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 NWXyb2xbS3m2b4TvfIlkKEG|c3H5 NUW5WnVrPDhiaB?= NUTDbmhTTE2VTx?= NX\FWVhmS3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhSkGIMzDj[YxteyCneIDy[ZN{cW6pIFHMT{BHOTF5NFygcZV1[W62IHPv[ZhxemW|c3nu[{BGVUx2IIfpeIghUUN3MDDv[kAxNjZ{IN88US=> M1i0NlIyPTd{NUi5
BAF3 NVq4bJpQS3m2b4TvfIlkKEG|c3H5 NXmzVpRuPDhiaB?= MYnEUXNQ NIXUVoNEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBDSUZ|IHPlcIx{KGW6cILld5NqdmdiQVzLJGwyOTl4TTDteZRidnRiY3;lfJBz\XO|aX7nJGVOVDRid3n0bEBKSzVyIH;mJFIvOiEQvF2= MnHSNlE2PzJ3OEm=
BAF3 NWjsZmJXS3m2b4TvfIlkKEG|c3H5 M{PMR|Q5KGh? MWjEUXNQ NHz1NpVEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBDSUZ|IHPlcIx{KGW6cILld5NqdmdiRV3MOE1CVEtid3n0bEBKSzVyIH;mJFAvOjhizszN NHH1SlgzOTV5MkW4PS=>
Kelly NYTUSVdNS3m2b4TvfIlkKEG|c3H5 MknpSG1UVw>? MYHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDL[YxtgSClZXzsd{BmgHC{ZYPzbY5oKEGOSzDGNVE4PExibYX0ZY51KHerdHigTWM2OCCxZjCwMlQzKM7:TR?= M4XEOlIyPTd{NUi5
SH-SY5Y NIDsVFBEgXSxdH;4bYMhSXO|YYm= MYfEUXNQ MYnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTTE1UYTW\IHPlcIx{KGW6cILld5NqdmdiQVzLJGYyOTd2TDDteZRidnRid3n0bEBKSzVyIH;mJFAvPTNizszN NXLwZnUxOjF3N{K1PFk>
SMS-KCN MXzDfZRwfG:6aXOgRZN{[Xl? MljNSG1UVw>? MYrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTUXMuU0OQIHPlcIx{KGW6cILld5NqdmdiQVzLJHIyOjd3UTDteZRidnRid3n0bEBKSzVyIH;mJFAvQTFizszN NHzJZXAzOTV5MkW4PS=>
BAF3 MUXDfZRwfG:6aXOgRZN{[Xl? M4SzNlQ5KGh? MnT5SG1UVw>? MmS1R5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgRmFHOyClZXzsd{BmgHC{ZYPzbY5oKFSnbD3BUGshf2m2aDDJR|UxKG:oIECuNVkh|ryP M1nkNlIyPTd{NUi5
3T3 NYjIbldjTnWwY4Tpc44hSXO|YYm= MVyxJIg> MmizSG1UVw>? MojRTY5pcWKrdHnvckBw\iCUT16gZZN{\XO|ZXSgZZMh\3Kxd4ToJIZi[3Sxcj3pcoR2[2WmIHH1eI9xcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEig{txO M4rPVFIyQDF{NEG0
3T3-E MWrGeY5kfGmxbjDBd5NigQ>? MkOwNUBp MkTHSG1UVw>? NXT1V3NmUW6qaXLpeIlwdiCxZjDUTWUzKGG|c3Xzd4VlKGe{b4f0bEBn[WO2b4KtbY5lfWOnZDDheZRweGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkS0PEDPxE1? NGjkVpkzOThzMkSxOC=>
A549 Mo[wT4lv[XOnIFHzd4F6 NYLmO2ZsOSCq NV\Xfo13TE2VTx?= NFr6XJZKdmirYnn0bY9vKG:oIHj1cYFvKHKnY3;tZolv[W62IHOtUWVVKGurbnHz[UBmgHC{ZYPz[YQh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBJT0ZvaX7keYNm\CCjdYTvdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjByODFOwG0> MoCxNlE5OTJ2MUS=
