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

高品質保証

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Quality Control & MSDS

製品説明

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

製品の説明

生物活性

製品説明 Crizotinib (PF-02341066) は1種の有効な小分子の卵白の阻害剤の再編人プロテインキナーゼ、 Kiが 4 nM。
ターゲット c-Met ALK
IC50 11 nM 24 nM [1]
In vitro試験 PF-2341066 displays similar potency against c-Met phosphorylation in mIMCD3 mouse or MDCK canine epithelial cells with IC50 of 5 nM and 20 nM, respectivly. PF-2341066 shows improved or similar activity against NIH3T3 cells engineered to express c-Met ATP-binding site mutants V1092I or H1094R or the P-loop mutant M1250T with IC50 of 19 nM, 2 nM and 15 nM, respectively, compared with NIH3T3 cells expressing wild-type receptor with IC50 of 13 nM. In contrast, a marked shift in potency of PF-2341066 is observed against cells engineered to express c-Met activation loop mutants Y1230C and Y1235D with IC50 of 127 nM and 92 nM, respectively, compared with wild-type receptor. PF-2341066 also potently prevents the phosphorylation of c-Met in NCI-H69 and HOP92 cells, with IC50 of 13 nM and 16 nM, respectively, which express the endogenous c-Met variants R988C and T1010I, respectively. PF-2341066 is >1,000-fold selective for the VEGFR2 and PDGFRβ RTKs, >250-fold selective for IRK and Lck, and ∼40- to 60-fold selective for Tie2, TrkA, and TrkB, all compared with c-Met. PF-2341066 is 20- to 30-fold selective for RON and Axl RTKs. In contrast, PF-2341066 shows a near-equivalent IC50 of 24 nM against the nucleophosmin (NPM)-anaplastic lymphoma kinase (ALK) oncogenic fusion variant of the ALK RTK expressed by the KARPAS299 human anaplastic large cell lymphoma (ALCL) cell line. PF-2341066 inhibits c-Met–dependent neoplastic phenotypes of cancer cells and angiogenic phenotypes of endothelial cells. PF-2341066 suppresses human GTL-16 gastric carcinoma cell growth with IC50 of 9.7 nM. PF-2341066 induces apoptosis in GTL-16 cells with IC50 of 8.4 nM. PF-2341066 inhibits HGF-stimulated human NCI-H441 lung carcinoma cell migration and invasion with IC50 of 11 nM and 6.1 nM, respectively. PF-2341066 inhibits MDCK cell scattering with IC50 of 16 nM. PF-2341066 prevents HGF-stimulated c-Met phosphorylation, cell survival, and Matrigel invasion with IC50 of 11 nM, 14 nM and 35 nM, respectively. In addition, PF-2341066 prevents serum-stimulated HMVEC branching tubulogenesis (formation of vascular tubes) in fibrin gels. [1] PF-2341066 also potently inhibits NPM-ALK phosphorylation in Karpas299 or SU-DHL-1 ALCL cells with an IC50 of 24 nM. PF-2341066 potently prevents cell proliferation, which is associated with G(1)-S-phase cell cycle arrest and induction of apoptosis in ALK-positive ALCL cells with IC50 of 30 nM, but not ALK-negative lymphoma cells. [2] Besides, PF-2341066 prevents osteosarcoma behavior associated with primary tumor growth (i.e., proliferation and survival) as well as metastasis (eg, invasion and clonogenicity). [3]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
BAF3 M2W3NmN6fG:2b4jpZ{BCe3OjeR?= M2\NT|Q5KGh? MlH5SG1UVw>? NIrS[o9EgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBDSUZ|IHPlcIx{KGW6cILld5NqdmdiQVzLJGYyOTd2TDDteZRidnRiY3;lfJBz\XO|aX7nJGVOVDRid3n0bEBKSzVyIH;mJFAvPjJizszN M3q5S|IyPTd{NUi5
BAF3 NYXXO4JLS3m2b4TvfIlkKEG|c3H5 NXSzb3NxPDhiaB?= M{\iZWROW09? NYG0ZXlFS3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhSkGIMzDj[YxteyCneIDy[ZN{cW6pIFHMT{BNOTF7Nl2gcZV1[W62IHPv[ZhxemW|c3nu[{BGVUx2IIfpeIghUUN3MDDv[kAzNjJizszN MkXoNlE2PzJ3OEm=
BAF3 MkjIR5l1d3SxeHnjJGF{e2G7 M{O3cVQ5KGh? NHHO[21FVVOR NV3MRXU2S3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhSkGIMzDj[YxteyCneIDy[ZN{cW6pIFXNUFQuSUyNIIfpeIghUUN3MDDv[kAxNjJ6IN88US=> NGXxPZYzOTV5MkW4PS=>
Kelly MXrDfZRwfG:6aXOgRZN{[Xl? M4PaZmROW09? NGjxPJhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBM\WyueTDj[YxteyCneIDy[ZN{cW6pIFHMT{BHOTF5NFygcZV1[W62IIfpeIghUUN3MDDv[kAxNjR{IN88US=> MXmyNVU4OjV6OR?=
SH-SY5Y NEfnR3VEgXSxdH;4bYMhSXO|YYm= MmPUSG1UVw>? M17BUWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNJNVO\NWmgZ4VtdHNiZYjwdoV{e2mwZzDBUGshTjFzN{TMJI12fGGwdDD3bZRpKEmFNUCgc4YhOC53MzFOwG0> NYK4Ood[OjF3N{K1PFk>
SMS-KCN M4HMcWN6fG:2b4jpZ{BCe3OjeR?= M3;nNGROW09? MoLER5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV21UNUuFTjDj[YxteyCneIDy[ZN{cW6pIFHMT{BTOTJ5NWGgcZV1[W62IIfpeIghUUN3MDDv[kAxNjlzIN88US=> MoHvNlE2PzJ3OEm=
BAF3 Ml3KR5l1d3SxeHnjJGF{e2G7 MU[0PEBp M1LGe2ROW09? MnLwR5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgRmFHOyClZXzsd{BmgHC{ZYPzbY5oKFSnbD3BUGshf2m2aDDJR|UxKG:oIECuNVkh|ryP M1rNWFIyPTd{NUi5
3T3 MU\GeY5kfGmxbjDBd5NigQ>? MmfxNUBp NFjDVIVFVVOR NYjKXItIUW6qaXLpeIlwdiCxZjDSU24h[XO|ZYPz[YQh[XNiZ4Lve5RpKG[jY4Tvdk1qdmS3Y3XkJIF2fG:yaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIECuNFgh|ryP NFHkTG4zOThzMkSxOC=>
3T3-E MlzlSpVv[3Srb36gRZN{[Xl? NIHyb2cyKGh? NF\yfGlFVVOR MkjMTY5pcWKrdHnvckBw\iCWSVWyJIF{e2W|c3XkJIdzd3e2aDDmZYN1d3JvaX7keYNm\CCjdYTvdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjR2ODFOwG0> M4D5VVIyQDF{NEG0
