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

高品質保証

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カスタマーフィードバック(8)

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 MXLDfZRwfG:6aXOgRZN{[Xl? MWe0PEBp NFm2O3BFVVOR NGTxRllEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBDSUZ|IHPlcIx{KGW6cILld5NqdmdiQVzLJGYyOTd2TDDteZRidnRiY3;lfJBz\XO|aX7nJGVOVDRid3n0bEBKSzVyIH;mJFAvPjJizszN NWn1colvOjF3N{K1PFk>
BAF3 M3jtb2N6fG:2b4jpZ{BCe3OjeR?= NInCO4c1QCCq MkT4SG1UVw>? NFrKNZZEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBDSUZ|IHPlcIx{KGW6cILld5NqdmdiQVzLJGwyOTl4TTDteZRidnRiY3;lfJBz\XO|aX7nJGVOVDRid3n0bEBKSzVyIH;mJFIvOiEQvF2= NH7rWW8zOTV5MkW4PS=>
BAF3 NUnFWnB{S3m2b4TvfIlkKEG|c3H5 MVS0PEBp MUPEUXNQ MnXNR5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgRmFHOyClZXzsd{BmgHC{ZYPzbY5oKEWPTEStRWxMKHerdHigTWM2OCCxZjCwMlI5KM7:TR?= M4XWeFIyPTd{NUi5
Kelly NVnxW|VWS3m2b4TvfIlkKEG|c3H5 MmPGSG1UVw>? M4foVmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGtmdGy7IHPlcIx{KGW6cILld5NqdmdiQVzLJGYyOTd2TDDteZRidnRid3n0bEBKSzVyIH;mJFAvPDJizszN NXz3dmJDOjF3N{K1PFk>
SH-SY5Y MkXlR5l1d3SxeHnjJGF{e2G7 MXjEUXNQ NWL5UJVbS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0hvU2m1XUBk\WyuczDlfJBz\XO|aX7nJGFNUyCIMUG3OGwhdXW2YX70JJdqfGhiSVO1NEBw\iByLkWzJO69VQ>? M3\GcFIyPTd{NUi5
SMS-KCN NWC2fG9FS3m2b4TvfIlkKEG|c3H5 NWXjfoJPTE2VTx?= M37Tc2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNOWy2NQ16gZ4VtdHNiZYjwdoV{e2mwZzDBUGshWjF{N{XRJI12fGGwdDD3bZRpKEmFNUCgc4YhOC57MTFOwG0> M{PiclIyPTd{NUi5
BAF3 NVS4WmNoS3m2b4TvfIlkKEG|c3H5 NFvJeY81QCCq NUm0Nmd3TE2VTx?= MVfDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDCRWY{KGOnbHzzJIV5eHKnc4PpcochXGWuLVHMT{B4cXSqIFnDOVAhd2ZiMD6xPUDPxE1? MYOyNVU4OjV6OR?=
3T3 MUPGeY5kfGmxbjDBd5NigQ>? MU[xJIg> NV7sOm5TTE2VTx?= MmPoTY5pcWKrdHnvckBw\iCUT16gZZN{\XO|ZXSgZZMh\3Kxd4ToJIZi[3Sxcj3pcoR2[2WmIHH1eI9xcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEig{txO NFH1fmMzOThzMkSxOC=>
3T3-E M1v2cmZ2dmO2aX;uJGF{e2G7 NYS3SopsOSCq NFq2NIJFVVOR NWDZbmtwUW6qaXLpeIlwdiCxZjDUTWUzKGG|c3Xzd4VlKGe{b4f0bEBn[WO2b4KtbY5lfWOnZDDheZRweGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkS0PEDPxE1? MUiyNVgyOjRzNB?=