BAF3-BCL M1y3fmZ2dmO2aX;uJGF{e2G7 M3vvXFEhcA>? NXfmRYROTE2VTx?= M1vEXmlvcGmkaYTpc44hd2ZiQVLMJIF{e2W|c3XkJIF{KGe{b4f0bEBn[WO2b4KtbY5lfWOnZDDheZRweGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iBzLkG1PUDPxE1? NECxRogzOThzMkSxOC=>
HEK293 M{OzfWZ2dmO2aX;uJGF{e2G7 MXSxJIg> NH2wZnRFVVOR MXnJcohq[mm2aX;uJI9nKEG[TDDhd5Nme3OnZDDhd{Boem:5dHig[oFkfG:{LXnu[JVk\WRiYYX0c5Bpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5{OUSg{txO NWDETm9qOjF6MUK0NVQ>
HEK293 MXfGeY5kfGmxbjDBd5NigQ>? Mkf6NUBp NVrpXVhmTE2VTx?= MnvpTY5pcWKrdHnvckBw\iCLUjDhd5Nme3OnZDDhd{Boem:5dHig[oFkfG:{LXnu[JVk\WRiYYX0c5Bpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOi56OEeg{txO M1i3fVIyQDF{NEG0
Jurkat NGnoRmVHfW6ldHnvckBCe3OjeR?= NHPLeocyKGh? MUjEUXNQ NE\pTndKdmirYnn0bY9vKG:oIFzDT{Bie3Onc4Pl[EBieyCpcn;3eIgh\mGldH;yMYlv\HWlZXSgZZV1d3Cqb4PwbI9zgWyjdHnvckB4cXSqIFnDOVAhd2ZiMj63OFEh|ryP NV\SPW81OjF6MUK0NVQ>
KARPAS299 NVrFfZBCU2mwYYPlJGF{e2G7 NUW5eVZzOSCq MV7EUXNQ MYPJcohq[mm2aX;uJI9nKEGOSzDhd5Nme3OnZDDhd{Boem:5dHig[oFkfG:{LXnu[JVk\WRiYYX0c5Bpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5yMjFOwG0> MWqyNVgyOjRzNB?=
PAE NXvn[Gc{TnWwY4Tpc44hSXO|YYm= NIC4U20yKGh? MYfEUXNQ MmPoTY5pcWKrdHnvckBw\iCWUlvCJIF{e2W|c3XkJIF{KGe{b4f0bEBn[WO2b4KtbY5lfWOnZDDheZRweGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkO5PUDPxE1? MYSyNVgyOjRzNB?=
BAF3 MXLGeY5kfGmxbjDBd5NigQ>? Mnv3Nk0{KGR? NInlPHhFVVOR M1LxWGlvcGmkaYTpc44hd2ZiVFXMMYZ2e2WmIHnud5VtcW5icnXj[ZB1d3JiZYjwdoV{e2WmIIfpeIghUUN3MDDv[kAyNjZ2MzFOwG0> MnHhNlM4PDJ{NUK=
KARPAS299 M1L0SGN6fG:2b4jpZ{BCe3OjeR?= MmewNk0{KGR? M{SweWROW09? NV[2fZJbUUN3ME2wMlA3PDJizszN MVSyN|c1OjJ3Mh?=
EBC1 M1nTd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVy3NkBp NGDVXFVFVVOR MlTkTWM2OD1yLkCyN{DPxE1? NV3VUmN1OjN7OUOzNlg>
HCT116 M1HLb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXJRmZlPzJiaB?= NVrkW5Q3TE2VTx?= NIDCZWNKSzVyPUG0MlgzKM7:TR?= MkPtNlM6QTN|Mki=
MCF7 NGXxRphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4f5S|czKGh? NUWyVmVoTE2VTx?= MlvOTWM2OD17LkW4JO69VQ>? MWSyN|k6OzN{OB?=
MDA-MB-231 M2XMOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HHbFczKGh? NGqyV4pFVVOR NGHzZZNKSzVyPUGwMlgh|ryP MV[yN|k6OzN{OB?=
MKN45 NH33NoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXUO|IhcA>? NImy[WtFVVOR NXXvfYlDUUN3ME2wMlAyOyEQvF2= Ml;NNlM6QTN|Mki=
NCI-H441 NHnuNmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TTNFczKGh? MnnnSG1UVw>? M4nUeWlEPTB;MUeuNlUh|ryP NF25WFYzOzl7M{OyPC=>