A549 NXTPd28{U2mwYYPlJGF{e2G7 M4r0XlEhcA>? MmPqSG1UVw>? MWnJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KGNvTVXUJItqdmG|ZTDlfJBz\XO|ZXSgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDIS2YucW6mdXPl[EBifXSxcHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCwMlAxQCEQvF2= MWeyNVgyOjRzNB?=
BAF3-BCL NHTWPZRHfW6ldHnvckBCe3OjeR?= MXSxJIg> M3PlNGROW09? MljCTY5pcWKrdHnvckBw\iCDQlygZZN{\XO|ZXSgZZMh\3Kxd4ToJIZi[3Sxcj3pcoR2[2WmIHH1eI9xcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDFwMUW5JO69VQ>? NGnBZ5YzOThzMkSxOC=>
HEK293 MXLGeY5kfGmxbjDBd5NigQ>? NE\yOZcyKGh? MXLEUXNQ MXfJcohq[mm2aX;uJI9nKEG[TDDhd5Nme3OnZDDhd{Boem:5dHig[oFkfG:{LXnu[JVk\WRiYYX0c5Bpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5{OUSg{txO MoPUNlE5OTJ2MUS=
HEK293 NHy3[GxHfW6ldHnvckBCe3OjeR?= MlezNUBp NYfz[|VbTE2VTx?= MUDJcohq[mm2aX;uJI9nKEmUIHHzd4V{e2WmIHHzJIdzd3e2aDDmZYN1d3JvaX7keYNm\CCjdYTvdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAzNjh6NzFOwG0> NF;WXY8zOThzMkSxOC=>
Jurkat M4HlSGZ2dmO2aX;uJGF{e2G7 NXjaeXcxOSCq MXLEUXNQ M2HjVmlvcGmkaYTpc44hd2ZiTFPLJIF{e2W|c3XkJIF{KGe{b4f0bEBn[WO2b4KtbY5lfWOnZDDheZRweGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iB{Lke0NUDPxE1? NWG4PHVZOjF6MUK0NVQ>
KARPAS299 M13McGtqdmG|ZTDBd5NigQ>? MW[xJIg> M2HZTmROW09? M{m2TGlvcGmkaYTpc44hd2ZiQVzLJIF{e2W|c3XkJIF{KGe{b4f0bEBn[WO2b4KtbY5lfWOnZDDheZRweGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCyJO69VQ>? M{T0SFIyQDF{NEG0
PAE NUm5doFMTnWwY4Tpc44hSXO|YYm= NXzEeGEzOSCq NGHydG5FVVOR NGT1PYpKdmirYnn0bY9vKG:oIGTST2Ih[XO|ZYPz[YQh[XNiZ4Lve5RpKG[jY4Tvdk1qdmS3Y3XkJIF2fG:yaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIECuN|k6KM7:TR?= MlPQNlE5OTJ2MUS=
BAF3 M4H6XWZ2dmO2aX;uJGF{e2G7 MV6yMVMh\A>? NUm3VokyTE2VTx?= MnnOTY5pcWKrdHnvckBw\iCWRVyt[pV{\WRiaX7zeYxqdiC{ZXPldJRweiCneIDy[ZN{\WRid3n0bEBKSzVyIH;mJFEvPjR|IN88US=> Mn65NlM4PDJ{NUK=
KARPAS299 NYDqZmxpS3m2b4TvfIlkKEG|c3H5 M4L3d|IuOyCm MWjEUXNQ NGTmWmdKSzVyPUCuNFY1OiEQvF2= M{nkVVI{PzR{MkWy
EBC1 M3HkdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDGO|IhcA>? M376b2ROW09? MUnJR|UxRTBwMEKzJO69VQ>? M1fZcFI{QTl|M{K4
HCT116 NYLicohST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlW2O|IhcA>? MnTPSG1UVw>? MY\JR|UxRTF2LkiyJO69VQ>? M2X0cFI{QTl|M{K4
MCF7 NVrSbZZ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnYdnhQPzJiaB?= NGLCRpJFVVOR MkTaTWM2OD17LkW4JO69VQ>? M{jqW|I{QTl|M{K4
MDA-MB-231 NHTSWmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHUUJJlPzJiaB?= Mlr5SG1UVw>? M3vOe2lEPTB;MUCuPEDPxE1? M2jZbFI{QTl|M{K4
MKN45 NILZZ3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\HO|IhcA>? NH72NYRFVVOR NEjxXGRKSzVyPUCuNFE{KM7:TR?= M33VbFI{QTl|M{K4
NCI-H441 NGDUU|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXDfIZVPzJiaB?= MVXEUXNQ NWfRbYhoUUN3ME2xO{4zPSEQvF2= M1;CdVI{QTl|M{K4
NCI-H661 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX[3NkBp MWDEUXNQ Mom2TWM2OD1zMT60O{DPxE1? MWeyN|k6OzN{OB?=
SK-MEL-28 NVz1Z|lZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rPPVczKGh? M2PtbWROW09? Mn\6TWM2OD1zMD65O{DPxE1? M{\G[VI{QTl|M{K4
SKOV3 NITYTZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jrdlczKGh? NGnGdWVFVVOR MmLFTWM2OD1zMj64OUDPxE1? Moq4NlM6QTN|Mki=
SNU5 M3LLR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmWyO|IhcA>? MXzEUXNQ MWPJR|UxRTBwMEG2JO69VQ>? MkTKNlM6QTN|Mki=
NCI-H2228 M2fHfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWm3NkBp MnTySG1UVw>? NVXlbGRRUW6qaXLpeIlwdiCxZjDBUGsu\nW|aX;uJIRzcX[nbjDj[YxtKHC{b3zp[oVz[XSrb36ge4l1cCCLQ{WwJI9nKDBwMUG4JO69VQ>? NEmyOFQzPDR|MkmwPS=>
NCI-H3122 NHH0SmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4j3RlczKGh? M3PU[WROW09? M{SxV2lvcGmkaYTpc44hd2ZiQVzLMYZ2e2mxbjDkdol3\W5iY3XscEBxem:uaX\ldoF1cW:wIIfpeIghUUN3MDDv[kAxNjFyODFOwG0> NIrKXpMzPDR|MkmwPS=>
NCI-H3122 MmWyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17he|czKGh? NEfWWJNFVVOR NWLsS3F1UW6qaXLpeIlwdiCxZjDBUGsu\nW|aX;uJIRzcX[nbjDj[YxtKHC{b3zp[oVz[XSrb36gbY4hcHWvYX6gUmNKNUh|MUKyJINmdGy|IHjhdoJwemmwZzDBUGshTzF{NknBJI12fGGwdDD3bZRpKEmFNUCgc4YhOC54MkOg{txO NVLCWFlMOjR2M{K5NFk>
NCI-H3122 NWrObGt4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmn5O|IhcA>? NISwXlNFVVOR MXjJcohq[mm2aX;uJI9nKEGOSz3meZNqd25iZILpeoVvKGOnbHygdJJwdGmoZYLheIlwdiCrbjDoeY1idiCQQ1mtTFMyOjJiY3XscJMhcGG{Yn;ybY5oKEGOSzDMNVE6Pk1ibYX0ZY51KHerdHigTWM2OCCxZjCwMlg{QCEQvF2= MUeyOFQ{OjlyOR?=
NIH-3T3 M4DremtqdmG|ZTDBd5NigQ>? MYOxJIg> NW\V[HVDTE2VTx?= NVW1OnVlUW6qaXLpeIlwdiCxZjDoeY1idiC5aXzkJJR6eGViRV3MOE1nfXOnZDDBUGsh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IIDoc5NxcG:{eXzheIVlKEGOSzDs[ZZmdCC5aYToJGlEPTBib3[gNE4xQCEQvF2= MWmyOFQ{OjlyOR?=
NIH-3T3 MYfLbY5ie2ViQYPzZZk> M4nNdFEhcA>? MYHEUXNQ MljETY5pcWKrdHnvckBw\iCqdX3hckBGVUx2LX\1d4VlKEGOSzDHNVI3QUFibYX0ZY51KGW6cILld5Nm\CCjc4Pld5Nm\CCjczDwbI9{eGixLVHMT{Bt\X[nbDD3bZRpKEmFNUCgc4YhOC54MEWg{txO Mn\0NlQ1OzJ7MEm=
NIH-3T3 MWDLbY5ie2ViQYPzZZk> NG\JTW8yKGh? NFvOVHZFVVOR NXizVmJYUW6qaXLpeIlwdiCxZjDoeY1idiCHTVy0MYZ2e2WmIFHMT{BUOTJyNmmgcZV1[W62IHX4dJJme3OnZDDhd5Nme3OnZDDhd{BxcG:|cHjvMWFNUyCuZY\lcEB4cXSqIFnDOVAhd2ZiMD62NlYh|ryP M3e2fVI1PDN{OUC5
NIH-3T3 NYnjPWQ6U2mwYYPlJGF{e2G7 NXXl[WlEOSCq NEP1SGRFVVOR NIfudlhKdmirYnn0bY9vKG:oIHj1cYFvKEWPTESt[pV{\WRiQVzLJGwyOTl4TTDteZRidnRiZYjwdoV{e2WmIHHzd4V{e2WmIHHzJJBpd3OyaH:tRWxMKGyndnXsJJdqfGhiSVO1NEBw\iByLki0N{DPxE1? M1POVlI1PDN{OUC5