A549 NIX5NIVMcW6jc3WgRZN{[Xl? NILOdJUyKGh? MmrKSG1UVw>? M2PNSGlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiYz3NSXQhc2mwYYPlJIV5eHKnc4Pl[EBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGhITi2rbnT1Z4VlKGG3dH;wbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFAvODB6IN88US=> M2rzdVIyQDF{NEG0
BAF3-BCL MoHpSpVv[3Srb36gRZN{[Xl? MWGxJIg> NWLkTm54TE2VTx?= M17sO2lvcGmkaYTpc44hd2ZiQVLMJIF{e2W|c3XkJIF{KGe{b4f0bEBn[WO2b4KtbY5lfWOnZDDheZRweGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iBzLkG1PUDPxE1? M2HxU|IyQDF{NEG0
HEK293 NHjFd|ZHfW6ldHnvckBCe3OjeR?= MXqxJIg> NYXTTZo2TE2VTx?= MoHXTY5pcWKrdHnvckBw\iCDWFygZZN{\XO|ZXSgZZMh\3Kxd4ToJIZi[3Sxcj3pcoR2[2WmIHH1eI9xcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMkm0JO69VQ>? NHfpeFUzOThzMkSxOC=>
HEK293 MULGeY5kfGmxbjDBd5NigQ>? MoDiNUBp NV63bXN6TE2VTx?= MWfJcohq[mm2aX;uJI9nKEmUIHHzd4V{e2WmIHHzJIdzd3e2aDDmZYN1d3JvaX7keYNm\CCjdYTvdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAzNjh6NzFOwG0> M1nyNlIyQDF{NEG0
Jurkat MmXkSpVv[3Srb36gRZN{[Xl? MnvxNUBp M{[yV2ROW09? MX\Jcohq[mm2aX;uJI9nKEyFSzDhd5Nme3OnZDDhd{Boem:5dHig[oFkfG:{LXnu[JVk\WRiYYX0c5Bpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOi55NEGg{txO MkHuNlE5OTJ2MUS=
KARPAS299 NUTHcI0xU2mwYYPlJGF{e2G7 MXOxJIg> MXjEUXNQ NXfXWGpMUW6qaXLpeIlwdiCxZjDBUGsh[XO|ZYPz[YQh[XNiZ4Lve5RpKG[jY4Tvdk1qdmS3Y3XkJIF2fG:yaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIECuNFIh|ryP Mo\jNlE5OTJ2MUS=
PAE M4\aVGZ2dmO2aX;uJGF{e2G7 MX6xJIg> MXfEUXNQ M1LidGlvcGmkaYTpc44hd2ZiVGLLRkBie3Onc4Pl[EBieyCpcn;3eIgh\mGldH;yMYlv\HWlZXSgZZV1d3Cqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMD6zPVkh|ryP M1nDT|IyQDF{NEG0
BAF3 NGPpbVNHfW6ldHnvckBCe3OjeR?= M{XKc|IuOyCm NYj1cVFbTE2VTx?= NGPyXnNKdmirYnn0bY9vKG:oIGTFUE1nfXOnZDDpcpN2dGmwIILlZ4VxfG:{IHX4dJJme3OnZDD3bZRpKEmFNUCgc4YhOS54NEOg{txO NHzhPIUzOzd2MkK1Ni=>
KARPAS299 NFXH[pVEgXSxdH;4bYMhSXO|YYm= M2HnOlIuOyCm NXe1WmVXTE2VTx?= NXfUWGhNUUN3ME2wMlA3PDJizszN MUOyN|c1OjJ3Mh?=
EBC1 MmH2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWq3NkBp MULEUXNQ M{DzS2lEPTB;MD6wNlMh|ryP NVviTJlROjN7OUOzNlg>
HCT116 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\j[VczKGh? MY\EUXNQ MlHzTWM2OD1zND64NkDPxE1? MW[yN|k6OzN{OB?=
MCF7 NV7jOXRnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXO3NkBp MVjEUXNQ NH2weZJKSzVyPUmuOVgh|ryP MkPRNlM6QTN|Mki=