NCI-H661 M1yxNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nubVczKGh? NH7NOZVFVVOR MlfoTWM2OD1zMT60O{DPxE1? MlToNlM6QTN|Mki=
SK-MEL-28 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHMeI9TPzJiaB?= M2PpOGROW09? NGnIS4JKSzVyPUGwMlk4KM7:TR?= M3W5RVI{QTl|M{K4
SKOV3 M2XmNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDjfmE4OiCq MkDTSG1UVw>? Mnf1TWM2OD1zMj64OUDPxE1? MWOyN|k6OzN{OB?=
SNU5 MoC4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTne2N7PzJiaB?= Mk\wSG1UVw>? M3HqZWlEPTB;MD6wNVYh|ryP M4jyflI{QTl|M{K4
NCI-H2228 NYKwSpNxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\GdFczKGh? M3OwWmROW09? M{jH[mlvcGmkaYTpc44hd2ZiQVzLMYZ2e2mxbjDkdol3\W5iY3XscEBxem:uaX\ldoF1cW:wIIfpeIghUUN3MDDv[kAxNjFzODFOwG0> M{DMVFI1PDN{OUC5
NCI-H3122 M125b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX:3NkBp MlK4SG1UVw>? M{WzdmlvcGmkaYTpc44hd2ZiQVzLMYZ2e2mxbjDkdol3\W5iY3XscEBxem:uaX\ldoF1cW:wIIfpeIghUUN3MDDv[kAxNjFyODFOwG0> NXjrUm5qOjR2M{K5NFk>
NCI-H3122 M1jOSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnhfVA4OiCq NYO0VWR[TE2VTx?= NF2zd5ZKdmirYnn0bY9vKG:oIFHMT{1nfXOrb36g[JJqfmWwIHPlcIwheHKxbHnm[ZJifGmxbjDpckBpfW2jbjDOR2kuUDNzMkKgZ4VtdHNiaHHyZo9zcW6pIFHMT{BIOTJ4OVGgcZV1[W62IIfpeIghUUN3MDDv[kAxNjZ{MzFOwG0> MVmyOFQ{OjlyOR?=
NCI-H3122 NGjaOItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVq3NkBp NWXYSXk1TE2VTx?= M{LxNWlvcGmkaYTpc44hd2ZiQVzLMYZ2e2mxbjDkdol3\W5iY3XscEBxem:uaX\ldoF1cW:wIHnuJIh2dWGwIF7DTU1JOzF{MjDj[YxteyCqYYLic5JqdmdiQVzLJGwyOTl4TTDteZRidnRid3n0bEBKSzVyIH;mJFAvQDN6IN88US=> NHnndFkzPDR|MkmwPS=>
NIH-3T3 MkW3T4lv[XOnIFHzd4F6 NFe0cVUyKGh? NIHaO2pFVVOR NHnhXWFKdmirYnn0bY9vKG:oIHj1cYFvKHerbHSgeJlx\SCHTVy0MYZ2e2WmIFHMT{BmgHC{ZYPz[YQh[XO|ZYPz[YQh[XNicHjvd5Bpd3K7bHH0[YQhSUyNIHzleoVtKHerdHigTWM2OCCxZjCwMlA5KM7:TR?= MX2yOFQ{OjlyOR?=
NIH-3T3 M4Dib2tqdmG|ZTDBd5NigQ>? MoLGNUBp M2LvW2ROW09? Mn:wTY5pcWKrdHnvckBw\iCqdX3hckBGVUx2LX\1d4VlKEGOSzDHNVI3QUFibYX0ZY51KGW6cILld5Nm\CCjc4Pld5Nm\CCjczDwbI9{eGixLVHMT{Bt\X[nbDD3bZRpKEmFNUCgc4YhOC54MEWg{txO MVyyOFQ{OjlyOR?=
NIH-3T3 MYPLbY5ie2ViQYPzZZk> MV[xJIg> M2r1UmROW09? MlfOTY5pcWKrdHnvckBw\iCqdX3hckBGVUx2LX\1d4VlKEGOSzDTNVIxPllibYX0ZY51KGW6cILld5Nm\CCjc4Pld5Nm\CCjczDwbI9{eGixLVHMT{Bt\X[nbDD3bZRpKEmFNUCgc4YhOC54Mk[g{txO M3PzVVI1PDN{OUC5