NIH-3T3 MYLLbY5ie2ViQYPzZZk> M4XyfFEhcA>? MVrEUXNQ MVjJcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIFyxNVUzWiCvdYThcpQh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IIDoc5NxcG9vQVzLJIxmfmWuIIfpeIghUUN3MDDv[kAyNjB{NjFOwG0> NX2xeXBVOjR2M{K5NFk>
BAF3 NITERZdHfW6ldHnvckBCe3OjeR?= M4\JOlczKGh? MXnEUXNQ M3j2[GlvcGmkaYTpc44hd2ZiTmDNM2FNUyC2cnHud4Zm[3SnZDDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIIfpeIghUUN3MDDv[kAxNjB3MTFOwG0> Mn\tNlQ1Pjh4M{K=
BAF3 M2rycmN6fG:2b4jpZ{BCe3OjeR?= NVnFcXZPPzJiaB?= MXvEUXNQ NGnJb|ZKSzVyPUCuPVgh|ryP NUS0bnQzOjR2Nki2N|I>
NIH-3T3 M4GxOGtqdmG|ZTDBd5NigQ>? NGGxOo8yKGh? NH\LR4RKdmirYnn0bY9vKG:oIHj1cYFvKEWPTESt[pV{\WRiQVzLJGYyOTd2TDDteZRidnRiZYjwdoV{e2WmIHHzd4V{e2WmIHHzJJBpd3OyaH:tRWxMKGyndnXsJJdqfGhiSVO1NEBw\iByLkG2OUDPxE1? Mn7iNlQ5OTlzMU[=
NIH-3T3 NE\FdVdMcW6jc3WgRZN{[Xl? NFLuXlQyKGh? NV\CNYRbUW6qaXLpeIlwdiCxZjDoeY1idiCHTVy0MYZ2e2WmIFHMT{BEOTF3NmmgcZV1[W62IHX4dJJme3OnZDDhd5Nme3OnZDDhd{BxcG:|cHjvMWFNUyCuZY\lcEB4cXSqIFnDOVAhd2ZiMD60O|gh|ryP M{j2OFI1QDF7MUG2
NIH-3T3 MVPLbY5ie2ViQYPzZZk> NWXwOlhKOSCq MYXJcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIFexNlAzWiCvdYThcpQh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IIDoc5NxcG9vQVzLJIxmfmWuIIfpeIghUUN3MDDv[kAyNjF2ODFOwG0> MVuyOFgyQTFzNh?=
NIH-3T3 MnqxT4lv[XOnIFHzd4F6 NXGycFVFOSCq NWnWNnVXUW6qaXLpeIlwdiCxZjDoeY1idiCHTVy0MYZ2e2WmIFHMT{AyOTVzVHnud{BufXSjboSg[ZhxemW|c3XkJIF{e2W|c3XkJIF{KHCqb4PwbI8uSUyNIHzleoVtKHerdHigTWM2OCCxZjCzMlA{QSEQvF2= MUmyOFgyQTFzNh?=
KARPAS299 NUTyfFdEU2mwYYPlJGF{e2G7 MkfxPVAhdWmw NFz0TJhFVVOR NYn6bHFCUW6qaXLpeIlwdiCxZjDOVG0u\nW|ZXSgRWxMKHCqb4PwbI9zgWyjdHnvckBmgHC{ZYPz[YQhf2m2aDDJR|UxKG:oIECuNVEh|ryP MmfVNlQ6ODB5NUC=
MKN 45 NUjLTnhsU2mwYYPlJGF{e2G7 M1jhclEhcA>? M4T2TWROW09? MlfiTY5pcWKrdHnvckBw\iClLV3leEBxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEKg{txO Mk[2NlQ6ODB5NUC=
A549 NYfWOGU2S3m2b4TvfIlkKEG|c3H5 MnK2OFghcA>? M1jL[mROW09? MkSyTWM2OCCxZjC0MlA5PCEQvF2= NXj1WGdNOjR7MEC4N|A>
NCI-H1975 MWTDfZRwfG:6aXOgRZN{[Xl? NXK0boFYPDhiaB?= NWPWfVhYTE2VTx?= MYrJR|UxKG:oIEeuOVUyKM7:TR?= MYqyOFkxODh|MB?=
NCI-H1993 M1;JcmN6fG:2b4jpZ{BCe3OjeR?= Ml:5OFghcA>? MXrEUXNQ MUnJR|UxKG:oIECuNFYyKM7:TR?= NYjhXoEyOjR7MEC4N|A>
NCI-H1993 MXXBdI91d3OrczDBd5NigQ>? NEH0PIwyKM7:TR?= MXSyOEBp NV3nd2UxTE2VTx?= MUPkc4V{KG6xdDDpcoR2[2ViYYDvdJRwe2m| MYeyOFkxODh|MB?=
NIH-3T3 NG\jVZJEgXSxdH;4bYMhSXO|YYm= MVy0PEBp NEDGUpdFVVOR NXHPN5lvUUN3MDDv[kAxNjN4NDFOwG0> MYqyOFkxODh|MB?=
EBC1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFG4eXA4OiCq NYLDN4ZZTE2VTx?= NH32dVBKSzVyIH;mJFAvODB4OTFOwG0> MluzNlQ6ODB6M{G=
KARPAS299 NFLGbmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUm5O49uPzJiaB?= MlruSG1UVw>? M2PFb2lEPTBib3[gNE4zKM7:TR?= M1OxV|I1QTByOEOx
NB1 NHTjNmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jweWlEPTB;OUGuPVghdk1? NWDCdoJxW0GQR1XS
NCI-SNU-5 MkjOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTFyNT63OUBvVQ>? M1T6e3NCVkeHUh?=
SR NHfueG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnKyTWM2OD1zMk[uN|Ehdk1? NYXoVJBXW0GQR1XS
SF539 NXnpT|B5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXmPXNKSzVyPUKwOE4zPCCwTR?= NGHxXJlUSU6JRWK=
SU-DHL-1 M{[xXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTN|Nj64NkBvVQ>? NV3G[GxWW0GQR1XS
SCC-3 MnWyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXyfld2UUN3ME2zOVYvPzZibl2= MVLTRW5ITVJ?
DEL MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PDNmlEPTB;M{[5Mlkhdk1? M1zSWXNCVkeHUh?=
CTV-1 MmHoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2m4bWlEPTB;NUm2MlQ5KG6P MojJV2FPT0WU
EM-2 NWH6[HJuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nSdmlEPTB;NkCxMlM1KG6P NWPRemcxW0GQR1XS
MHH-CALL-2 NXHES3drT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTZ6Mj61O{BvVQ>? MYLTRW5ITVJ?
KM12 MkDuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnO0TWM2OD15ME[uPUBvVQ>? M33PU3NCVkeHUh?=
KINGS-1 M1:yd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\QRWlEPTB;N{S5Mlc2KG6P NImwTWJUSU6JRWK=
MEG-01 NWjXe5ZIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrnTWM2OD16NUeuOlYhdk1? NYrJWWxvW0GQR1XS
BV-173 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3e3ZWlEPTB;MT6wOVk6PyEQvF2= MXzTRW5ITVJ?
LAMA-84 M4KzeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jwfWlEPTB;MT6zPFI5OiEQvF2= M4HXcnNCVkeHUh?=
KARPAS-299 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXDcHJKSzVyPUGuOFA5PjFizszN MXjTRW5ITVJ?
K-562 MnTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjEOGV2UUN3ME2xMlczOjZ7IN88US=> NHvGbpZUSU6JRWK=
SK-LMS-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILkRZdKSzVyPUGuO|Y5PjdizszN M{j4[HNCVkeHUh?=
MOLT-16 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIezOIRKSzVyPUGuPVU2PzVizszN MUnTRW5ITVJ?
CMK M3v1fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\l[2lEPTB;MT65OlE2QSEQvF2= NFSxcI9USU6JRWK=
ST486 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnP1TWM2OD1{LkSzNFc{KM7:TR?= MWHTRW5ITVJ?
CI-1 NWrBS29OT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{K0WWlEPTB;Mj60PVY2QSEQvF2= NWWybHhSW0GQR1XS
KP-N-RT-BM-1 M{POT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnkTWM2OD1{LkewNVIzKM7:TR?= NFS2VZZUSU6JRWK=
