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 NU\VTY97S3m2b4TvfIlkKEG|c3H5 NWjZ[nBxPDhiaB?= NHHtOmpFVVOR MmOxR5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgRmFHOyClZXzsd{BmgHC{ZYPzbY5oKEGOSzDGNVE4PExibYX0ZY51KGOxZYjwdoV{e2mwZzDFUWw1KHerdHigTWM2OCCxZjCwMlYzKM7:TR?= MmnuNlE2PzJ3OEm=
BAF3 NFHxPJZEgXSxdH;4bYMhSXO|YYm= MV60PEBp NHLTSG5FVVOR NHXBRYdEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBDSUZ|IHPlcIx{KGW6cILld5NqdmdiQVzLJGwyOTl4TTDteZRidnRiY3;lfJBz\XO|aX7nJGVOVDRid3n0bEBKSzVyIH;mJFIvOiEQvF2= NGfVZYQzOTV5MkW4PS=>
BAF3 MW\DfZRwfG:6aXOgRZN{[Xl? MWC0PEBp NFq2XpdFVVOR MYjDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDCRWY{KGOnbHzzJIV5eHKnc4PpcochTU2OND3BUGshf2m2aDDJR|UxKG:oIECuNlgh|ryP MV6yNVU4OjV6OR?=
Kelly MmTsR5l1d3SxeHnjJGF{e2G7 M1TsWGROW09? Mn7mR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gT4VtdHliY3XscJMh\XiycnXzd4lv\yCDTFugSlEyPzSOIH31eIFvfCC5aYToJGlEPTBib3[gNE41OiEQvF2= NE\jXWIzOTV5MkW4PS=>
SH-SY5Y NHGzWYxEgXSxdH;4bYMhSXO|YYm= MkXrSG1UVw>? MUDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTTE1UYTW\IHPlcIx{KGW6cILld5NqdmdiQVzLJGYyOTd2TDDteZRidnRid3n0bEBKSzVyIH;mJFAvPTNizszN M3m5RVIyPTd{NUi5
SMS-KCN NWnR[3pHS3m2b4TvfIlkKEG|c3H5 NVnkUotSTE2VTx?= MWnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTUXMuU0OQIHPlcIx{KGW6cILld5NqdmdiQVzLJHIyOjd3UTDteZRidnRid3n0bEBKSzVyIH;mJFAvQTFizszN NEf6R3ozOTV5MkW4PS=>
BAF3 M1nNN2N6fG:2b4jpZ{BCe3OjeR?= M4nieFQ5KGh? NUDiW4NwTE2VTx?= NUDRV2M1S3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhSkGIMzDj[YxteyCneIDy[ZN{cW6pIGTlcE1CVEtid3n0bEBKSzVyIH;mJFAvOTlizszN NGDBOngzOTV5MkW4PS=>
3T3 NFnhPWRHfW6ldHnvckBCe3OjeR?= MkDVNUBp NWHuNZRSTE2VTx?= NH;ZfJhKdmirYnn0bY9vKG:oIGLPUkBie3Onc4Pl[EBieyCpcn;3eIgh\mGldH;yMYlv\HWlZXSgZZV1d3Cqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMD6wPEDPxE1? M3q3bFIyQDF{NEG0
3T3-E NIr6bFVHfW6ldHnvckBCe3OjeR?= MXSxJIg> M4XDOGROW09? MXXJcohq[mm2aX;uJI9nKFSLRUKgZZN{\XO|ZXSg[5Jwf3SqIH\hZ5Rwei2rbnT1Z4VlKGG3dH;wbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFAvPDR6IN88US=> MnXXNlE5OTJ2MUS=
A549 M4K4cGtqdmG|ZTDBd5NigQ>? MmXuNUBp NWf4bI1WTE2VTx?= NVXXTXJtUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDjMW1GXCCtaX7hd4Uh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhUEeILXnu[JVk\WRiYYX0c5Bpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5yMEig{txO NGXKcG0zOThzMkSxOC=>
