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

高品質保証

文献中の引用(65)

カスタマーフィードバック(8)

MSDS

製品説明

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

製品の説明

生物活性

製品説明 Crizotinib (PF-02341066) は1種の有効な小分子の卵白の阻害剤の再編人プロテインキナーゼ、 Kiが 4 nM。
ターゲット c-Met ALK
IC50 11 nM 24 nM [1]
In vitro試験 PF-2341066 displays similar potency against c-Met phosphorylation in mIMCD3 mouse or MDCK canine epithelial cells with IC50 of 5 nM and 20 nM, respectivly. PF-2341066 shows improved or similar activity against NIH3T3 cells engineered to express c-Met ATP-binding site mutants V1092I or H1094R or the P-loop mutant M1250T with IC50 of 19 nM, 2 nM and 15 nM, respectively, compared with NIH3T3 cells expressing wild-type receptor with IC50 of 13 nM. In contrast, a marked shift in potency of PF-2341066 is observed against cells engineered to express c-Met activation loop mutants Y1230C and Y1235D with IC50 of 127 nM and 92 nM, respectively, compared with wild-type receptor. PF-2341066 also potently prevents the phosphorylation of c-Met in NCI-H69 and HOP92 cells, with IC50 of 13 nM and 16 nM, respectively, which express the endogenous c-Met variants R988C and T1010I, respectively. PF-2341066 is >1,000-fold selective for the VEGFR2 and PDGFRβ RTKs, >250-fold selective for IRK and Lck, and ∼40- to 60-fold selective for Tie2, TrkA, and TrkB, all compared with c-Met. PF-2341066 is 20- to 30-fold selective for RON and Axl RTKs. In contrast, PF-2341066 shows a near-equivalent IC50 of 24 nM against the nucleophosmin (NPM)-anaplastic lymphoma kinase (ALK) oncogenic fusion variant of the ALK RTK expressed by the KARPAS299 human anaplastic large cell lymphoma (ALCL) cell line. PF-2341066 inhibits c-Met–dependent neoplastic phenotypes of cancer cells and angiogenic phenotypes of endothelial cells. PF-2341066 suppresses human GTL-16 gastric carcinoma cell growth with IC50 of 9.7 nM. PF-2341066 induces apoptosis in GTL-16 cells with IC50 of 8.4 nM. PF-2341066 inhibits HGF-stimulated human NCI-H441 lung carcinoma cell migration and invasion with IC50 of 11 nM and 6.1 nM, respectively. PF-2341066 inhibits MDCK cell scattering with IC50 of 16 nM. PF-2341066 prevents HGF-stimulated c-Met phosphorylation, cell survival, and Matrigel invasion with IC50 of 11 nM, 14 nM and 35 nM, respectively. In addition, PF-2341066 prevents serum-stimulated HMVEC branching tubulogenesis (formation of vascular tubes) in fibrin gels. [1] PF-2341066 also potently inhibits NPM-ALK phosphorylation in Karpas299 or SU-DHL-1 ALCL cells with an IC50 of 24 nM. PF-2341066 potently prevents cell proliferation, which is associated with G(1)-S-phase cell cycle arrest and induction of apoptosis in ALK-positive ALCL cells with IC50 of 30 nM, but not ALK-negative lymphoma cells. [2] Besides, PF-2341066 prevents osteosarcoma behavior associated with primary tumor growth (i.e., proliferation and survival) as well as metastasis (eg, invasion and clonogenicity). [3]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