ALL-PO M4POUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvWTWM2OD1|LkG4NlA4KM7:TR?= MoDNV2FPT0WU
KS-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlq3TWM2OD1|LkKxNlI2KM7:TR?= M1;sU3NCVkeHUh?=
Becker MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rqNGlEPTB;ND6yN|k{KM7:TR?= Mn72V2FPT0WU
GDM-1 MlqyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTRwMkS2NVch|ryP NHv0OnNUSU6JRWK=
BC-1 MnH3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjteGxjUUN3ME20MlQ6Ojd5IN88US=> M{flN3NCVkeHUh?=
NB14 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlK0TWM2OD12LkizOVI1KM7:TR?= MUTTRW5ITVJ?
NOS-1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1j3WmlEPTB;NT6zN|g4PCEQvF2= MkXTV2FPT0WU
MZ1-PC M2LsbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDVWJUxUUN3ME21MlgzOTVzIN88US=> NWXOdJhiW0GQR1XS
A498 NUfHXYpuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLITWM2OD14LkC4OFc{KM7:TR?= NUDxO2p{W0GQR1XS
EW-16 NXj0XmFbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTZwM{e3O|Mh|ryP M4jzOXNCVkeHUh?=
NALM-6 MkfiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTZwNkizPFch|ryP MorWV2FPT0WU
EB-3 NGTTdnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXntSFJxUUN3ME23MlA4OjN|IN88US=> NE\kXHVUSU6JRWK=
697 NVPYb2p6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\JTWM2OD17LkK0N|I6KM7:TR?= M4PRfXNCVkeHUh?=
Ramos-2G6-4C10 Ml\3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrNSJVDUUN3ME25MlU6QDR{IN88US=> M{fMPHNCVkeHUh?=
KNS-81-FD NYD6dnZUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NISxe|dKSzVyPUmuOlk3PTNizszN NW[4cmRyW0GQR1XS
HUTU-80 Ml7tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13CZWlEPTB;OT63OFY1OiEQvF2= NE\3bJBUSU6JRWK=
LS-411N MnT1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HBXmlEPTB;MUCuNFU3PyEQvF2= NIrDcWFUSU6JRWK=
RPMI-8402 Mnn4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnxcYFKSzVyPUGwMlEyPiEQvF2= NFTJ[W9USU6JRWK=
KU812 NILuU41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HRZmlEPTB;MUCuNlk6OSEQvF2= MX7TRW5ITVJ?
EW-1 NHy1d41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTFyLkS0NlUh|ryP MXnTRW5ITVJ?
HC-1 NXHjO2lFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LwUGlEPTB;MUCuOFg1PCEQvF2= NUTPSY5JW0GQR1XS
NB69 M3vJdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HDd2lEPTB;MUCuOVA1OyEQvF2= MknYV2FPT0WU
MFH-ino Mmj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTFyLkizNFMh|ryP MWTTRW5ITVJ?
CCRF-CEM MkXhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDUOIc5UUN3ME2xNU42QTdizszN MWTTRW5ITVJ?
SK-N-DZ MlLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnsTWM2OD1zMj6wOFM3KM7:TR?= NFPRTmZUSU6JRWK=
NCI-H720 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DGU2lEPTB;MUKuNVcxPSEQvF2= MorWV2FPT0WU
HCC1187 M1T1SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPrZ2hxUUN3ME2xNk4zODRzIN88US=> NVrk[3pHW0GQR1XS
IST-SL2 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vxN2lEPTB;MUKuOFg4OiEQvF2= MVTTRW5ITVJ?
KE-37 NFrTOJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTF{Lke5OlYh|ryP NVHhZWJVW0GQR1XS
HCC1599 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4H1SmlEPTB;MUKuPVA3QSEQvF2= NVuy[XQxW0GQR1XS
A4-Fuk M4T2OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofLTWM2OD1zMj65OVg3KM7:TR?= M3P1UnNCVkeHUh?=
NKM-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDnTWM2OD1zMz6yPVI2KM7:TR?= MlHEV2FPT0WU
BE-13 M2XlcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHL3WGNKSzVyPUGzMlc6QDlizszN M3SyZ3NCVkeHUh?=
MV-4-11 NX\oRVhST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1OxZ2lEPTB;MUSuNFMzPCEQvF2= MorDV2FPT0WU
OPM-2 NXP5THFnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2nCcGlEPTB;MUSuOFA5PSEQvF2= Moq2V2FPT0WU
KARPAS-422 MonoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\J[mlEPTB;MUSuOVEzPiEQvF2= NFrBSmVUSU6JRWK=
RPMI-8226 M{m5VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTF2Lki5NVUh|ryP MVrTRW5ITVJ?
KARPAS-45 M4nnZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTF3Lke3NVYh|ryP M1rYZXNCVkeHUh?=
SK-PN-DW NGnUeHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfNTWM2OD1zNT64OlMyKM7:TR?= NXzlXVNZW0GQR1XS
LC-2 NHXzWopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\NXWlEPTB;MU[uNVUxPiEQvF2= M2K5U3NCVkeHUh?=
NCI-H1648 NGjSWGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHHTWM2OD1zNj6yOVQh|ryP MUDTRW5ITVJ?
RL95-2 NELEOmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPmfI57UUN3ME2xOk4{QTd6IN88US=> NF75TZBUSU6JRWK=
KNS-42 NUiycnJqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvBOFlKSzVyPUG2MlczPzRizszN NHLJXHFUSU6JRWK=
RPMI-6666 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{i3WGlEPTB;MU[uPVIyOSEQvF2= MkjNV2FPT0WU
SIG-M5 M3Kzcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjZRndKSzVyPUG3MlE6ODNizszN MXfTRW5ITVJ?
VA-ES-BJ NFXmW29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrUTWM2OD1zNz63OFUyKM7:TR?= MmPRV2FPT0WU
MONO-MAC-6 MoGxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTF5LkmzNVIh|ryP MmXuV2FPT0WU
LAN-6 M2HOb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTF6Lke1OVch|ryP MkHwV2FPT0WU