MDA-MB-231 NWHOUmE3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfRO|IhcA>? M4fGPGROW09? NWf5RpFQUUN3ME2xNE45KM7:TR?= MU[yN|k6OzN{OB?=
MKN45 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnmPJg4OiCq NX:wTW9oTE2VTx?= MnnuTWM2OD1yLkCxN{DPxE1? M3W4UlI{QTl|M{K4
NCI-H441 NUfTU25vT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXGzVXRjPzJiaB?= Mm[1SG1UVw>? M2LTemlEPTB;MUeuNlUh|ryP MV2yN|k6OzN{OB?=
NCI-H661 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;0O|IhcA>? NETjT4lFVVOR M364RmlEPTB;MUGuOFch|ryP MV2yN|k6OzN{OB?=
SK-MEL-28 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3f3fFczKGh? MUHEUXNQ MkTlTWM2OD1zMD65O{DPxE1? MV:yN|k6OzN{OB?=
SKOV3 NITyclRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PVPVczKGh? M{\sNmROW09? NF3lNJNKSzVyPUGyMlg2KM7:TR?= Mn7PNlM6QTN|Mki=
SNU5 MlXoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWj5WHJbPzJiaB?= MnHpSG1UVw>? MYDJR|UxRTBwMEG2JO69VQ>? M4\qbVI{QTl|M{K4
NCI-H2228 M1G2Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUO3NkBp MYfEUXNQ MYjJcohq[mm2aX;uJI9nKEGOSz3meZNqd25iZILpeoVvKGOnbHygdJJwdGmoZYLheIlwdiC5aYToJGlEPTBib3[gNE4yOThizszN Mkm1NlQ1OzJ7MEm=
NCI-H3122 NHq2TXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nndFczKGh? NG\MRoJFVVOR NFriWm1KdmirYnn0bY9vKG:oIFHMT{1nfXOrb36g[JJqfmWwIHPlcIwheHKxbHnm[ZJifGmxbjD3bZRpKEmFNUCgc4YhOC5zMEig{txO NHfZPJkzPDR|MkmwPS=>
NCI-H3122 M{fUfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHi2VWs4OiCq MnnrSG1UVw>? Mk[3TY5pcWKrdHnvckBw\iCDTFut[pV{cW:wIHTybZZmdiClZXzsJJBzd2yrZnXyZZRqd25iaX6gbJVu[W5iTlPJMWg{OTJ{IHPlcIx{KGijcnLvdolv\yCDTFugS|EzPjmDIH31eIFvfCC5aYToJGlEPTBib3[gNE43OjNizszN NXTodZJNOjR2M{K5NFk>
NCI-H3122 MnmxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzIO|IhcA>? M3G4V2ROW09? MX;Jcohq[mm2aX;uJI9nKEGOSz3meZNqd25iZILpeoVvKGOnbHygdJJwdGmoZYLheIlwdiCrbjDoeY1idiCQQ1mtTFMyOjJiY3XscJMhcGG{Yn;ybY5oKEGOSzDMNVE6Pk1ibYX0ZY51KHerdHigTWM2OCCxZjCwMlg{QCEQvF2= M2DXSVI1PDN{OUC5
NIH-3T3 NX[1dnBMU2mwYYPlJGF{e2G7 Moi1NUBp MX7EUXNQ NUfVfopUUW6qaXLpeIlwdiCxZjDoeY1idiC5aXzkJJR6eGViRV3MOE1nfXOnZDDBUGsh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IIDoc5NxcG:{eXzheIVlKEGOSzDs[ZZmdCC5aYToJGlEPTBib3[gNE4xQCEQvF2= NGLkcYszPDR|MkmwPS=>