BAF3 M{OyV2N6fG:2b4jpZ{BCe3OjeR?= MVG0PEBp MYrEUXNQ NGqyPWpEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBDSUZ|IHPlcIx{KGW6cILld5NqdmdiQVzLJGYyOTd2TDDteZRidnRiY3;lfJBz\XO|aX7nJGVOVDRid3n0bEBKSzVyIH;mJFAvPjJizszN M2\WdFIyPTd{NUi5
BAF3 Mlz6R5l1d3SxeHnjJGF{e2G7 M2jrblQ5KGh? M3X1VGROW09? NWLTWJk1S3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhSkGIMzDj[YxteyCneIDy[ZN{cW6pIFHMT{BNOTF7Nl2gcZV1[W62IHPv[ZhxemW|c3nu[{BGVUx2IIfpeIghUUN3MDDv[kAzNjJizszN NWXhc2U2OjF3N{K1PFk>
BAF3 M{LONWN6fG:2b4jpZ{BCe3OjeR?= NU[4e4VqPDhiaB?= MYTEUXNQ NXHjPZBxS3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhSkGIMzDj[YxteyCneIDy[ZN{cW6pIFXNUFQuSUyNIIfpeIghUUN3MDDv[kAxNjJ6IN88US=> MVWyNVU4OjV6OR?=
Kelly NHP3dFBEgXSxdH;4bYMhSXO|YYm= NWSxVYVKTE2VTx?= M{PkNmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGtmdGy7IHPlcIx{KGW6cILld5NqdmdiQVzLJGYyOTd2TDDteZRidnRid3n0bEBKSzVyIH;mJFAvPDJizszN NXz4TG41OjF3N{K1PFk>
SH-SY5Y M2rCfWN6fG:2b4jpZ{BCe3OjeR?= MYXEUXNQ NXixeFRkS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0hvU2m1XUBk\WyuczDlfJBz\XO|aX7nJGFNUyCIMUG3OGwhdXW2YX70JJdqfGhiSVO1NEBw\iByLkWzJO69VQ>? NUDqe|g{OjF3N{K1PFk>
SMS-KCN Ml2xR5l1d3SxeHnjJGF{e2G7 NGj0dlBFVVOR M3\mVGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNOWy2NQ16gZ4VtdHNiZYjwdoV{e2mwZzDBUGshWjF{N{XRJI12fGGwdDD3bZRpKEmFNUCgc4YhOC57MTFOwG0> NYnwVpIyOjF3N{K1PFk>
BAF3 MnrMR5l1d3SxeHnjJGF{e2G7 NWT1e2J1PDhiaB?= NIX6dYpFVVOR M1jUZWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KG2xdYPlJGJCTjNiY3XscJMh\XiycnXzd4lv\yCWZXytRWxMKHerdHigTWM2OCCxZjCwMlE6KM7:TR?= MX:yNVU4OjV6OR?=
3T3 MV;GeY5kfGmxbjDBd5NigQ>? MXKxJIg> M3fSbWROW09? MYjJcohq[mm2aX;uJI9nKFKRTjDhd5Nme3OnZDDhd{Boem:5dHig[oFkfG:{LXnu[JVk\WRiYYX0c5Bpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5yODFOwG0> M4j6NVIyQDF{NEG0
3T3-E MVjGeY5kfGmxbjDBd5NigQ>? NHzMSFUyKGh? M2DOZmROW09? M4H5bGlvcGmkaYTpc44hd2ZiVFnFNkBie3Onc4Pl[EBoem:5dHig[oFkfG:{LXnu[JVk\WRiYYX0c5Bpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC52NEig{txO NWjXVJRKOjF6MUK0NVQ>
A549 M13SSWtqdmG|ZTDBd5NigQ>? M{H1ZVEhcA>? M1nJTWROW09? MlHITY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCClLV3FWEBscW6jc3Wg[ZhxemW|c3XkJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gTGdHNWmwZIXj[YQh[XW2b4Doc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNE4xODhizszN NUDzb4ZEOjF6MUK0NVQ>
BAF3-BCL MlHqSpVv[3Srb36gRZN{[Xl? Mn;1NUBp NVfMOmltTE2VTx?= Mn7MTY5pcWKrdHnvckBw\iCDQlygZZN{\XO|ZXSgZZMh\3Kxd4ToJIZi[3Sxcj3pcoR2[2WmIHH1eI9xcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDFwMUW5JO69VQ>? M3rGSVIyQDF{NEG0