A388 M1vXUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3nVVRKSzVyPUG5MlMxPTlizszN NVTM[pZ2W0GQR1XS
SK-NEP-1 NXnafFQ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\YR2lEPTB;MkCuNlE{OiEQvF2= NFvQS4dUSU6JRWK=
TE-10 NFfteIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rETWlEPTB;MkCuOVIzOSEQvF2= NYjWU4l2W0GQR1XS
HL-60 MnfpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrWRmtHUUN3ME2yNE46ODl7IN88US=> M3jmWHNCVkeHUh?=
MC116 Mn70S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HCT2lEPTB;MkGuO|IzOSEQvF2= M1TGSXNCVkeHUh?=
SW962 NYezbFdTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTJzLke5NVUh|ryP MYjTRW5ITVJ?
NOMO-1 NHvsb3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDCT4xYUUN3ME2yNk43PTZ2IN88US=> MVXTRW5ITVJ?
CTB-1 MkXVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTJ{Lki2O|Eh|ryP MWjTRW5ITVJ?
MRK-nu-1 NH3HbmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2nwR2lEPTB;MkKuPVA4PCEQvF2= NHjPNotUSU6JRWK=
GR-ST MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkC0TWM2OD1{Mz63OkDPxE1? NVn2N2RvW0GQR1XS
HH NInBd4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPGN4NyUUN3ME2yOE4xODNizszN M2DI[nNCVkeHUh?=
NCI-H1963 MofrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXuTWM2OD1{ND6wO|gzKM7:TR?= Mnq4V2FPT0WU
QIMR-WIL NUO4[2FxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jBWmlEPTB;MkSuPFc4OiEQvF2= NF61[YxUSU6JRWK=
CGTH-W-1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV[wdot1UUN3ME2yOU4xPzJ|IN88US=> NX[1PYtTW0GQR1XS
LP-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXCTWM2OD1{NT62OVUyKM7:TR?= M3TKZnNCVkeHUh?=
NCI-H748 NUSydldET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTJ4LkWxN|ch|ryP NGnxfZBUSU6JRWK=
PF-382 Mlm2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPvdZhKSzVyPUK3MlIzOjNizszN NYPDW5dwW0GQR1XS
ATN-1 M4LGUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG\B[IRKSzVyPUK3MlM4OzJizszN MWTTRW5ITVJ?
L-540 NIfRdGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvFTXJKSzVyPUK3MlY1PTlizszN NGHYboNUSU6JRWK=
LXF-289 MkC1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoGyTWM2OD1{Nz63OVE6KM7:TR?= MV\TRW5ITVJ?
LS-513 NEjiXVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTJ6LkG4NFch|ryP NFjke2FUSU6JRWK=
NCI-H1581 MlzOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfEfGw4UUN3ME2zNE4{QTd4IN88US=> NFLoXJdUSU6JRWK=
ES6 NGfZNWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTiSYJKSzVyPUOwMlY5QTlizszN NGH6N29USU6JRWK=
SW982 NFjZXFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7JTWM2OD1|MD64OVY3KM7:TR?= MWPTRW5ITVJ?
DOHH-2 M2riW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TEbWlEPTB;M{GuOVg6OyEQvF2= NFq0d4xUSU6JRWK=
DB NHu3XHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{X6fmlEPTB;M{OuPVQ{OSEQvF2= MYPTRW5ITVJ?
MPP-89 NWL0WZhRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTN2LkG3OVYh|ryP MnriV2FPT0WU
LB831-BLC M3zt[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTN2LkWxPFQh|ryP NUK0VFU5W0GQR1XS
NB5 NIe0eHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnMbYFKSzVyPUO0Mlg2OzVizszN NFn6eJRUSU6JRWK=
GB-1 NIfHPVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHqTWM2OD1|NT6wOFY6KM7:TR?= NVHGXINGW0GQR1XS
TE-15 NIjjdHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTN3LkKyN|gh|ryP Mor3V2FPT0WU
LC4-1 NVnMTYJxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTN3LkO4OFch|ryP NEfvc3RUSU6JRWK=
NCI-H747 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjFTWM2OD1|Nj6xN|Y6KM7:TR?= M{WwOHNCVkeHUh?=
NTERA-S-cl-D1 M2rs[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37NemlEPTB;M{iuO|M1PyEQvF2= NGj4dFZUSU6JRWK=
SK-MM-2 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHOTY5HUUN3ME20NE4yOTR4IN88US=> MlfkV2FPT0WU
TGW NVmxXWY{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH22b3ZKSzVyPUSxMlA2PjNizszN M{\OVXNCVkeHUh?=
ONS-76 NHjvc5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTR{LkS4PFMh|ryP MVjTRW5ITVJ?
CPC-N MoftS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4P6VWlEPTB;NEKuPVk4OSEQvF2= NV7DPZRjW0GQR1XS
ES4 NXq4fHRYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLtTWM2OD12ND60NVU{KM7:TR?= NXnqXXRJW0GQR1XS
Daudi NFf4SFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzk[ZZoUUN3ME20OU4xQDJ5IN88US=> MYHTRW5ITVJ?
MOLT-4 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIexOZBKSzVyPUS1MlA5PTNizszN NFLQfYhUSU6JRWK=
HT-144 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3nfVBKSzVyPUS2MlczPiEQvF2= NV\vdFB7W0GQR1XS
SW872 M2rxUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33j[2lEPTB;NEiuNVk{OyEQvF2= MXTTRW5ITVJ?
D-283MED MnnkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzxTWM2OD12OD6zOVQzKM7:TR?= MUDTRW5ITVJ?
NCI-H2126 NHywVo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3L[2M2UUN3ME20PE45PDd4IN88US=> NFK2[YdUSU6JRWK=
NCI-SNU-16 NEXrcVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fxT2lEPTB;NEmuNlE1OyEQvF2= MVLTRW5ITVJ?
CESS MofCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIe1ToZKSzVyPUS5MlUxQDhizszN Mm\YV2FPT0WU
A101D NXrpS|ZqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTR7Lkm3N|Yh|ryP M2THS3NCVkeHUh?=