NIH-3T3 MlfrT4lv[XOnIFHzd4F6 NETONVUyKGh? NUK3cJRKTE2VTx?= Ml;QTY5pcWKrdHnvckBw\iCqdX3hckBGVUx2LX\1d4VlKEGOSzDHNVI3QUFibYX0ZY51KGW6cILld5Nm\CCjc4Pld5Nm\CCjczDwbI9{eGixLVHMT{Bt\X[nbDD3bZRpKEmFNUCgc4YhOC54MEWg{txO NHL6[2wzPDR|MkmwPS=>
NIH-3T3 NHvqTotMcW6jc3WgRZN{[Xl? NWDBd25qOSCq Ml7nSG1UVw>? MYDJcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIGOxNlA3YSCvdYThcpQh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IIDoc5NxcG9vQVzLJIxmfmWuIIfpeIghUUN3MDDv[kAxNjZ{NjFOwG0> NVHPfGdbOjR2M{K5NFk>
NIH-3T3 NUX4fpVuU2mwYYPlJGF{e2G7 M4LWTVEhcA>? M33jW2ROW09? NVPERW82UW6qaXLpeIlwdiCxZjDoeY1idiCHTVy0MYZ2e2WmIFHMT{BNOTF7Nl2gcZV1[W62IHX4dJJme3OnZDDhd5Nme3OnZDDhd{BxcG:|cHjvMWFNUyCuZY\lcEB4cXSqIFnDOVAhd2ZiMD64OFMh|ryP MU[yOFQ{OjlyOR?=
NIH-3T3 MWHLbY5ie2ViQYPzZZk> MY[xJIg> MY\EUXNQ NULkUVF1UW6qaXLpeIlwdiCxZjDoeY1idiCHTVy0MYZ2e2WmIFHMT{BNOTF3MmKgcZV1[W62IHX4dJJme3OnZDDhd5Nme3OnZDDhd{BxcG:|cHjvMWFNUyCuZY\lcEB4cXSqIFnDOVAhd2ZiMT6wNlYh|ryP MmfRNlQ1OzJ7MEm=
BAF3 MVrGeY5kfGmxbjDBd5NigQ>? M2n1XFczKGh? Ml35SG1UVw>? MX;Jcohq[mm2aX;uJI9nKE6STT;BUGshfHKjboPm[YN1\WRiYYPz[ZN{\WRiYYOgZ4VtdCCpcn;3eIghcW6qaXLpeIlwdiC5aYToJGlEPTBib3[gNE4xPTFizszN MV6yOFQ3QDZ|Mh?=
BAF3 NXjxWot[S3m2b4TvfIlkKEG|c3H5 M1PtbVczKGh? M2Xl[WROW09? Mn;aTWM2OD1yLkm4JO69VQ>? NXq2b5FbOjR2Nki2N|I>
NIH-3T3 MorZT4lv[XOnIFHzd4F6 NFPpU2gyKGh? M4\HUGlvcGmkaYTpc44hd2ZiaIXtZY4hTU2OND3meZNm\CCDTFugSlEyPzSOIH31eIFvfCCneIDy[ZN{\WRiYYPz[ZN{\WRiYYOgdIhwe3Cqbz3BUGshdGW4ZXyge4l1cCCLQ{WwJI9nKDBwMU[1JO69VQ>? NH63SIEzPDhzOUGxOi=>
NIH-3T3 MVPLbY5ie2ViQYPzZZk> MmXnNUBp MX;Jcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIFOxNVU3YSCvdYThcpQh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IIDoc5NxcG9vQVzLJIxmfmWuIIfpeIghUUN3MDDv[kAxNjR5ODFOwG0> NUHxTWhtOjR6MUmxNVY>
NIH-3T3 NID4WWlMcW6jc3WgRZN{[Xl? NEewTnUyKGh? NWjqSnhlUW6qaXLpeIlwdiCxZjDoeY1idiCHTVy0MYZ2e2WmIFHMT{BIOTJyMmKgcZV1[W62IHX4dJJme3OnZDDhd5Nme3OnZDDhd{BxcG:|cHjvMWFNUyCuZY\lcEB4cXSqIFnDOVAhd2ZiMT6xOFgh|ryP NIPV[Y0zPDhzOUGxOi=>
NIH-3T3 MUXLbY5ie2ViQYPzZZk> NEPxWZcyKGh? NFqyOlRKdmirYnn0bY9vKG:oIHj1cYFvKEWPTESt[pV{\WRiQVzLJFEyPTGWaX7zJI12fGGwdDDlfJBz\XO|ZXSgZZN{\XO|ZXSgZZMheGixc4Doc{1CVEtibHX2[Ywhf2m2aDDJR|UxKG:oIEOuNFM6KM7:TR?= Mn[0NlQ5OTlzMU[=
KARPAS299 NX\udmdoU2mwYYPlJGF{e2G7 Mm[wPVAhdWmw M{fuTWROW09? NInCZVFKdmirYnn0bY9vKG:oIF7QUU1nfXOnZDDBUGsheGixc4Doc5J6dGG2aX;uJIV5eHKnc4Pl[EB4cXSqIFnDOVAhd2ZiMD6xNUDPxE1? MkDKNlQ6ODB5NUC=