HEK293 NUPOR3ZNTnWwY4Tpc44hSXO|YYm= MX2xJIg> NYLXbmlTTE2VTx?= MlfjTY5pcWKrdHnvckBw\iCDWFygZZN{\XO|ZXSgZZMh\3Kxd4ToJIZi[3Sxcj3pcoR2[2WmIHH1eI9xcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMkm0JO69VQ>? NH;JeY8zOThzMkSxOC=>
HEK293 MlfQSpVv[3Srb36gRZN{[Xl? NXvC[os3OSCq M1i0XmROW09? MVrJcohq[mm2aX;uJI9nKEmUIHHzd4V{e2WmIHHzJIdzd3e2aDDmZYN1d3JvaX7keYNm\CCjdYTvdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAzNjh6NzFOwG0> M3X1ZVIyQDF{NEG0
Jurkat MVXGeY5kfGmxbjDBd5NigQ>? NWi1TYJJOSCq MlTzSG1UVw>? M4XSemlvcGmkaYTpc44hd2ZiTFPLJIF{e2W|c3XkJIF{KGe{b4f0bEBn[WO2b4KtbY5lfWOnZDDheZRweGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iB{Lke0NUDPxE1? NVrndI5SOjF6MUK0NVQ>
KARPAS299 M1rLRmtqdmG|ZTDBd5NigQ>? MYWxJIg> MofRSG1UVw>? MVzJcohq[mm2aX;uJI9nKEGOSzDhd5Nme3OnZDDhd{Boem:5dHig[oFkfG:{LXnu[JVk\WRiYYX0c5Bpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5yMjFOwG0> MYKyNVgyOjRzNB?=
PAE M{e4RWZ2dmO2aX;uJGF{e2G7 M3rZOFEhcA>? MYXEUXNQ NWWxRmxGUW6qaXLpeIlwdiCxZjDUVmtDKGG|c3Xzd4VlKGG|IHfyc5d1cCCoYXP0c5IucW6mdXPl[EBifXSxcHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCwMlM6QSEQvF2= MUOyNVgyOjRzNB?=
BAF3 MWHGeY5kfGmxbjDBd5NigQ>? M4P3cFIuOyCm M1LHZ2ROW09? NIj1SINKdmirYnn0bY9vKG:oIGTFUE1nfXOnZDDpcpN2dGmwIILlZ4VxfG:{IHX4dJJme3OnZDD3bZRpKEmFNUCgc4YhOS54NEOg{txO NVXXUYllOjN5NEKyOVI>
KARPAS299 MWfDfZRwfG:6aXOgRZN{[Xl? M4fTelIuOyCm MnLBSG1UVw>? MmiwTWM2OD1yLkC2OFIh|ryP M1XURVI{PzR{MkWy
EBC1 NFrae3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPJRmk4OiCq M1LSU2ROW09? M{PnbWlEPTB;MD6wNlMh|ryP NVPISXZzOjN7OUOzNlg>
HCT116 M{H4dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVu3NkBp NGf4OGFFVVOR MnHLTWM2OD1zND64NkDPxE1? NIDNbWwzOzl7M{OyPC=>
MCF7 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnu4O|IhcA>? M4X6e2ROW09? MmHUTWM2OD17LkW4JO69VQ>? NWG3OYdoOjN7OUOzNlg>
MDA-MB-231 MkPiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTVXnk4OiCq Mnn5SG1UVw>? MlPxTWM2OD1zMD64JO69VQ>? M3rENVI{QTl|M{K4
MKN45 MnuyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;pO|IhcA>? M1\U[WROW09? NHT6NJNKSzVyPUCuNFE{KM7:TR?= Mle4NlM6QTN|Mki=
NCI-H441 NVnIeWFlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjoO|IhcA>? Ml:wSG1UVw>? MofxTWM2OD1zNz6yOUDPxE1? MkjQNlM6QTN|Mki=
NCI-H661 NXrDe21yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUC3NkBp NWHqVIhETE2VTx?= NXPHZpZ6UUN3ME2xNU41PyEQvF2= Mnr1NlM6QTN|Mki=
SK-MEL-28 M3jmfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLTO|IhcA>? NVPXT3o2TE2VTx?= NGrT[mZKSzVyPUGwMlk4KM7:TR?= NXXPeG5GOjN7OUOzNlg>
SKOV3 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvTfok4OiCq NVW3[ohCTE2VTx?= NFu0Z3RKSzVyPUGyMlg2KM7:TR?= NFuxWWEzOzl7M{OyPC=>