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In vivo試験 In the GTL-16 model, PF-2341066 reveals the ability to cause marked regression of large established tumors (>600 mm3) in both the 50 mg/kg/day and 75 mg/kg/day treatment cohorts, with a 60% decrease in mean tumor volume over the 43-day administration schedule. In an another study, PF-2341066 displays the ability to completely inhibits GTL-16 tumor growth for >3 months, with only 1 of 12 mice exhibiting a significant increase in tumor growth over the 3-month treatment schedule at 50 mg/kg/day. In the NCI-H441 NSCLC model, a 43% decrease in mean tumor volume is observed at 50 mg/kg/day during the 38-day PF-2341066 administration cycle. In the Caki-1 RCC model, a 53% decrease in mean tumor volume is observed to be associated with decreased volume of each tumor by at least 30% at 50 mg/kg/day during the 33-day PF-2341066 administration cycle. PF-2341066 also reveals near-complete prevention of the growth of established tumors at 50 mg/kg/day in the U87MG glioblastoma or PC-3 prostate carcinoma xenograft models, with 97% or 84% inhibition on the final study day, respectively. In contrast, PF-2341066 p.o. given at 50 mg/kg/day does not significantly inhibit tumor growth in the MDA-MB-231 breast carcinoma model, or the DLD-1 colon carcinoma model. A significant dose-dependent reduction of CD31–positive endothelial cells is observed at 12.5 mg/kg/day, 25 mg/kg/day, and 50 mg/kg/day in GTL-16 tumors, indicating that inhibition of MVD shows a dose-dependent correlation to antitumor efficacy. PF-2341066 displays a significant dose-dependent reduction of human VEGFA and IL-8 plasma levels in both the GTL-16 and U87MG models. Marked inhibition of phosphorylated c-Met, Akt, Erk, PLCλ1, and STAT5 levels is observed in GTL-16 tumors following p.o. administration of PF-2341066.[1] P.o. administration of PF-2341066 to severe combined immunodeficient-Beige mice bearing Karpas299 ALCL tumor xenografts leads to dose-dependent antitumor efficacy with complete regression of all tumors at the 100 mg/kg/d dose within 15 days of initial compound administration. In addition, inhibition of key NPM-ALK signaling mediators, including phospholipase C-gamma, signal transducers and activators of transcription 3, extracellular signal-regulated kinases, and Akt by PF-2341066 are observed at concentrations or dose levels, which correlated with inhibition of NPM-ALK phosphorylation and function.[2] PF-2341066 prevents osteosarcoma behavior associated with primary tumor growth (eg, proliferation and survival) as well as metastasis (eg, invasion and clonogenicity). In nude mice treated with PF-2341066 via oral gavage, the growth and associated osteolysis and extracortical bone matrix formation of osteosarcoma xenografts are prevented by PF-2341066.[3] Treatment of c-MET-amplified GTL-16 xenografts with 50 mg/kg PF-2341066 elicits tumor regression that is associated with a slow reduction in 18F-FDG uptake and decreases expression of the glucose transporter 1, GLUT-1.[4]
臨床試験 PF-2341066 is currently in a Phase III clinical trial in the treatment of non squamous lung cancer.
特集