BAF3-BCL NX;EdJpyTnWwY4Tpc44hSXO|YYm= M2PZRVEhcA>? M{HMVmROW09? M{jXR2lvcGmkaYTpc44hd2ZiQVLMJIF{e2W|c3XkJIF{KGe{b4f0bEBn[WO2b4KtbY5lfWOnZDDheZRweGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iBzLkG1PUDPxE1? Mmj4NlE5OTJ2MUS=
HEK293 NHjaVm1HfW6ldHnvckBCe3OjeR?= M2H6XFEhcA>? MXTEUXNQ M2rw[WlvcGmkaYTpc44hd2ZiQWjMJIF{e2W|c3XkJIF{KGe{b4f0bEBn[WO2b4KtbY5lfWOnZDDheZRweGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkK5OEDPxE1? NEX1Z|IzOThzMkSxOC=>
HEK293 NYnzPVdTTnWwY4Tpc44hSXO|YYm= NF:0ZY8yKGh? MY\EUXNQ NUHx[VFtUW6qaXLpeIlwdiCxZjDJVkBie3Onc4Pl[EBieyCpcn;3eIgh\mGldH;yMYlv\HWlZXSgZZV1d3Cqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMj64PFch|ryP MXeyNVgyOjRzNB?=
Jurkat MYrGeY5kfGmxbjDBd5NigQ>? M{nmSlEhcA>? NF;SW3dFVVOR MnTHTY5pcWKrdHnvckBw\iCOQ1ugZZN{\XO|ZXSgZZMh\3Kxd4ToJIZi[3Sxcj3pcoR2[2WmIHH1eI9xcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDJwN{SxJO69VQ>? MW[yNVgyOjRzNB?=
KARPAS299 M1KxZWtqdmG|ZTDBd5NigQ>? NW\IdodMOSCq M2P6WWROW09? NEXOVGdKdmirYnn0bY9vKG:oIFHMT{Bie3Onc4Pl[EBieyCpcn;3eIgh\mGldH;yMYlv\HWlZXSgZZV1d3Cqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMD6wNkDPxE1? MkLRNlE5OTJ2MUS=
PAE M{PXSmZ2dmO2aX;uJGF{e2G7 MVSxJIg> NFXYXmdFVVOR NUOzVo44UW6qaXLpeIlwdiCxZjDUVmtDKGG|c3Xzd4VlKGG|IHfyc5d1cCCoYXP0c5IucW6mdXPl[EBifXSxcHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCwMlM6QSEQvF2= M33CR|IyQDF{NEG0
BAF3 MnftSpVv[3Srb36gRZN{[Xl? NXvscmxtOi1|IHS= M3fUfGROW09? MUHJcohq[mm2aX;uJI9nKFSHTD3meZNm\CCrboP1cIlvKHKnY3XweI9zKGW6cILld5Nm\CC5aYToJGlEPTBib3[gNU43PDNizszN MnzENlM4PDJ{NUK=
KARPAS299 M1zyWmN6fG:2b4jpZ{BCe3OjeR?= M2LrZVIuOyCm M2jNcWROW09? NFPOTodKSzVyPUCuNFY1OiEQvF2= MneyNlM4PDJ{NUK=
EBC1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7MUoc4OiCq NETCNIxFVVOR MkDlTWM2OD1yLkCyN{DPxE1? M4fnRlI{QTl|M{K4
HCT116 NVy5U5BkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDyO|IhcA>? M1XXeWROW09? MnvvTWM2OD1zND64NkDPxE1? MlP2NlM6QTN|Mki=
MCF7 NW\KfYtHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXiO|IhcA>? NIXFZ4xFVVOR NV:4RZVMUUN3ME25MlU5KM7:TR?= M3O5NFI{QTl|M{K4
MDA-MB-231 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEm1RXQ4OiCq NEH0cXRFVVOR NFHUXo1KSzVyPUGwMlgh|ryP M1KzclI{QTl|M{K4
MKN45 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjUTnNDPzJiaB?= M3X6RWROW09? NITSdGFKSzVyPUCuNFE{KM7:TR?= NWHpcoFtOjN7OUOzNlg>
NCI-H441 NHOyO2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nDdVczKGh? NVXxdIZMTE2VTx?= MWnJR|UxRTF5LkK1JO69VQ>? MV2yN|k6OzN{OB?=
NCI-H661 NXj4dZoyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIr0NWQ4OiCq NILJ[GJFVVOR M{TvdWlEPTB;MUGuOFch|ryP M1\XfVI{QTl|M{K4