SNU5 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;JNFczKGh? MWnEUXNQ NWrsPIpTUUN3ME2wMlAyPiEQvF2= M1HXSFI{QTl|M{K4
NCI-H2228 NEPpXY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHhO|IhcA>? NF2xbHdFVVOR NGPueotKdmirYnn0bY9vKG:oIFHMT{1nfXOrb36g[JJqfmWwIHPlcIwheHKxbHnm[ZJifGmxbjD3bZRpKEmFNUCgc4YhOC5zMUig{txO NUexZXVnOjR2M{K5NFk>
NCI-H3122 M3vMfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjiO|IhcA>? NFvsW49FVVOR M3fDUGlvcGmkaYTpc44hd2ZiQVzLMYZ2e2mxbjDkdol3\W5iY3XscEBxem:uaX\ldoF1cW:wIIfpeIghUUN3MDDv[kAxNjFyODFOwG0> NFHOZpgzPDR|MkmwPS=>
NCI-H3122 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3K2XFczKGh? M1f6RmROW09? M2Tj[WlvcGmkaYTpc44hd2ZiQVzLMYZ2e2mxbjDkdol3\W5iY3XscEBxem:uaX\ldoF1cW:wIHnuJIh2dWGwIF7DTU1JOzF{MjDj[YxteyCqYYLic5JqdmdiQVzLJGcyOjZ7QTDteZRidnRid3n0bEBKSzVyIH;mJFAvPjJ|IN88US=> M{\GZlI1PDN{OUC5
NCI-H3122 NISyXHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFO2S2g4OiCq NIPkcnhFVVOR MnjsTY5pcWKrdHnvckBw\iCDTFut[pV{cW:wIHTybZZmdiClZXzsJJBzd2yrZnXyZZRqd25iaX6gbJVu[W5iTlPJMWg{OTJ{IHPlcIx{KGijcnLvdolv\yCDTFugUFEyQT[PIH31eIFvfCC5aYToJGlEPTBib3[gNE45OzhizszN NYDoeGJOOjR2M{K5NFk>
NIH-3T3 MWfLbY5ie2ViQYPzZZk> MWixJIg> Mlq3SG1UVw>? NH2yS5RKdmirYnn0bY9vKG:oIHj1cYFvKHerbHSgeJlx\SCHTVy0MYZ2e2WmIFHMT{BmgHC{ZYPz[YQh[XO|ZYPz[YQh[XNicHjvd5Bpd3K7bHH0[YQhSUyNIHzleoVtKHerdHigTWM2OCCxZjCwMlA5KM7:TR?= M3rnfVI1PDN{OUC5
NIH-3T3 MnnXT4lv[XOnIFHzd4F6 MYGxJIg> M2HHSmROW09? M123NGlvcGmkaYTpc44hd2ZiaIXtZY4hTU2OND3meZNm\CCDTFugS|EzPjmDIH31eIFvfCCneIDy[ZN{\WRiYYPz[ZN{\WRiYYOgdIhwe3Cqbz3BUGshdGW4ZXyge4l1cCCLQ{WwJI9nKDBwNkC1JO69VQ>? MmK2NlQ1OzJ7MEm=
NIH-3T3 NILIeopMcW6jc3WgRZN{[Xl? NEXHXo8yKGh? MVLEUXNQ NUPJcnVSUW6qaXLpeIlwdiCxZjDoeY1idiCHTVy0MYZ2e2WmIFHMT{BUOTJyNmmgcZV1[W62IHX4dJJme3OnZDDhd5Nme3OnZDDhd{BxcG:|cHjvMWFNUyCuZY\lcEB4cXSqIFnDOVAhd2ZiMD62NlYh|ryP M3LLbVI1PDN{OUC5
NIH-3T3 MknoT4lv[XOnIFHzd4F6 MUCxJIg> MoXvSG1UVw>? MWDJcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIFyxNVk3VSCvdYThcpQh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IIDoc5NxcG9vQVzLJIxmfmWuIIfpeIghUUN3MDDv[kAxNjh2MzFOwG0> NHqwengzPDR|MkmwPS=>
NIH-3T3 NXTEdoE6U2mwYYPlJGF{e2G7 MWSxJIg> MXrEUXNQ MnT0TY5pcWKrdHnvckBw\iCqdX3hckBGVUx2LX\1d4VlKEGOSzDMNVE2OlJibYX0ZY51KGW6cILld5Nm\CCjc4Pld5Nm\CCjczDwbI9{eGixLVHMT{Bt\X[nbDD3bZRpKEmFNUCgc4YhOS5yMk[g{txO MYeyOFQ{OjlyOR?=
BAF3 MWTGeY5kfGmxbjDBd5NigQ>? MXu3NkBp NYrUTpM4TE2VTx?= NXnHRWlzUW6qaXLpeIlwdiCxZjDOVG0wSUyNIITyZY5{\mWldHXkJIF{e2W|c3XkJIF{KGOnbHyg[5Jwf3SqIHnubIljcXSrb36ge4l1cCCLQ{WwJI9nKDBwMEWxJO69VQ>? MXuyOFQ3QDZ|Mh?=
BAF3 MYLDfZRwfG:6aXOgRZN{[Xl? M4rNclczKGh? MUnEUXNQ MVLJR|UxRTBwOUig{txO MYCyOFQ3QDZ|Mh?=
NIH-3T3 NHT6S2FMcW6jc3WgRZN{[Xl? MmDkNUBp NUO3eGF{UW6qaXLpeIlwdiCxZjDoeY1idiCHTVy0MYZ2e2WmIFHMT{BHOTF5NFygcZV1[W62IHX4dJJme3OnZDDhd5Nme3OnZDDhd{BxcG:|cHjvMWFNUyCuZY\lcEB4cXSqIFnDOVAhd2ZiMD6xOlUh|ryP NFHOXnkzPDhzOUGxOi=>