MKN 45 NEnkR2VMcW6jc3WgRZN{[Xl? M1;MZVEhcA>? MYLEUXNQ NYW3ZXI2UW6qaXLpeIlwdiCxZjDjMW1mfCCyaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIECuNFIh|ryP NFLLbXMzPDlyMEe1NC=>
A549 MkXQR5l1d3SxeHnjJGF{e2G7 MYG0PEBp M{j6[GROW09? MYHJR|UxKG:oIESuNFg1KM7:TR?= MWiyOFkxODh|MB?=
NCI-H1975 NHT4NVJEgXSxdH;4bYMhSXO|YYm= M3z5blQ5KGh? MkXpSG1UVw>? Mmn0TWM2OCCxZjC3MlU2OSEQvF2= Mnv1NlQ6ODB6M{C=
NCI-H1993 MYHDfZRwfG:6aXOgRZN{[Xl? NVriNGJkPDhiaB?= Mo\rSG1UVw>? NFXmOYJKSzVyIH;mJFAvODZzIN88US=> MX6yOFkxODh|MB?=
NCI-H1993 NXvtTndFSXCxdH;zbZMhSXO|YYm= MlL2NUDPxE1? MYqyOEBp NF;MW|JFVVOR NXPyPJZk\G:nczDuc5QhcW6mdXPlJIFxd3C2b4Ppdy=> M4j5e|I1QTByOEOw
NIH-3T3 NUX6THVpS3m2b4TvfIlkKEG|c3H5 NV\uS4FuPDhiaB?= NFXEVY9FVVOR NYnrd5d6UUN3MDDv[kAxNjN4NDFOwG0> MU[yOFkxODh|MB?=
EBC1 MnTMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUW3NkBp NUfwZlVUTE2VTx?= Mnr6TWM2OCCxZjCwMlAxPjlizszN NX\5RXRROjR7MEC4N|E>
KARPAS299 M37zNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWK3NkBp MVvEUXNQ M3PROWlEPTBib3[gNE4zKM7:TR?= NF\ZW2MzPDlyMEizNS=>
NB1 M2nm[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvGbppKSzVyPUmxMlk5KG6P M4\WXHNCVkeHUh?=
NCI-SNU-5 M1Tz[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTFyNT63OUBvVQ>? NHHq[pdUSU6JRWK=
SR NUnQSGtWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrmTWM2OD1zMk[uN|Ehdk1? MYfTRW5ITVJ?
SF539 MkDMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTJyND6yOEBvVQ>? MUXTRW5ITVJ?
SU-DHL-1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTN|Nj64NkBvVQ>? NHzZNHlUSU6JRWK=
SCC-3 NYHWTIxzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGGxO|JKSzVyPUO1Ok44PiCwTR?= MoXZV2FPT0WU
DEL Ml\2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;xNYVpUUN3ME2zOlkvQSCwTR?= NFjw[G1USU6JRWK=
CTV-1 NEX5RW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\YTWM2OD13OU[uOFghdk1? MnTHV2FPT0WU
EM-2 M3jMTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vTdWlEPTB;NkCxMlM1KG6P NIn3fGVUSU6JRWK=
MHH-CALL-2 MoPxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7m[JlOUUN3ME22PFIvPTdibl2= NVLpS3UxW0GQR1XS
KM12 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInJfplKSzVyPUewOk46KG6P MUDTRW5ITVJ?