SK-MEL-28 MlTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;GbpdXPzJiaB?= Mlm3SG1UVw>? NFu2NnBKSzVyPUGwMlk4KM7:TR?= MlexNlM6QTN|Mki=
SKOV3 NHmzUZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXXWmFZPzJiaB?= Mmq4SG1UVw>? MX;JR|UxRTF{Lki1JO69VQ>? MV2yN|k6OzN{OB?=
SNU5 M3XUSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXpO|IhcA>? NHr3TZhFVVOR MlP3TWM2OD1yLkCxOkDPxE1? MnW5NlM6QTN|Mki=
NCI-H2228 NUXPOXRrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUS3NkBp M1zVSGROW09? M2\FemlvcGmkaYTpc44hd2ZiQVzLMYZ2e2mxbjDkdol3\W5iY3XscEBxem:uaX\ldoF1cW:wIIfpeIghUUN3MDDv[kAxNjFzODFOwG0> MYSyOFQ{OjlyOR?=
NCI-H3122 NIntVldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnkclBsPzJiaB?= MnPtSG1UVw>? MWDJcohq[mm2aX;uJI9nKEGOSz3meZNqd25iZILpeoVvKGOnbHygdJJwdGmoZYLheIlwdiC5aYToJGlEPTBib3[gNE4yODhizszN M2[3O|I1PDN{OUC5
NCI-H3122 MoDNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlzuO|IhcA>? M2LKXGROW09? NULwbFF3UW6qaXLpeIlwdiCxZjDBUGsu\nW|aX;uJIRzcX[nbjDj[YxtKHC{b3zp[oVz[XSrb36gbY4hcHWvYX6gUmNKNUh|MUKyJINmdGy|IHjhdoJwemmwZzDBUGshTzF{NknBJI12fGGwdDD3bZRpKEmFNUCgc4YhOC54MkOg{txO M{jLcVI1PDN{OUC5
NCI-H3122 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDYT4pNPzJiaB?= NG\IVI9FVVOR NIq5RnZKdmirYnn0bY9vKG:oIFHMT{1nfXOrb36g[JJqfmWwIHPlcIwheHKxbHnm[ZJifGmxbjDpckBpfW2jbjDOR2kuUDNzMkKgZ4VtdHNiaHHyZo9zcW6pIFHMT{BNOTF7Nl2gcZV1[W62IIfpeIghUUN3MDDv[kAxNjh|ODFOwG0> M{jNV|I1PDN{OUC5
NIH-3T3 Mly4T4lv[XOnIFHzd4F6 MX[xJIg> MlLwSG1UVw>? NIPMfotKdmirYnn0bY9vKG:oIHj1cYFvKHerbHSgeJlx\SCHTVy0MYZ2e2WmIFHMT{BmgHC{ZYPz[YQh[XO|ZYPz[YQh[XNicHjvd5Bpd3K7bHH0[YQhSUyNIHzleoVtKHerdHigTWM2OCCxZjCwMlA5KM7:TR?= NWLnToZ2OjR2M{K5NFk>
NIH-3T3 M4DFOGtqdmG|ZTDBd5NigQ>? MYOxJIg> MVHEUXNQ M1LNcWlvcGmkaYTpc44hd2ZiaIXtZY4hTU2OND3meZNm\CCDTFugS|EzPjmDIH31eIFvfCCneIDy[ZN{\WRiYYPz[ZN{\WRiYYOgdIhwe3Cqbz3BUGshdGW4ZXyge4l1cCCLQ{WwJI9nKDBwNkC1JO69VQ>? NEXNeWIzPDR|MkmwPS=>
NIH-3T3 NEH5WG5McW6jc3WgRZN{[Xl? NVr3NoVoOSCq M{n3eGROW09? MnvZTY5pcWKrdHnvckBw\iCqdX3hckBGVUx2LX\1d4VlKEGOSzDTNVIxPllibYX0ZY51KGW6cILld5Nm\CCjc4Pld5Nm\CCjczDwbI9{eGixLVHMT{Bt\X[nbDD3bZRpKEmFNUCgc4YhOC54Mk[g{txO MWqyOFQ{OjlyOR?=
NIH-3T3 MlvlT4lv[XOnIFHzd4F6 NF\6SGgyKGh? NVzKNoRNTE2VTx?= MkPTTY5pcWKrdHnvckBw\iCqdX3hckBGVUx2LX\1d4VlKEGOSzDMNVE6Pk1ibYX0ZY51KGW6cILld5Nm\CCjc4Pld5Nm\CCjczDwbI9{eGixLVHMT{Bt\X[nbDD3bZRpKEmFNUCgc4YhOC56NEOg{txO M1HDflI1PDN{OUC5