NIH-3T3 NF\tbJJMcW6jc3WgRZN{[Xl? MV[xJIg> MXXJcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIFOxNVU3YSCvdYThcpQh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IIDoc5NxcG9vQVzLJIxmfmWuIIfpeIghUUN3MDDv[kAxNjR5ODFOwG0> M2X2VFI1QDF7MUG2
NIH-3T3 M1H6b2tqdmG|ZTDBd5NigQ>? MUWxJIg> MX;Jcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIFexNlAzWiCvdYThcpQh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IIDoc5NxcG9vQVzLJIxmfmWuIIfpeIghUUN3MDDv[kAyNjF2ODFOwG0> NHfEc3IzPDhzOUGxOi=>
NIH-3T3 NYr6OpkyU2mwYYPlJGF{e2G7 NGS1[5IyKGh? NIntO|RKdmirYnn0bY9vKG:oIHj1cYFvKEWPTESt[pV{\WRiQVzLJFEyPTGWaX7zJI12fGGwdDDlfJBz\XO|ZXSgZZN{\XO|ZXSgZZMheGixc4Doc{1CVEtibHX2[Ywhf2m2aDDJR|UxKG:oIEOuNFM6KM7:TR?= MVmyOFgyQTFzNh?=
KARPAS299 MUjLbY5ie2ViQYPzZZk> NXv3VHZiQTBibXnu NW\TUVdtTE2VTx?= NXr5cXlYUW6qaXLpeIlwdiCxZjDOVG0u\nW|ZXSgRWxMKHCqb4PwbI9zgWyjdHnvckBmgHC{ZYPz[YQhf2m2aDDJR|UxKG:oIECuNVEh|ryP NVKwS3BmOjR7MEC3OVA>
MKN 45 MmDmT4lv[XOnIFHzd4F6 Mm\tNUBp NFrsUHhFVVOR MlrxTY5pcWKrdHnvckBw\iClLV3leEBxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEKg{txO NVzib49OOjR7MEC3OVA>
A549 M37qe2N6fG:2b4jpZ{BCe3OjeR?= Ml\sOFghcA>? MkO2SG1UVw>? NH[2b41KSzVyIH;mJFQvODh2IN88US=> MXSyOFkxODh|MB?=
NCI-H1975 NUPibJpIS3m2b4TvfIlkKEG|c3H5 M1vO[lQ5KGh? Mom5SG1UVw>? Mnf2TWM2OCCxZjC3MlU2OSEQvF2= M1fuNlI1QTByOEOw
NCI-H1993 NF3BR29EgXSxdH;4bYMhSXO|YYm= MoDWOFghcA>? MlzwSG1UVw>? NHXPU3RKSzVyIH;mJFAvODZzIN88US=> NVL3WGpnOjR7MEC4N|A>
NCI-H1993 MoLIRZBwfG:|aYOgRZN{[Xl? M160VFEh|ryP NVm2V5J4OjRiaB?= MV;EUXNQ Mme4[I9meyCwb4SgbY5lfWOnIHHwc5B1d3Orcx?= M3PCcFI1QTByOEOw
NIH-3T3 M4O1S2N6fG:2b4jpZ{BCe3OjeR?= MXW0PEBp NHT4UWNFVVOR MmDPTWM2OCCxZjCwMlM3PCEQvF2= MlfGNlQ6ODB6M{C=
EBC1 M1TxRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHhfm0yPzJiaB?= NV3OdYkyTE2VTx?= M4XwW2lEPTBib3[gNE4xODZ7IN88US=> M2rHVlI1QTByOEOx
KARPAS299 MljLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vaZVczKGh? NF33elBFVVOR MWPJR|UxKG:oIECuNkDPxE1? Mk\tNlQ6ODB6M{G=
NB1 Mln5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PRUGlEPTB;OUGuPVghdk1? MlX5V2FPT0WU
NCI-SNU-5 NUG3ZoNsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTuTWM2OD1zMEWuO|Uhdk1? MmewV2FPT0WU
SR MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTF{Nj6zNUBvVQ>? M1PxT3NCVkeHUh?=
SF539 NW\Xe4FrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVW1dFBGUUN3ME2yNFQvOjRibl2= MXHTRW5ITVJ?
SU-DHL-1 MlPjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVn2UWdIUUN3ME2zN|YvQDJibl2= NIrI[2FUSU6JRWK=
SCC-3 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfTXoxKSzVyPUO1Ok44PiCwTR?= NYjUe49{W0GQR1XS
DEL MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTN4OT65JI5O MVXTRW5ITVJ?
CTV-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jlR2lEPTB;NUm2MlQ5KG6P MWPTRW5ITVJ?