KINGS-1 MkHYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTaTWM2OD15NEmuO|Uhdk1? NYi5WllNW0GQR1XS
MEG-01 NXvFS4JXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7YTWM2OD16NUeuOlYhdk1? M1PWTHNCVkeHUh?=
BV-173 MnPHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjEOHZKSzVyPUGuNFU6QTdizszN MoDZV2FPT0WU
LAMA-84 MnXKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\JNmlEPTB;MT6zPFI5OiEQvF2= M{Hp[HNCVkeHUh?=
KARPAS-299 M1vXWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjlVWlKSzVyPUGuOFA5PjFizszN M4H4OXNCVkeHUh?=
K-562 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVu2WoV[UUN3ME2xMlczOjZ7IN88US=> MkfxV2FPT0WU
SK-LMS-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzzV45mUUN3ME2xMlc3QDZ5IN88US=> Mlu5V2FPT0WU
MOLT-16 NYW4ZWhVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jDemlEPTB;MT65OVU4PSEQvF2= M1u3V3NCVkeHUh?=
CMK NFn1eYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;1PXJSUUN3ME2xMlk3OTV7IN88US=> NWTme2tFW0GQR1XS
ST486 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LLfGlEPTB;Mj60N|A4OyEQvF2= NGjIU2JUSU6JRWK=
CI-1 MnW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWSweI9NUUN3ME2yMlQ6PjV7IN88US=> NXf5bpRnW0GQR1XS
KP-N-RT-BM-1 M4H4dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVW5OYRtUUN3ME2yMlcxOTJ{IN88US=> NYjzd3FSW0GQR1XS
ALL-PO MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjzW3RKSzVyPUOuNVgzODdizszN MontV2FPT0WU
KS-1 M4\kN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVnaTI1YUUN3ME2zMlIyOjJ3IN88US=> M2XqeXNCVkeHUh?=
Becker NFrrfFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTRwMkO5N{DPxE1? MV;TRW5ITVJ?
GDM-1 MlvoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmG3TWM2OD12LkK0OlE4KM7:TR?= NHiwfmZUSU6JRWK=
BC-1 M1O2Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4KzV2lEPTB;ND60PVI4PyEQvF2= MV;TRW5ITVJ?
NB14 MkS1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTRwOEO1NlQh|ryP MWLTRW5ITVJ?
NOS-1 NF75S|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXJVpNKSzVyPUWuN|M5PzRizszN MXXTRW5ITVJ?
MZ1-PC NVns[|lJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofYTWM2OD13LkiyNVUyKM7:TR?= NF7keGlUSU6JRWK=
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EW-16 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jBVGlEPTB;Nj6zO|c4OyEQvF2= NVjpNGZtW0GQR1XS
NALM-6 MorrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnDTWM2OD14Lk[4N|g4KM7:TR?= NVS4UlR3W0GQR1XS
EB-3 NWnJfmVMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHXZmZrUUN3ME23MlA4OjN|IN88US=> MmnEV2FPT0WU
697 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELQb3dKSzVyPUmuNlQ{OjlizszN MUjTRW5ITVJ?
Ramos-2G6-4C10 NWXiW3dQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnH5TWM2OD17LkW5PFQzKM7:TR?= NYm1TVZnW0GQR1XS
KNS-81-FD Mmr6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjibGltUUN3ME25MlY6PjV|IN88US=> M{e2U3NCVkeHUh?=
HUTU-80 MlTFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPlcHNuUUN3ME25Mlc1PjR{IN88US=> MXrTRW5ITVJ?
LS-411N MnfJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHmTWM2OD1zMD6wOVY4KM7:TR?= MV3TRW5ITVJ?
RPMI-8402 MkTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;P[GlEPTB;MUCuNVE3KM7:TR?= MUjTRW5ITVJ?
KU812 NEfZNYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTFyLkK5PVEh|ryP MVvTRW5ITVJ?
EW-1 MkDCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGD2dWNKSzVyPUGwMlQ1OjVizszN MWHTRW5ITVJ?
HC-1 NVW2WZMyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTFyLkS4OFQh|ryP MXfTRW5ITVJ?
NB69 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTFyLkWwOFMh|ryP MkD5V2FPT0WU
MFH-ino NF7KRYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\6TWM2OD1zMD64N|A{KM7:TR?= MX7TRW5ITVJ?
CCRF-CEM NFfS[HFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljhTWM2OD1zMT61PVch|ryP MUXTRW5ITVJ?