NIH-3T3 NXKy[2U1U2mwYYPlJGF{e2G7 NXXjOYtYOSCq M1XrfmROW09? NVr6eGs3UW6qaXLpeIlwdiCxZjDoeY1idiCHTVy0MYZ2e2WmIFHMT{BNOTF3MmKgcZV1[W62IHX4dJJme3OnZDDhd5Nme3OnZDDhd{BxcG:|cHjvMWFNUyCuZY\lcEB4cXSqIFnDOVAhd2ZiMT6wNlYh|ryP NGjXeVYzPDR|MkmwPS=>
BAF3 NEHtfVBHfW6ldHnvckBCe3OjeR?= NHfSNo04OiCq NYrj[3ZzTE2VTx?= M1zlRmlvcGmkaYTpc44hd2ZiTmDNM2FNUyC2cnHud4Zm[3SnZDDhd5Nme3OnZDDhd{Bk\WyuIHfyc5d1cCCrbnjpZol1cW:wIIfpeIghUUN3MDDv[kAxNjB3MTFOwG0> MYCyOFQ3QDZ|Mh?=
BAF3 NYD4WnI6S3m2b4TvfIlkKEG|c3H5 NHexOVU4OiCq NEDz[XZFVVOR Mki5TWM2OD1yLkm4JO69VQ>? MojCNlQ1Pjh4M{K=
NIH-3T3 M{Py[2tqdmG|ZTDBd5NigQ>? NUX1cHU{OSCq MVTJcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIF[xNVc1VCCvdYThcpQh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IIDoc5NxcG9vQVzLJIxmfmWuIIfpeIghUUN3MDDv[kAxNjF4NTFOwG0> MmjGNlQ5OTlzMU[=
NIH-3T3 M2PrSWtqdmG|ZTDBd5NigQ>? Mli2NUBp NFrVOFBKdmirYnn0bY9vKG:oIHj1cYFvKEWPTESt[pV{\WRiQVzLJGMyOTV4WTDteZRidnRiZYjwdoV{e2WmIHHzd4V{e2WmIHHzJJBpd3OyaH:tRWxMKGyndnXsJJdqfGhiSVO1NEBw\iByLkS3PEDPxE1? M334XVI1QDF7MUG2
NIH-3T3 M{HFZmtqdmG|ZTDBd5NigQ>? M1jnd|EhcA>? MmLITY5pcWKrdHnvckBw\iCqdX3hckBGVUx2LX\1d4VlKEGOSzDHNVIxOlJibYX0ZY51KGW6cILld5Nm\CCjc4Pld5Nm\CCjczDwbI9{eGixLVHMT{Bt\X[nbDD3bZRpKEmFNUCgc4YhOS5zNEig{txO NUPUdXUzOjR6MUmxNVY>
NIH-3T3 Mlv5T4lv[XOnIFHzd4F6 NGfKVW4yKGh? M{HLdWlvcGmkaYTpc44hd2ZiaIXtZY4hTU2OND3meZNm\CCDTFugNVE2OVSrboOgcZV1[W62IHX4dJJme3OnZDDhd5Nme3OnZDDhd{BxcG:|cHjvMWFNUyCuZY\lcEB4cXSqIFnDOVAhd2ZiMz6wN|kh|ryP NVSzOnVHOjR6MUmxNVY>
KARPAS299 MnXxT4lv[XOnIFHzd4F6 NXX1VGpZQTBibXnu NXXjc5B2TE2VTx?= MVrJcohq[mm2aX;uJI9nKE6STT3meZNm\CCDTFugdIhwe3Cqb4L5cIF1cW:wIHX4dJJme3OnZDD3bZRpKEmFNUCgc4YhOC5zMTFOwG0> MmD6NlQ6ODB5NUC=
MKN 45 Mk\zT4lv[XOnIFHzd4F6 M3O5VlEhcA>? MnrRSG1UVw>? NVe0TY96UW6qaXLpeIlwdiCxZjDjMW1mfCCyaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIECuNFIh|ryP MWCyOFkxODd3MB?=
A549 M1O4T2N6fG:2b4jpZ{BCe3OjeR?= M2XtTlQ5KGh? M4q4bWROW09? M2K1fGlEPTBib3[gOE4xQDRizszN NHqyN3MzPDlyMEizNC=>
NCI-H1975 MWLDfZRwfG:6aXOgRZN{[Xl? NYn2d3hnPDhiaB?= NFvPWWhFVVOR NILKUYZKSzVyIH;mJFcvPTVzIN88US=> NXrDbHN3OjR7MEC4N|A>
NCI-H1993 MmrIR5l1d3SxeHnjJGF{e2G7 MnHLOFghcA>? NX3Vd5VRTE2VTx?= MmO2TWM2OCCxZjCwMlA3OSEQvF2= M3foXlI1QTByOEOw
NCI-H1993 NEXyWmJCeG:2b4Ppd{BCe3OjeR?= NXP1fo1QOSEQvF2= M13PbFI1KGh? M4jndGROW09? M3LWVIRw\XNibn;0JIlv\HWlZTDhdI9xfG:|aYO= NIDhfI4zPDlyMEizNC=>
NIH-3T3 MV7DfZRwfG:6aXOgRZN{[Xl? Ml7OOFghcA>? MlvnSG1UVw>? MXXJR|UxKG:oIECuN|Y1KM7:TR?= NVz0WYQyOjR7MEC4N|A>
EBC1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWG3NkBp MYLEUXNQ MV;JR|UxKG:oIECuNFA3QSEQvF2= Mle4NlQ6ODB6M{G=