EM-2 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmG4TWM2OD14MEGuN|Qhdk1? NWXWOllPW0GQR1XS
MHH-CALL-2 NYWzSYIyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zFW2lEPTB;NkiyMlU4KG6P M1KzS3NCVkeHUh?=
KM12 M2[wdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7k[4ZKSzVyPUewOk46KG6P NV7hZVVLW0GQR1XS
KINGS-1 NEfBNGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjYbI1DUUN3ME23OFkvPzVibl2= M2rJO3NCVkeHUh?=
MEG-01 NWfubpB5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfDT2lrUUN3ME24OVcvPjZibl2= MnHhV2FPT0WU
BV-173 M1jlcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7jWIRKSzVyPUGuNFU6QTdizszN M{jXRXNCVkeHUh?=
LAMA-84 NGnCXZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrWTWM2OD1zLkO4NlgzKM7:TR?= NWLQeZd2W0GQR1XS
KARPAS-299 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\PTWM2OD1zLkSwPFYyKM7:TR?= M3fXN3NCVkeHUh?=
K-562 NXThdnBET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkezTWM2OD1zLkeyNlY6KM7:TR?= NH6xUmhUSU6JRWK=
SK-LMS-1 M4i1[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnYeIdKSzVyPUGuO|Y5PjdizszN NV3pUplSW0GQR1XS
MOLT-16 NWfPd3FOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrM[|BNUUN3ME2xMlk2PTd3IN88US=> MWnTRW5ITVJ?
CMK MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1na[2lEPTB;MT65OlE2QSEQvF2= M3rmV3NCVkeHUh?=
ST486 M{f2Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmC2TWM2OD1{LkSzNFc{KM7:TR?= NITNc4xUSU6JRWK=
CI-1 M2rxeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzHUlRKSzVyPUKuOFk3PTlizszN MmfRV2FPT0WU
KP-N-RT-BM-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHDTWM2OD1{LkewNVIzKM7:TR?= MWPTRW5ITVJ?
ALL-PO M1HHbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljxTWM2OD1|LkG4NlA4KM7:TR?= Mmj1V2FPT0WU
KS-1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTNwMkGyNlUh|ryP NEn5Zo9USU6JRWK=
Becker NIDLcG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\PfZhKSzVyPUSuNlM6OyEQvF2= NUH2cmR6W0GQR1XS
GDM-1 Mm\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3v4c2lEPTB;ND6yOFYyPyEQvF2= NWn3dY1JW0GQR1XS
BC-1 NYfJO2dlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzV[HdKSzVyPUSuOFkzPzdizszN M2DpenNCVkeHUh?=
NB14 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTsZVhmUUN3ME20Mlg{PTJ2IN88US=> MUTTRW5ITVJ?
NOS-1 MnjSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\xSWlKSzVyPUWuN|M5PzRizszN MojCV2FPT0WU
MZ1-PC MmPrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTVwOEKxOVEh|ryP NGjNPWFUSU6JRWK=
A498 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LHRWlEPTB;Nj6wPFQ4OyEQvF2= NVHKdWY6W0GQR1XS
EW-16 NYfwTW5bT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;EXWlEPTB;Nj6zO|c4OyEQvF2= NWjaPW1SW0GQR1XS
NALM-6 NEDa[pZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1qyUmlEPTB;Nj62PFM5PyEQvF2= NH7LT5ZUSU6JRWK=
EB-3 M4Dn[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTdwMEeyN|Mh|ryP MnXzV2FPT0WU
697 M1;y[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjQTWM2OD17LkK0N|I6KM7:TR?= M3HHRnNCVkeHUh?=
Ramos-2G6-4C10 Mn\PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzONZB5UUN3ME25MlU6QDR{IN88US=> Mkf2V2FPT0WU
KNS-81-FD NV;IO3FsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTlwNkm2OVMh|ryP MUfTRW5ITVJ?
HUTU-80 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTlwN{S2OFIh|ryP MXvTRW5ITVJ?
LS-411N NXTITnZST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTFyLkC1Olch|ryP NGnLNpBUSU6JRWK=
RPMI-8402 MmPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jCVWlEPTB;MUCuNVE3KM7:TR?= M3XhRnNCVkeHUh?=
KU812 M{nJbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTFyLkK5PVEh|ryP M{TpW3NCVkeHUh?=
EW-1 M3:wVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVu4eXpYUUN3ME2xNE41PDJ3IN88US=> MW\TRW5ITVJ?
HC-1 Mlm5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTjVIZvUUN3ME2xNE41QDR2IN88US=> MYrTRW5ITVJ?