SK-N-DZ MmrpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTF{LkC0N|Yh|ryP M1XRWXNCVkeHUh?=
NCI-H720 NVzwfGxET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlv2TWM2OD1zMj6xO|A2KM7:TR?= M3zyd3NCVkeHUh?=
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KE-37 MkSwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonKTWM2OD1zMj63PVY3KM7:TR?= NGPNOIlUSU6JRWK=
HCC1599 NFLhd4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTLPJU3UUN3ME2xNk46ODZ7IN88US=> MnnxV2FPT0WU
A4-Fuk M1e3[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\lN2lEPTB;MUKuPVU5PiEQvF2= M1XmOHNCVkeHUh?=
NKM-1 NEHoPGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWe2cJlLUUN3ME2xN{4zQTJ3IN88US=> MX7TRW5ITVJ?
BE-13 NUPjXldMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jPZ2lEPTB;MUOuO|k5QSEQvF2= M1PzVHNCVkeHUh?=
MV-4-11 NFHQVlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkWwTWM2OD1zND6wN|I1KM7:TR?= NELjW4xUSU6JRWK=
OPM-2 NWHldItjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTF2LkSwPFUh|ryP M4XJN3NCVkeHUh?=
KARPAS-422 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zKZWlEPTB;MUSuOVEzPiEQvF2= M3\NUnNCVkeHUh?=
RPMI-8226 MmrvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HlcGlEPTB;MUSuPFkyPSEQvF2= MoTzV2FPT0WU
KARPAS-45 NF3EVpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTF3Lke3NVYh|ryP NWj0bG9FW0GQR1XS
SK-PN-DW Mlq3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTF3Lki2N|Eh|ryP NF;0TpJUSU6JRWK=
LC-2 NV\DNplyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHCTWM2OD1zNj6xOVA3KM7:TR?= NGewSppUSU6JRWK=
NCI-H1648 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXwTWM2OD1zNj6yOVQh|ryP M4rWcXNCVkeHUh?=
RL95-2 M3T3cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTF4LkO5O|gh|ryP M3e0fHNCVkeHUh?=
KNS-42 M2jyNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTF4LkeyO|Qh|ryP MkLwV2FPT0WU
RPMI-6666 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLWTWM2OD1zNj65NlEyKM7:TR?= NYfyUJRzW0GQR1XS
SIG-M5 M2n0cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;QRoRYUUN3ME2xO{4yQTB|IN88US=> MXnTRW5ITVJ?
VA-ES-BJ NUfxVohbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkizTWM2OD1zNz63OFUyKM7:TR?= NGrMV|JUSU6JRWK=
MONO-MAC-6 NE\1ZlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX71eVlSUUN3ME2xO{46OzF{IN88US=> M2Kx[3NCVkeHUh?=
LAN-6 NWnGO4ROT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mkm2TWM2OD1zOD63OVU4KM7:TR?= NI\k[2hUSU6JRWK=
A388 M1nWV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTF7LkOwOVkh|ryP MYXTRW5ITVJ?
SK-NEP-1 NVHhb5BCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PtfmlEPTB;MkCuNlE{OiEQvF2= MVLTRW5ITVJ?
TE-10 NF3DPVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTJyLkWyNlEh|ryP M{LqPXNCVkeHUh?=
HL-60 MoH5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTJyLkmwPVkh|ryP M1fhOnNCVkeHUh?=
MC116 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXtTWM2OD1{MT63NlIyKM7:TR?= NX2xVIZ5W0GQR1XS
SW962 NGHxbm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnreJp4UUN3ME2yNU44QTF3IN88US=> M{jEd3NCVkeHUh?=
NOMO-1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fSdmlEPTB;MkKuOlU3PCEQvF2= M3\DXXNCVkeHUh?=
CTB-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETGOZBKSzVyPUKyMlg3PzFizszN NXLkUWh5W0GQR1XS
MRK-nu-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTJ{LkmwO|Qh|ryP M{LQbXNCVkeHUh?=
GR-ST Mlq2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTJ|Lke2JO69VQ>? MVfTRW5ITVJ?
HH NGn2[lBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfVXYtMUUN3ME2yOE4xODNizszN NH;sOVlUSU6JRWK=
NCI-H1963 M1rCT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFq4bllKSzVyPUK0MlA4QDJizszN MYnTRW5ITVJ?