NIH-3T3 MoCzT4lv[XOnIFHzd4F6 M4XiWFEhcA>? MmP0SG1UVw>? MYDJcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIFyxNVk3VSCvdYThcpQh\XiycnXzd4VlKGG|c3Xzd4VlKGG|IIDoc5NxcG9vQVzLJIxmfmWuIIfpeIghUUN3MDDv[kAxNjh2MzFOwG0> M3\EdFI1PDN{OUC5
NIH-3T3 M3Pz[WtqdmG|ZTDBd5NigQ>? NXP4d2Z1OSCq MmTGSG1UVw>? MmW3TY5pcWKrdHnvckBw\iCqdX3hckBGVUx2LX\1d4VlKEGOSzDMNVE2OlJibYX0ZY51KGW6cILld5Nm\CCjc4Pld5Nm\CCjczDwbI9{eGixLVHMT{Bt\X[nbDD3bZRpKEmFNUCgc4YhOS5yMk[g{txO M{f3elI1PDN{OUC5
BAF3 NHPXdXRHfW6ldHnvckBCe3OjeR?= MYO3NkBp MlvGSG1UVw>? MorMTY5pcWKrdHnvckBw\iCQUF2vRWxMKHS{YX7z[oVkfGWmIHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25id3n0bEBKSzVyIH;mJFAvODVzIN88US=> MWGyOFQ3QDZ|Mh?=
BAF3 Mo\NR5l1d3SxeHnjJGF{e2G7 M1X3fVczKGh? M4XydWROW09? MX3JR|UxRTBwOUig{txO M{LCNlI1PDZ6NkOy
NIH-3T3 NX33WYZkU2mwYYPlJGF{e2G7 MlnwNUBp NEfpc2pKdmirYnn0bY9vKG:oIHj1cYFvKEWPTESt[pV{\WRiQVzLJGYyOTd2TDDteZRidnRiZYjwdoV{e2WmIHHzd4V{e2WmIHHzJJBpd3OyaH:tRWxMKGyndnXsJJdqfGhiSVO1NEBw\iByLkG2OUDPxE1? MmTFNlQ5OTlzMU[=
NIH-3T3 M1\KdGtqdmG|ZTDBd5NigQ>? M3vXNVEhcA>? NIDRN2tKdmirYnn0bY9vKG:oIHj1cYFvKEWPTESt[pV{\WRiQVzLJGMyOTV4WTDteZRidnRiZYjwdoV{e2WmIHHzd4V{e2WmIHHzJJBpd3OyaH:tRWxMKGyndnXsJJdqfGhiSVO1NEBw\iByLkS3PEDPxE1? M1XlU|I1QDF7MUG2
NIH-3T3 NICwNGdMcW6jc3WgRZN{[Xl? NVSzd|JmOSCq MmS0TY5pcWKrdHnvckBw\iCqdX3hckBGVUx2LX\1d4VlKEGOSzDHNVIxOlJibYX0ZY51KGW6cILld5Nm\CCjc4Pld5Nm\CCjczDwbI9{eGixLVHMT{Bt\X[nbDD3bZRpKEmFNUCgc4YhOS5zNEig{txO MUOyOFgyQTFzNh?=
NIH-3T3 NXn4N5kyU2mwYYPlJGF{e2G7 MXexJIg> MWTJcohq[mm2aX;uJI9nKGi3bXHuJGVOVDRvZoXz[YQhSUyNIEGxOVFVcW6|IH31eIFvfCCneIDy[ZN{\WRiYYPz[ZN{\WRiYYOgdIhwe3Cqbz3BUGshdGW4ZXyge4l1cCCLQ{WwJI9nKDNwMEO5JO69VQ>? NHLncWkzPDhzOUGxOi=>
KARPAS299 M3Kz[2tqdmG|ZTDBd5NigQ>? NHjJRpU6OCCvaX6= MX;EUXNQ NV24OIdGUW6qaXLpeIlwdiCxZjDOVG0u\nW|ZXSgRWxMKHCqb4PwbI9zgWyjdHnvckBmgHC{ZYPz[YQhf2m2aDDJR|UxKG:oIECuNVEh|ryP NYjTZpUxOjR7MEC3OVA>
MKN 45 M1:5d2tqdmG|ZTDBd5NigQ>? NGjTdm8yKGh? M2Xoe2ROW09? NUm2[|hkUW6qaXLpeIlwdiCxZjDjMW1mfCCyaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIECuNFIh|ryP MlvrNlQ6ODB5NUC=
A549 NXPIcJN4S3m2b4TvfIlkKEG|c3H5 NIjp[3o1QCCq MX;EUXNQ M12xNmlEPTBib3[gOE4xQDRizszN NV7ybmVlOjR7MEC4N|A>
NCI-H1975 MYLDfZRwfG:6aXOgRZN{[Xl? NYT2XVlGPDhiaB?= M1XMfGROW09? MXPJR|UxKG:oIEeuOVUyKM7:TR?= MXiyOFkxODh|MB?=
NCI-H1993 MlnNR5l1d3SxeHnjJGF{e2G7 MWm0PEBp MnHTSG1UVw>? MkfqTWM2OCCxZjCwMlA3OSEQvF2= M{[5OFI1QTByOEOw
NCI-H1993 MnHSRZBwfG:|aYOgRZN{[Xl? MoX0NUDPxE1? NHfoS2ozPCCq MorTSG1UVw>? M2jsdYRw\XNibn;0JIlv\HWlZTDhdI9xfG:|aYO= MX:yOFkxODh|MB?=