KARPAS299 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHe3cpk4OiCq M3KwfWROW09? MoPITWM2OCCxZjCwMlIh|ryP M2rabFI1QTByOEOx
NB1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYi2UXM3UUN3ME25NU46QCCwTR?= MYLTRW5ITVJ?
NCI-SNU-5 M2W5fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3y2SWlEPTB;MUC1Mlc2KG6P NFjUV5BUSU6JRWK=
SR NWKyRVd4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfHSGlKSzVyPUGyOk4{OSCwTR?= MXPTRW5ITVJ?
SF539 NGTwVpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTJyND6yOEBvVQ>? NGLMVopUSU6JRWK=
SU-DHL-1 NFX6NXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELQU3VKSzVyPUOzOk45OiCwTR?= NFf3OnhUSU6JRWK=
SCC-3 Mki0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLIWppKSzVyPUO1Ok44PiCwTR?= MWDTRW5ITVJ?
DEL NHf3eYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTN4OT65JI5O MUXTRW5ITVJ?
CTV-1 M3H1T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTV7Nj60PEBvVQ>? MkjUV2FPT0WU
EM-2 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfrO3ZCUUN3ME22NFEvOzRibl2= NH;tVWRUSU6JRWK=
MHH-CALL-2 NYn6VZhRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTrTWM2OD14OEKuOVchdk1? M3fwWnNCVkeHUh?=
KM12 Ml34S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDyTWM2OD15ME[uPUBvVQ>? NGDaN2hUSU6JRWK=
KINGS-1 NUnJWmJMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXXTWM2OD15NEmuO|Uhdk1? M1PW[HNCVkeHUh?=
MEG-01 NFPlTGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DTR2lEPTB;OEW3MlY3KG6P NXSyZ3pRW0GQR1XS
BV-173 NEftOWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jKeGlEPTB;MT6wOVk6PyEQvF2= MWDTRW5ITVJ?
LAMA-84 NWXiW3Z[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknJTWM2OD1zLkO4NlgzKM7:TR?= M1nYOXNCVkeHUh?=
KARPAS-299 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXJSJJKSzVyPUGuOFA5PjFizszN NFOyfJZUSU6JRWK=
K-562 M{nhfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTFwN{KyOlkh|ryP NHr0[JBUSU6JRWK=
SK-LMS-1 NXjreXJGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXizbGVZUUN3ME2xMlc3QDZ5IN88US=> Mn[1V2FPT0WU
MOLT-16 M32xeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYi4fJo5UUN3ME2xMlk2PTd3IN88US=> NHfBWlRUSU6JRWK=
CMK NXH6eFZDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PRUmlEPTB;MT65OlE2QSEQvF2= MlfRV2FPT0WU
ST486 NUDITndZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPhTWM2OD1{LkSzNFc{KM7:TR?= NXLhPJdXW0GQR1XS
CI-1 NHnHd|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvlWIhuUUN3ME2yMlQ6PjV7IN88US=> MV;TRW5ITVJ?