NB69 M1PhOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLITWM2OD1zMD61NFQ{KM7:TR?= NYDhcXJPW0GQR1XS
MFH-ino M2ny[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jYVmlEPTB;MUCuPFMxOyEQvF2= M1TCOXNCVkeHUh?=
CCRF-CEM M1LvN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTFzLkW5O{DPxE1? NYW4TnhEW0GQR1XS
SK-N-DZ NUDHTYk6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjsTWM2OD1zMj6wOFM3KM7:TR?= NIfnS3FUSU6JRWK=
NCI-H720 NXT1WnExT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGjrPZdKSzVyPUGyMlE4ODVizszN MWfTRW5ITVJ?
HCC1187 M2C4XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTOTWM2OD1zMj6yNFQyKM7:TR?= MWPTRW5ITVJ?
IST-SL2 MlLTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGCwe4tKSzVyPUGyMlQ5PzJizszN M1XSbnNCVkeHUh?=
KE-37 M33LVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\MTWM2OD1zMj63PVY3KM7:TR?= MonUV2FPT0WU
HCC1599 MmfsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTF{LkmwOlkh|ryP MlTOV2FPT0WU
A4-Fuk MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPLN4dHUUN3ME2xNk46PTh4IN88US=> MWLTRW5ITVJ?
NKM-1 NHr5PWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4[zfWlEPTB;MUOuNlkzPSEQvF2= NEO0N4tUSU6JRWK=
BE-13 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvL[3lKSzVyPUGzMlc6QDlizszN M4DZTHNCVkeHUh?=
MV-4-11 MlHpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\XTWM2OD1zND6wN|I1KM7:TR?= NEK0SpJUSU6JRWK=
OPM-2 M4DwWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPEeYo4UUN3ME2xOE41ODh3IN88US=> NVL6eVNmW0GQR1XS
KARPAS-422 MlrHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfCdXhEUUN3ME2xOE42OTJ4IN88US=> NXL1ZVh[W0GQR1XS
RPMI-8226 MoHxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnXSnhkUUN3ME2xOE45QTF3IN88US=> NWro[Ho{W0GQR1XS
KARPAS-45 NYS3fGd{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXOxSIx6UUN3ME2xOU44PzF4IN88US=> MXzTRW5ITVJ?
SK-PN-DW MnTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTF3Lki2N|Eh|ryP NYTOVVF3W0GQR1XS
LC-2 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTF4LkG1NFYh|ryP NIqxVZFUSU6JRWK=
NCI-H1648 MnTvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTF4LkK1OEDPxE1? MnfEV2FPT0WU
RL95-2 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYXJR|UxRTF4LkO5O|gh|ryP NHe1[XdUSU6JRWK=
KNS-42 M4nRSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfZXXBKSzVyPUG2MlczPzRizszN NH[yZ3hUSU6JRWK=
RPMI-6666 NVHOfIxzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVyxPWJ3UUN3ME2xOk46OjFzIN88US=> Mln5V2FPT0WU
SIG-M5 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7IRlF7UUN3ME2xO{4yQTB|IN88US=> NWCxVZlrW0GQR1XS
VA-ES-BJ NXfrbVhrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXkN25KSzVyPUG3Mlc1PTFizszN M3PWWnNCVkeHUh?=
MONO-MAC-6 NYm2XGJjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjzTWM2OD1zNz65N|EzKM7:TR?= NG[xNYhUSU6JRWK=
LAN-6 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1za[WlEPTB;MUiuO|U2PyEQvF2= NXfOfW5jW0GQR1XS
A388 M3f3fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGew[pRKSzVyPUG5MlMxPTlizszN MljVV2FPT0WU
SK-NEP-1 NXrDSoxOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTJyLkKxN|Ih|ryP MoPqV2FPT0WU
TE-10 NWnFd2t4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTJyLkWyNlEh|ryP MnrKV2FPT0WU
HL-60 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTJyLkmwPVkh|ryP NEL3ZllUSU6JRWK=
MC116 M2\kfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33pU2lEPTB;MkGuO|IzOSEQvF2= MmPTV2FPT0WU
SW962 Ml;3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTJzLke5NVUh|ryP MWfTRW5ITVJ?
NOMO-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTxTWM2OD1{Mj62OVY1KM7:TR?= MWjTRW5ITVJ?