NIH-3T3 M4jxbGN6fG:2b4jpZ{BCe3OjeR?= NVvBdJQ6PDhiaB?= NX[w[JE4TE2VTx?= NWrU[oYyUUN3MDDv[kAxNjN4NDFOwG0> NUC1bmYxOjR7MEC4N|A>
EBC1 M{O0SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPrUJByPzJiaB?= NIHLc4tFVVOR NU\vWIdDUUN3MDDv[kAxNjByNkmg{txO M1PVZVI1QTByOEOx
KARPAS299 NUS1eFVsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTnO|IhcA>? NXr4[Ik2TE2VTx?= M{PMOWlEPTBib3[gNE4zKM7:TR?= NYP5O|RxOjR7MEC4N|E>
NB1 NH7BVlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\vO2lEPTB;OUGuPVghdk1? MXPTRW5ITVJ?
NCI-SNU-5 NWrP[YNMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jCOGlEPTB;MUC1Mlc2KG6P NG\DT3RUSU6JRWK=
SR MlXOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjqNHVrUUN3ME2xNlYvOzFibl2= NIjXZVJUSU6JRWK=
SF539 NXHabXdnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLLeI5KSzVyPUKwOE4zPCCwTR?= MV;TRW5ITVJ?
SU-DHL-1 NXrMdXJXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPLcWdoUUN3ME2zN|YvQDJibl2= Mn:xV2FPT0WU
SCC-3 M17mVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHTN25KSzVyPUO1Ok44PiCwTR?= MlruV2FPT0WU
DEL NWrSSG5CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzkdGpKSzVyPUO2PU46KG6P NEm1bmpUSU6JRWK=
CTV-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7PdZZKSzVyPUW5Ok41QCCwTR?= M{j5bnNCVkeHUh?=
EM-2 NYHwdGZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Moj6TWM2OD14MEGuN|Qhdk1? NUnkT4UyW0GQR1XS
MHH-CALL-2 NHvweYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHUXZNKSzVyPU[4Nk42PyCwTR?= NE\wU4RUSU6JRWK=
KM12 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFT1W5NKSzVyPUewOk46KG6P MWnTRW5ITVJ?
KINGS-1 NF\jcVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\4cYVKSzVyPUe0PU44PSCwTR?= MnPNV2FPT0WU
MEG-01 NFLVO3dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTh3Nz62OkBvVQ>? MYPTRW5ITVJ?
BV-173 M1n1U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;ieIpKSzVyPUGuNFU6QTdizszN MVfTRW5ITVJ?
LAMA-84 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH35XJZKSzVyPUGuN|gzQDJizszN MVPTRW5ITVJ?
KARPAS-299 MkPDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHkZpFKSzVyPUGuOFA5PjFizszN NVHo[Jo5W0GQR1XS
K-562 NVGzepg1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnuzTWM2OD1zLkeyNlY6KM7:TR?= NVPmXVNLW0GQR1XS
SK-LMS-1 M2\rN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfad5JKSzVyPUGuO|Y5PjdizszN MYHTRW5ITVJ?