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

Cellular kinase phosphorylation ELISA assays Cells are seeded in 96-well plates in media supplemented with 10% fetal bovine serum (FBS) and transferred to serum-free media [with 0.04% bovine serum albumin (BSA)] after 24 h. In experiments investigating ligand-dependent RTK phosphorylation, corresponding growth factors are added for up to 20 min. After incubation of cells with PF-2341066 for 1 h and/or appropriate ligands for the designated times, cells are washed once with HBSS supplemented with 1 mM Na3VO4, and protein lysates are generated from cells. Subsequently, phosphorylation of selected protein kinases is assessed by a sandwich ELISA method using specific capture antibodies used to coat 96-well plates and a detection antibody specific for phosphorylated tyrosine residues. Antibody-coated plates are (a) incubated in the presence of protein lysates at 4°C overnight; (b) washed seven times in 1% Tween 20 in PBS; (c) incubated in a horseradish peroxidase–conjugated anti–total-phosphotyrosine (PY-20) antibody (1:500) for 30 min; (d) washed seven times again; (e) incubated in 3,3′,5,5′-tetramethyl benzidine peroxidase substrate to initiate a colorimetric reaction that is stopped by adding 0.09 N H2SO4; and (f) measured for absorbance in 450 nm using a spectrophotometer.