CTB-1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjoSJlKSzVyPUKyMlg3PzFizszN MlnqV2FPT0WU
MRK-nu-1 NHT3cJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zI[WlEPTB;MkKuPVA4PCEQvF2= NX:0RXVlW0GQR1XS
GR-ST M2TYTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XmU2lEPTB;MkOuO|Yh|ryP NES0N4tUSU6JRWK=
HH MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LNUGlEPTB;MkSuNFA{KM7:TR?= M1vIeHNCVkeHUh?=
NCI-H1963 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3mTWM2OD1{ND6wO|gzKM7:TR?= NX[xeYFkW0GQR1XS
QIMR-WIL MoTaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrXSHBKSzVyPUK0Mlg4PzJizszN NUXOUYd6W0GQR1XS
CGTH-W-1 M3vBbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XJOmlEPTB;MkWuNFczOyEQvF2= MlLaV2FPT0WU
LP-1 NXXOUpVFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;MXHVUUUN3ME2yOU43PTVzIN88US=> MkX6V2FPT0WU
NCI-H748 M{DlOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLPTWM2OD1{Nj61NVM4KM7:TR?= M3X4UnNCVkeHUh?=
PF-382 NWfrdpo1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{C3ZmlEPTB;MkeuNlIzOyEQvF2= Mn3tV2FPT0WU
ATN-1 M{TjN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjsdGU5UUN3ME2yO{4{PzN{IN88US=> NVLtO3R6W0GQR1XS
L-540 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTHbYhKUUN3ME2yO{43PDV7IN88US=> MW\TRW5ITVJ?
LXF-289 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjDTWM2OD1{Nz63OVE6KM7:TR?= M4PYenNCVkeHUh?=
LS-513 MnHTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jITWlEPTB;MkiuNVgxPyEQvF2= NU\VS3I4W0GQR1XS
NCI-H1581 MkjmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTNyLkO5O|Yh|ryP MX3TRW5ITVJ?
ES6 M4PQZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;zTWM2OD1|MD62PFk6KM7:TR?= Ml[zV2FPT0WU
SW982 MofLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLpTWM2OD1|MD64OVY3KM7:TR?= NGPnSZlUSU6JRWK=
DOHH-2 M{fwfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXvT2xKSzVyPUOxMlU5QTNizszN MWDTRW5ITVJ?
DB MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTHS5VqUUN3ME2zN{46PDNzIN88US=> MY\TRW5ITVJ?
MPP-89 NGHXUZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4q2emlEPTB;M{SuNVc2PiEQvF2= NEHab4NUSU6JRWK=
LB831-BLC MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\td4tOUUN3ME2zOE42OTh2IN88US=> NWTGNpp1W0GQR1XS
NB5 NV22SYxoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnn[YVxUUN3ME2zOE45PTN3IN88US=> NGC3TFhUSU6JRWK=
GB-1 NHfRVmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTN3LkC0Olkh|ryP Mk[wV2FPT0WU
TE-15 Ml7aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;WTWM2OD1|NT6yNlM5KM7:TR?= M3u2cHNCVkeHUh?=
LC4-1 NYTYSZNVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljRTWM2OD1|NT6zPFQ4KM7:TR?= MVLTRW5ITVJ?
NCI-H747 M3i0T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfjb25KSzVyPUO2MlE{PjlizszN MVvTRW5ITVJ?
NTERA-S-cl-D1 MkTrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrub2s3UUN3ME2zPE44OzR5IN88US=> M1zC[3NCVkeHUh?=
SK-MM-2 NFnSe5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonlTWM2OD12MD6xNVQ3KM7:TR?= MlHSV2FPT0WU
TGW NIPDTpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4rROWlEPTB;NEGuNFU3OyEQvF2= MVjTRW5ITVJ?
ONS-76 NGL0fWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTR{LkS4PFMh|ryP MVrTRW5ITVJ?
CPC-N M4joTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITJbo5KSzVyPUSyMlk6PzFizszN MWLTRW5ITVJ?
ES4 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3nT[GlEPTB;NESuOFE2OyEQvF2= MVnTRW5ITVJ?
Daudi NVrVbI51T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTR3LkC4Nlch|ryP MYrTRW5ITVJ?
MOLT-4 NIjs[m5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\QcY9KSzVyPUS1MlA5PTNizszN M1\0cHNCVkeHUh?=
HT-144 M17ReGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEL6N5ZKSzVyPUS2MlczPiEQvF2= NIXnV2hUSU6JRWK=
SW872 MknhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fVN2lEPTB;NEiuNVk{OyEQvF2= M3jhS3NCVkeHUh?=
D-283MED MnjyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTR6LkO1OFIh|ryP MWPTRW5ITVJ?
NCI-H2126 NY\4SVV[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofITWM2OD12OD64OFc3KM7:TR?= MUTTRW5ITVJ?
NCI-SNU-16 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfCPGVMUUN3ME20PU4zOTR|IN88US=> NVj5WXg2W0GQR1XS
CESS NFPDUmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfY[phKSzVyPUS5MlUxQDhizszN MYjTRW5ITVJ?
A101D NUjHT5pLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTR7Lkm3N|Yh|ryP MlLuV2FPT0WU

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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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