MOLT-16 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLSTWM2OD1zLkm1OVc2KM7:TR?= Ml70V2FPT0WU
CMK M3zE[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlW0TWM2OD1zLkm2NVU6KM7:TR?= NEDDNoNUSU6JRWK=
ST486 NGHD[oFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml:yTWM2OD1{LkSzNFc{KM7:TR?= M2DLb3NCVkeHUh?=
CI-1 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTJwNEm2OVkh|ryP MUjTRW5ITVJ?
KP-N-RT-BM-1 MmPaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml32TWM2OD1{LkewNVIzKM7:TR?= NV7FSZQyW0GQR1XS
ALL-PO MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3y3e2lEPTB;Mz6xPFIxPyEQvF2= Mk\yV2FPT0WU
KS-1 NFLVTmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4KxW2lEPTB;Mz6yNVIzPSEQvF2= NYL5VGxSW0GQR1XS
Becker MoDUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVm3cYkzUUN3ME20MlI{QTNizszN MYjTRW5ITVJ?
GDM-1 NFi3TlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LHb2lEPTB;ND6yOFYyPyEQvF2= MmnkV2FPT0WU
BC-1 NX:yS3drT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1f1VmlEPTB;ND60PVI4PyEQvF2= NY[1PY02W0GQR1XS
NB14 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\ySGNPUUN3ME20Mlg{PTJ2IN88US=> MljqV2FPT0WU
NOS-1 NYLHNWI5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFn1fllKSzVyPUWuN|M5PzRizszN NIPKXJlUSU6JRWK=
MZ1-PC M1fFVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTVwOEKxOVEh|ryP NWnJWIJYW0GQR1XS
A498 MkTDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\LcWlEPTB;Nj6wPFQ4OyEQvF2= M4C3T3NCVkeHUh?=
EW-16 MkmyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTZwM{e3O|Mh|ryP M4HxS3NCVkeHUh?=
NALM-6 NF3oS|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfpPZZKSzVyPU[uOlg{QDdizszN NEXnTGZUSU6JRWK=
EB-3 NHfnb4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\vRnFKSzVyPUeuNFczOzNizszN MmHJV2FPT0WU
697 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDVWZg1UUN3ME25MlI1OzJ7IN88US=> MWXTRW5ITVJ?
Ramos-2G6-4C10 NV;PVnNjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTlwNUm4OFIh|ryP NFfZOXRUSU6JRWK=
KNS-81-FD NX3UfnVkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrNSXVKSzVyPUmuOlk3PTNizszN MkHLV2FPT0WU
HUTU-80 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTEbIc5UUN3ME25Mlc1PjR{IN88US=> NHPrcmpUSU6JRWK=
LS-411N NHi3dGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUeybndCUUN3ME2xNE4xPTZ5IN88US=> MkG3V2FPT0WU
RPMI-8402 MnO5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVj2O49FUUN3ME2xNE4yOTZizszN MYHTRW5ITVJ?
KU812 NEe3VYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTFyLkK5PVEh|ryP M1;XWXNCVkeHUh?=
EW-1 NW\3Z|NJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnz5TWM2OD1zMD60OFI2KM7:TR?= NVvGVoh2W0GQR1XS
HC-1 M3mxT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLmSYVKSzVyPUGwMlQ5PDRizszN M4XrU3NCVkeHUh?=
NB69 M1T4d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTiPJRKSzVyPUGwMlUxPDNizszN NWDLdWVOW0GQR1XS
MFH-ino MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonnTWM2OD1zMD64N|A{KM7:TR?= M2nZUnNCVkeHUh?=
CCRF-CEM Mn\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPQcXpyUUN3ME2xNU42QTdizszN Mk\1V2FPT0WU
SK-N-DZ NWLCdVVtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTF{LkC0N|Yh|ryP M3XOZXNCVkeHUh?=
NCI-H720 NFX5Wo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPxXmZKSzVyPUGyMlE4ODVizszN M{j3UXNCVkeHUh?=
HCC1187 NFrVTllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFH6O4xKSzVyPUGyMlIxPDFizszN MU\TRW5ITVJ?