KP-N-RT-BM-1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;kTWM2OD1{LkewNVIzKM7:TR?= NI\rUFBUSU6JRWK=
ALL-PO NF;6bphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7QdnRKSzVyPUOuNVgzODdizszN NWK3fYhLW0GQR1XS
KS-1 NXHFUHlIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzlclhKSzVyPUOuNlEzOjVizszN MVHTRW5ITVJ?
Becker MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrCS21KSzVyPUSuNlM6OyEQvF2= M{OzNXNCVkeHUh?=
GDM-1 NGfne2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTRwMkS2NVch|ryP M3TYZXNCVkeHUh?=
BC-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTRwNEmyO|ch|ryP NFvEW4ZUSU6JRWK=
NB14 NXfCW2w1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTRwOEO1NlQh|ryP MXnTRW5ITVJ?
NOS-1 M2\kfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXnTWM2OD13LkOzPFc1KM7:TR?= MX;TRW5ITVJ?
MZ1-PC NILWSm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Moe5TWM2OD13LkiyNVUyKM7:TR?= NIHiPI9USU6JRWK=
A498 M{ntZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfPTWM2OD14LkC4OFc{KM7:TR?= NYjJOHd{W0GQR1XS
EW-16 NEPybHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTZwM{e3O|Mh|ryP M{T1NXNCVkeHUh?=
NALM-6 M1G5c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3riNWlEPTB;Nj62PFM5PyEQvF2= MkHuV2FPT0WU
EB-3 MnPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\Le2lEPTB;Nz6wO|I{OyEQvF2= NHPu[JdUSU6JRWK=
697 NF7uOW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4SwRmlEPTB;OT6yOFMzQSEQvF2= MWrTRW5ITVJ?
Ramos-2G6-4C10 MknOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nWT2lEPTB;OT61PVg1OiEQvF2= MofWV2FPT0WU
KNS-81-FD NXruSIlFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTj[4NWUUN3ME25MlY6PjV|IN88US=> MX3TRW5ITVJ?
HUTU-80 MoW2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2Kx[2lEPTB;OT63OFY1OiEQvF2= NVm1TGJWW0GQR1XS
LS-411N NWTLcpJQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEOxR5hKSzVyPUGwMlA2PjdizszN Mn:wV2FPT0WU
RPMI-8402 MmD0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\ZdmlEPTB;MUCuNVE3KM7:TR?= MoHqV2FPT0WU
KU812 MlrKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnOOWRYUUN3ME2xNE4zQTlzIN88US=> MXLTRW5ITVJ?
EW-1 MnHhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LKZmlEPTB;MUCuOFQzPSEQvF2= MmnDV2FPT0WU
HC-1 NV70Z5ZQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkC0TWM2OD1zMD60PFQ1KM7:TR?= NWSxWI5VW0GQR1XS
NB69 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnPU25UUUN3ME2xNE42ODR|IN88US=> MnTzV2FPT0WU
MFH-ino NEfKdVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33vcWlEPTB;MUCuPFMxOyEQvF2= M2fjWnNCVkeHUh?=
CCRF-CEM Ml7TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3[2UWlEPTB;MUGuOVk4KM7:TR?= NEHHemlUSU6JRWK=
SK-N-DZ MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfkTWM2OD1zMj6wOFM3KM7:TR?= M4H6VnNCVkeHUh?=
NCI-H720 NUL1[GJjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTF{LkG3NFUh|ryP NX7HcJlmW0GQR1XS
HCC1187 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7mW|dKSzVyPUGyMlIxPDFizszN MYrTRW5ITVJ?
IST-SL2 Mn6yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;tbYNoUUN3ME2xNk41QDd{IN88US=> NVTSWYFEW0GQR1XS
KE-37 MlSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\z[mlEPTB;MUKuO|k3PiEQvF2= MkjhV2FPT0WU
HCC1599 NHvVUolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHFUXFKSzVyPUGyMlkxPjlizszN MWDTRW5ITVJ?