QIMR-WIL M1nrUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTJ2Lki3O|Ih|ryP NVzkPXBkW0GQR1XS
CGTH-W-1 NGnMPVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1yyemlEPTB;MkWuNFczOyEQvF2= NF3sfGVUSU6JRWK=
LP-1 NUjycIVxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTK[JJKSzVyPUK1MlY2PTFizszN M{ixS3NCVkeHUh?=
NCI-H748 NG\zU41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TacGlEPTB;Mk[uOVE{PyEQvF2= NGLafm9USU6JRWK=
PF-382 NGHi[XRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHJV4NKSzVyPUK3MlIzOjNizszN MnfJV2FPT0WU
ATN-1 MkjDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{izT2lEPTB;MkeuN|c{OiEQvF2= MYPTRW5ITVJ?
L-540 NWjG[lBUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTJ5Lk[0OVkh|ryP NFrWW2tUSU6JRWK=
LXF-289 Mnm0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXtTWM2OD1{Nz63OVE6KM7:TR?= Mn3kV2FPT0WU
LS-513 MkDuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXKTWM2OD1{OD6xPFA4KM7:TR?= NWnGO4xnW0GQR1XS
NCI-H1581 NUjpOGQ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3UTWM2OD1|MD6zPVc3KM7:TR?= MkLrV2FPT0WU
ES6 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnCNmxKSzVyPUOwMlY5QTlizszN NH23W4lUSU6JRWK=
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DOHH-2 NYS4eIw3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXrbWtvUUN3ME2zNU42QDl|IN88US=> MV7TRW5ITVJ?
DB NX:xUVNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTN|Lkm0N|Eh|ryP M{nMbHNCVkeHUh?=
MPP-89 NVn2VZlVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTN2LkG3OVYh|ryP MULTRW5ITVJ?
LB831-BLC MmjVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTN2LkWxPFQh|ryP NGfCOpVUSU6JRWK=
NB5 NHv2bY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17G[2lEPTB;M{SuPFU{PSEQvF2= M{fKfnNCVkeHUh?=
GB-1 Ml\CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrhfWlKSzVyPUO1MlA1PjlizszN Mnr1V2FPT0WU
TE-15 M{\BfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTN3LkKyN|gh|ryP NIDrZ2xUSU6JRWK=
LC4-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPwbI1UUUN3ME2zOU4{QDR5IN88US=> MYfTRW5ITVJ?
NCI-H747 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlX4TWM2OD1|Nj6xN|Y6KM7:TR?= M3fmW3NCVkeHUh?=
NTERA-S-cl-D1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfHS3pxUUN3ME2zPE44OzR5IN88US=> NYS0XYc1W0GQR1XS
SK-MM-2 Mk\WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\iNHFDUUN3ME20NE4yOTR4IN88US=> NEDRb5RUSU6JRWK=
TGW NGTEXIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTRzLkC1OlMh|ryP M3j4cXNCVkeHUh?=
ONS-76 NWrBRWJFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYe2Z2IxUUN3ME20Nk41QDh|IN88US=> M2TqSnNCVkeHUh?=
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ES4 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXyyN4pWUUN3ME20OE41OTV|IN88US=> NXHudY84W0GQR1XS
Daudi MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljZTWM2OD12NT6wPFI4KM7:TR?= MlK3V2FPT0WU
MOLT-4 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV20[JlvUUN3ME20OU4xQDV|IN88US=> MnLrV2FPT0WU
HT-144 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI[2U5VKSzVyPUS2MlczPiEQvF2= MXrTRW5ITVJ?
SW872 NYD3UGVmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTjN3l{UUN3ME20PE4yQTN|IN88US=> NHjJOY1USU6JRWK=
D-283MED NHrHbFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTR6LkO1OFIh|ryP MVfTRW5ITVJ?
NCI-H2126 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTR6Lki0O|Yh|ryP M{iyVXNCVkeHUh?=
NCI-SNU-16 MnPsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\hTWM2OD12OT6yNVQ{KM7:TR?= Mmf5V2FPT0WU
CESS NGfrNotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2j5TWlEPTB;NEmuOVA5QCEQvF2= NV70SHhQW0GQR1XS
A101D NEH0XYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV70dppVUUN3ME20PU46PzN4IN88US=> M1TKOXNCVkeHUh?=

... Click to View More Cell Line Experimental Data

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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