細胞アッセイ: [1]

細胞株 GTL-16 gastric carcinoma cells and T47D breast carcinoma cells
濃度 0-256 nM
反応時間 1 hour
実験の流れ Cells including GTL-16 gastric carcinoma cells and T47D breast carcinoma cells are seeded in 96-well plates in media supplemented with 10% fetal bovine serum (FBS) and transferred to serum-free media [with 0.04% bovine serum albumin (BSA)] after 24 hours. In experiments investigating ligand-dependent RTK phosphorylation, corresponding growth factors are added for up to 20 minutes. After incubation of cells with PF-2341066 for 1 hour and/or appropriate ligands for the designated times, cells are washed once with HBSS supplemented with 1 mM Na3VO4, and protein lysates are generated from cells. Subsequently, phosphorylation of selected protein kinases is assessed by a sandwich ELISA method using specific capture antibodies used to coat 96-well plates and a detection antibody specific for phosphorylated tyrosine residues. Antibody-coated plates are (a) incubated in the presence of protein lysates at 4 °C overnight; (b) washed seven times in 1% Tween 20 in PBS; (c) incubated in a horseradish peroxidase–conjugated anti–total-phosphotyrosine (PY-20) antibody (1:500) for 30 min; (d) washed seven times again; (e) incubated in 3,3,5,5-tetramethyl benzidine peroxidase substrate to initiate a colorimetric reaction that is stopped by adding 0.09 N H2SO4; and (f) measured for absorbance in 450 nm using a spectrophotometer.

動物実験: [1]

動物モデル Female or male nu/nu mice bearing NCI-H441,or DLD-1, or MDA-MB-231
製剤
投薬量 12.5 mg/kg/day, 25 mg/kg/day, and 50 mg/kg/day
投与方法 Administered via p.o.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Crizotinib (PF-02341066) SDF
分子量 450.34
化学式

C21H22Cl2FN5O

CAS No. 877399-52-5
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 9 mg/mL (19.98 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo 5% DMSO/30% PEG 300/dd H2O 5mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 3-((R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine

カスタマーフィードバック (8)


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Rating
Source Nat Med , 2011, 17, 1116-1120. Crizotinib (PF-02341066) purchased from Selleck
Method Western blot
Cell Lines RCT-E565 transplanted tumors
Concentrations 25 mg/kg/d, 50 mg/kg/d
Incubation Time 0-21 d
Results We then treated mice bearing RCT-E565 tumor transplants with PF02341066, a c-Met inhibitor currently in clinical development. PF02341066 abrogated both p-Akt and p-S6RP signals as well as tumor growth.

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Source Cancer Cell , 2011, 19, 679–690. Crizotinib (PF-02341066) purchased from Selleck
Method Cell Growth Inhibition Assay
Cell Lines Ba/F3 cells
Concentrations
Incubation Time 48 h
Results The sensitivities of L1196M-driven Ba/F3 cell clones to PF-02341066 were lower, closely resembling that of the Ba/F3 parental cells. The therapeutic indexes of CH5424802 and PF-02341066, the IC50 ratio of EML4-ALK L1196M-driven cell clones to the parental cells, were 7- to 12-fold and 1- to 2-fold.

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Source Cancer Cell , 2011, 19, 679–690. Crizotinib (PF-02341066) purchased from Selleck
Method Immunoblot analysis, Tumor growth inhibition Assay
Cell Lines xenograft models
Concentrations 100 mg/kg
Incubation Time 8 days
Results We showed that administration of CH5424802 led to significant tumor regression against both native EML4-ALK- and L1196M-driven tumors. On the other hand, PF-02341066 (100 mg/kg) resulted in no significant tumor growth inhibition against L1196M-driven tumors. Furthermore, we confirmed that phospho-STAT3, one of the downstream targets of ALK, was abolished in both tumors that were treated with CH5424802.

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Source J Biomol Screen , 2011, 16, 141-154. Crizotinib (PF-02341066) purchased from Selleck
Method VimPro-Fluc-MDA-MB-231 spheroid viability, Western blot
Cell Lines MDA-MB-231 spheroids
Concentrations
Incubation Time
Results When Vimpro-Fluc downregulation reaches ≥70%, then downregulation of vimentin protein expression is more pronounced. of the modulators tested—U0126, dasatinib,axitinib, and pF2341066-all downregulated Vimpro-Fluc activity by ≥70%, which correlated with a significant down-reglation of vimentin protein expression. Finally, dose-response curves were generated with both U0126 (iC50 = 2.5 µM) and axitinib (iC50 = 0.25 µM), demonstrating that these small molecules modulate Vimpro-Fluc activity in a dose-dependent manner, indicating that their respective target(s) and signaling pathways play a significant role in maintaining vimentin expression and possibly mesenchymal homeostasis (Fig. B)

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Rating
Source J Biomol Screen , 2011, 16, 141-154. Crizotinib (PF-02341066) purchased from Selleck
Method Secondary assay
Cell Lines MDA-MB-231 spheroids
Concentrations 10 µM
Incubation Time
Results U0126, pF2341066, axitinib, and pKC412 caused significant inhibition of the invasive potential of Mda-Mb-231 spheroids. Conversely, dasatinib, a potent inhibitor of vimentin gene expression, did not significantly alter the invasive potential of Mda-Mb-231 spheroids.

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Rating
Source Int J Proteomics , 2011, 2011, 215496. Crizotinib (PF-02341066) purchased from Selleck
Method CEER assay
Cell Lines H1993 cell line
Concentrations 0-10 μM
Incubation Time 4 h
Results In the c-MET amplified cell line H1993, activation of this pathway was blocked by the treatment with PF-2341066, a c-MET kinase inhibitor.

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Rating
Source Int J Proteomics, 2011, 2011, Article ID 215496. Crizotinib (PF-02341066) purchased from Selleck
Method Nikon inverted-phase microscope
Cell Lines lung tumor cell lines
Concentrations 0.1/1 µM
Incubation Time two weeks
Results Large colony formation of H1993 cells, whose proliferation in tissue culture was potently blocked by treatment with the c-MET kinase inhibitor PF-2341066, was also inhibited by treatment with the same inhibitor.

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Rating
Source Dr. Zhang of Tianjin Medical University. Crizotinib (PF-02341066) purchased from Selleck
Method Western blot
Cell Lines MDA-MB-231 cell line
Concentrations 0-100 nM
Incubation Time
Results

文献中の引用 (63)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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