A4-Fuk NIHvZ2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HQeGlEPTB;MUKuPVU5PiEQvF2= NY[4RpFVW0GQR1XS
NKM-1 Ml;rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPCTWM2OD1zMz6yPVI2KM7:TR?= MVLTRW5ITVJ?
BE-13 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTF|Lke5PFkh|ryP Mor6V2FPT0WU
MV-4-11 M1y2OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfkb2U3UUN3ME2xOE4xOzJ2IN88US=> MVfTRW5ITVJ?
OPM-2 NYO5RnMyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7wZ5dKSzVyPUG0MlQxQDVizszN MWrTRW5ITVJ?
KARPAS-422 M{K3cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV71PY04UUN3ME2xOE42OTJ4IN88US=> M1vVO3NCVkeHUh?=
RPMI-8226 NVn1S2ppT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\p[2lEPTB;MUSuPFkyPSEQvF2= NHfmZVdUSU6JRWK=
KARPAS-45 Ml7XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTF3Lke3NVYh|ryP MlXxV2FPT0WU
SK-PN-DW MmK5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTF3Lki2N|Eh|ryP NF7lNZhUSU6JRWK=
LC-2 MoCzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;KUmlEPTB;MU[uNVUxPiEQvF2= MWfTRW5ITVJ?
NCI-H1648 NXHkcJlrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTF4LkK1OEDPxE1? NHPifYxUSU6JRWK=
RL95-2 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjtUmlKSzVyPUG2MlM6PzhizszN NXrVRYNFW0GQR1XS
KNS-42 NVX0OJRYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTsWZc6UUN3ME2xOk44Ojd2IN88US=> NULBPVdKW0GQR1XS
RPMI-6666 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzHTWM2OD1zNj65NlEyKM7:TR?= M{TqTnNCVkeHUh?=
SIG-M5 MmOxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTUTWM2OD1zNz6xPVA{KM7:TR?= MUfTRW5ITVJ?
VA-ES-BJ NU\YPYJ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\jTWM2OD1zNz63OFUyKM7:TR?= MkO0V2FPT0WU
MONO-MAC-6 M{jFPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NED2NXhKSzVyPUG3Mlk{OTJizszN M{DYXnNCVkeHUh?=
LAN-6 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7DOVVUUUN3ME2xPE44PTV5IN88US=> NW[yPXkyW0GQR1XS
A388 M1\wNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTF7LkOwOVkh|ryP NH7kZ4pUSU6JRWK=
SK-NEP-1 NIfTR4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHlTWM2OD1{MD6yNVMzKM7:TR?= M4XsRnNCVkeHUh?=
TE-10 M2XOOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTJyLkWyNlEh|ryP M2rDU3NCVkeHUh?=
HL-60 NXLSfW5mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLBTWM2OD1{MD65NFk6KM7:TR?= NV2xc4tqW0GQR1XS
MC116 NVPBSVU3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zkRmlEPTB;MkGuO|IzOSEQvF2= MlPiV2FPT0WU
SW962 NVX3fFdpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3FUoVKSzVyPUKxMlc6OTVizszN MlL5V2FPT0WU
NOMO-1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTGboZoUUN3ME2yNk43PTZ2IN88US=> MoX1V2FPT0WU
CTB-1 M{T5PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfnTmlKSzVyPUKyMlg3PzFizszN M{DkV3NCVkeHUh?=
MRK-nu-1 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7OSphbUUN3ME2yNk46ODd2IN88US=> MUHTRW5ITVJ?
GR-ST NYTiVlYxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHVdXNKSzVyPUKzMlc3KM7:TR?= M2raVXNCVkeHUh?=
HH M{HhWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{X4O2lEPTB;MkSuNFA{KM7:TR?= MmnmV2FPT0WU
NCI-H1963 M4rCe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEizNINKSzVyPUK0MlA4QDJizszN MlTmV2FPT0WU
QIMR-WIL M2PTb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPsSVR{UUN3ME2yOE45Pzd{IN88US=> M2DNXHNCVkeHUh?=
CGTH-W-1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTJ3LkC3NlMh|ryP NXn5SolVW0GQR1XS
LP-1 NWPWbFI{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4juTWlEPTB;MkWuOlU2OSEQvF2= NIK5PWtUSU6JRWK=
NCI-H748 NWjafWtvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\mW2lEPTB;Mk[uOVE{PyEQvF2= NHzqZZVUSU6JRWK=
PF-382 MmD2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjjTWM2OD1{Nz6yNlI{KM7:TR?= MWfTRW5ITVJ?
