCI-H748 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTJ4LkWxN|ch|ryP M3;5SHNCVkeHUh?=
PF-382 NFn0UZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHqTWM2OD1{Nz6yNlI{KM7:TR?= MVTTRW5ITVJ?
ATN-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXSclBKUUN3ME2yO{4{PzN{IN88US=> Mn\EV2FPT0WU
L-540 M4HQWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmj3TWM2OD1{Nz62OFU6KM7:TR?= Mn;uV2FPT0WU
LXF-289 NHu4bItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTJ5Lke1NVkh|ryP MXPTRW5ITVJ?
LS-513 NH7wbW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVy3WGZnUUN3ME2yPE4yQDB5IN88US=> NYPDNnpLW0GQR1XS
NCI-H1581 M2PIU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jyRmlEPTB;M{CuN|k4PiEQvF2= MYPTRW5ITVJ?
ES6 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTNyLk[4PVkh|ryP M1W1b3NCVkeHUh?=
SW982 NWOzXHptT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTNyLki1OlYh|ryP MlfSV2FPT0WU
DOHH-2 NGHSd3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTNzLkW4PVMh|ryP MmnkV2FPT0WU
DB MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlz2TWM2OD1|Mz65OFMyKM7:TR?= MoP5V2FPT0WU
MPP-89 NV7zR2M3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHVZVVVUUN3ME2zOE4yPzV4IN88US=> NYHCUVMyW0GQR1XS
LB831-BLC NHr1R|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTN2LkWxPFQh|ryP NVPyVG5TW0GQR1XS
NB5 M3PYZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHuTWM2OD1|ND64OVM2KM7:TR?= MkPWV2FPT0WU
GB-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nUVGlEPTB;M{WuNFQ3QSEQvF2= M1HMTHNCVkeHUh?=
TE-15 NI\xdVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTN3LkKyN|gh|ryP NFHoNm9USU6JRWK=
LC4-1 NUXtWIE5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{Ll[2lEPTB;M{WuN|g1PyEQvF2= MUDTRW5ITVJ?
NCI-H747 M3jxPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3xWGxHUUN3ME2zOk4yOzZ7IN88US=> NWntT5dQW0GQR1XS
NTERA-S-cl-D1 NVz3Vpd7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M16wb2lEPTB;M{iuO|M1PyEQvF2= M2exdHNCVkeHUh?=
SK-MM-2 M1TRemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTRyLkGxOFYh|ryP M1z1NnNCVkeHUh?=
TGW NULLVGwyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHSx[ZRKSzVyPUSxMlA2PjNizszN MVzTRW5ITVJ?
ONS-76 NYHuZmNXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjGe5d2UUN3ME20Nk41QDh|IN88US=> MkTNV2FPT0WU
CPC-N MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTR{Lkm5O|Eh|ryP NVjBdGJRW0GQR1XS
ES4 M3jFfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTR2LkSxOVMh|ryP MYrTRW5ITVJ?
Daudi MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\KfFdKSzVyPUS1MlA5OjdizszN MkLoV2FPT0WU
MOLT-4 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3n3bWlEPTB;NEWuNFg2OyEQvF2= MkC0V2FPT0WU
HT-144 MkOyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\vTWM2OD12Nj63NlYh|ryP MmHpV2FPT0WU
SW872 MnKwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPuTWM2OD12OD6xPVM{KM7:TR?= MU\TRW5ITVJ?
D-283MED MoLMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;XTWM2OD12OD6zOVQzKM7:TR?= NEntUHZUSU6JRWK=
NCI-H2126 NXPO[nJxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLtTWM2OD12OD64OFc3KM7:TR?= NU[5ZXE3W0GQR1XS
NCI-SNU-16 M3HWZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXifoh1UUN3ME20PU4zOTR|IN88US=> MWDTRW5ITVJ?
CESS NFTaR|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmDMTWM2OD12OT61NFg5KM7:TR?= NHLLW4RUSU6JRWK=
A101D MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzETWM2OD12OT65O|M3KM7:TR?= M1TGWXNCVkeHUh?=

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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 (65)

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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