ATN-1 NEHKSZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HEdWlEPTB;MkeuN|c{OiEQvF2= Ml;mV2FPT0WU
L-540 NX7jXmtYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXMTWM2OD1{Nz62OFU6KM7:TR?= NHeySGlUSU6JRWK=
LXF-289 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXL2OpI1UUN3ME2yO{44PTF7IN88US=> NHPMfHhUSU6JRWK=
LS-513 NFvLUoVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrzdoNKSzVyPUK4MlE5ODdizszN M3zMNnNCVkeHUh?=
NCI-H1581 MmLVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3VTWM2OD1|MD6zPVc3KM7:TR?= MVvTRW5ITVJ?
ES6 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXkTWM2OD1|MD62PFk6KM7:TR?= MmTjV2FPT0WU
SW982 NH;SeW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;uOmlEPTB;M{CuPFU3PiEQvF2= MmDzV2FPT0WU
DOHH-2 M1LW[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLiTWM2OD1|MT61PFk{KM7:TR?= NYjMXXZDW0GQR1XS
DB NHizWIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTqSHNKSzVyPUOzMlk1OzFizszN NULJWnB2W0GQR1XS
MPP-89 Mmj0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjCe|RKSzVyPUO0MlE4PTZizszN MV3TRW5ITVJ?
LB831-BLC MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTN2LkWxPFQh|ryP NFLLOnhUSU6JRWK=
NB5 NXz2W3lHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUGwdXRwUUN3ME2zOE45PTN3IN88US=> MmDJV2FPT0WU
GB-1 M{G4WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TGeWlEPTB;M{WuNFQ3QSEQvF2= M3X3VXNCVkeHUh?=
TE-15 NYLIfolbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2S3fmlEPTB;M{WuNlI{QCEQvF2= NGHJT3BUSU6JRWK=
LC4-1 M3;sOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XwVGlEPTB;M{WuN|g1PyEQvF2= NV7qU5N4W0GQR1XS
NCI-H747 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPVVoNKSzVyPUO2MlE{PjlizszN MVzTRW5ITVJ?
NTERA-S-cl-D1 M4TpTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrQTWM2OD1|OD63N|Q4KM7:TR?= MkLyV2FPT0WU
SK-MM-2 NX7wWm11T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHkTlJLUUN3ME20NE4yOTR4IN88US=> Ml\pV2FPT0WU
TGW NHHVe2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TXUWlEPTB;NEGuNFU3OyEQvF2= NYLBTIlRW0GQR1XS
ONS-76 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HPXGlEPTB;NEKuOFg5OyEQvF2= M4\TNnNCVkeHUh?=
CPC-N MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vDe2lEPTB;NEKuPVk4OSEQvF2= MmfLV2FPT0WU
ES4 NHjQZ2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTR2LkSxOVMh|ryP MVzTRW5ITVJ?
Daudi MmnGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PUbGlEPTB;NEWuNFgzPyEQvF2= NYO4[|VwW0GQR1XS
MOLT-4 NXuxV5NqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;OO2lEPTB;NEWuNFg2OyEQvF2= NU\wSHd[W0GQR1XS
HT-144 NVLscVZVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPZTWM2OD12Nj63NlYh|ryP M2C2OnNCVkeHUh?=
SW872 NFTnNWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPnfYNKSzVyPUS4MlE6OzNizszN MWHTRW5ITVJ?
D-283MED MnjsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7OSXJKSzVyPUS4MlM2PDJizszN M3TweHNCVkeHUh?=
NCI-H2126 Mnz6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rmb2lEPTB;NEiuPFQ4PiEQvF2= NXr0e4trW0GQR1XS
NCI-SNU-16 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTR7LkKxOFMh|ryP NHnHZllUSU6JRWK=
CESS MkfjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3y0c2lEPTB;NEmuOVA5QCEQvF2= NHH6c4tUSU6JRWK=
A101D NHjhRoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTR7Lkm3N|Yh|ryP MVrTRW5ITVJ?

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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

文献中の引用 (65)

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