IST-SL2 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTF{LkS4O|Ih|ryP M2TRdHNCVkeHUh?=
KE-37 MlfWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknNTWM2OD1zMj63PVY3KM7:TR?= NE\2dItUSU6JRWK=
HCC1599 M{PUeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvsdnR6UUN3ME2xNk46ODZ7IN88US=> MoT2V2FPT0WU
A4-Fuk NV;rU2dQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7lTWM2OD1zMj65OVg3KM7:TR?= NVfLVVVlW0GQR1XS
NKM-1 NV7s[GcyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPLT2lZUUN3ME2xN{4zQTJ3IN88US=> NIfhTI9USU6JRWK=
BE-13 NWnofoNST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnrTWM2OD1zMz63PVg6KM7:TR?= NIHHOmVUSU6JRWK=
MV-4-11 MkWyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XKe2lEPTB;MUSuNFMzPCEQvF2= MX;TRW5ITVJ?
OPM-2 MmrkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUf6S|JIUUN3ME2xOE41ODh3IN88US=> NW\5O5NIW0GQR1XS
KARPAS-422 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{n2TmlEPTB;MUSuOVEzPiEQvF2= M3vGZ3NCVkeHUh?=
RPMI-8226 M1HFVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7NOVlKSzVyPUG0Mlg6OTVizszN MVTTRW5ITVJ?
KARPAS-45 NFTMSJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTIW5NKSzVyPUG1Mlc4OTZizszN NIXVbnFUSU6JRWK=
SK-PN-DW MkiwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3K5[2lEPTB;MUWuPFY{OSEQvF2= M17rUXNCVkeHUh?=
LC-2 M3q0dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnaTIZKSzVyPUG2MlE2ODZizszN M{PZXnNCVkeHUh?=
NCI-H1648 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HUVWlEPTB;MU[uNlU1KM7:TR?= NHOybZFUSU6JRWK=
RL95-2 NYDOcmJpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTF4LkO5O|gh|ryP NILQWVRUSU6JRWK=
KNS-42 NH\kcphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTF4LkeyO|Qh|ryP NWq5fm1VW0GQR1XS
RPMI-6666 NEPKSIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vMe2lEPTB;MU[uPVIyOSEQvF2= NIXs[29USU6JRWK=
SIG-M5 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILse5dKSzVyPUG3MlE6ODNizszN MYfTRW5ITVJ?
VA-ES-BJ MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTF5Lke0OVEh|ryP MV7TRW5ITVJ?
MONO-MAC-6 MkLyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTNO4ZjUUN3ME2xO{46OzF{IN88US=> M4\BXHNCVkeHUh?=
LAN-6 MoLlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHQTWM2OD1zOD63OVU4KM7:TR?= MWfTRW5ITVJ?
A388 M2O3e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVO1SodKUUN3ME2xPU4{ODV7IN88US=> M{T5e3NCVkeHUh?=
SK-NEP-1 NV7ZOlVuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXYTWM2OD1{MD6yNVMzKM7:TR?= NEnk[mNUSU6JRWK=
TE-10 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWLYc4sxUUN3ME2yNE42OjJzIN88US=> MmLIV2FPT0WU
HL-60 MnXZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHDW|E1UUN3ME2yNE46ODl7IN88US=> MoXDV2FPT0WU
MC116 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPUTWM2OD1{MT63NlIyKM7:TR?= M{ezbXNCVkeHUh?=
SW962 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;zVWlEPTB;MkGuO|kyPSEQvF2= NXPWVG9PW0GQR1XS
NOMO-1 MofQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXSTWM2OD1{Mj62OVY1KM7:TR?= MVPTRW5ITVJ?
CTB-1 M1fEW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILwSpVKSzVyPUKyMlg3PzFizszN M3rL[3NCVkeHUh?=
MRK-nu-1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTJ{LkmwO|Qh|ryP MWnTRW5ITVJ?
GR-ST NXHDR|NUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETIcGpKSzVyPUKzMlc3KM7:TR?= MmTDV2FPT0WU
HH NHPmemJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTJ2LkCwN{DPxE1? NXu2[oZsW0GQR1XS
NCI-H1963 M3\3bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nSR2lEPTB;MkSuNFc5OiEQvF2= MYDTRW5ITVJ?
QIMR-WIL Mm\jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTSUodEUUN3ME2yOE45Pzd{IN88US=> M1nJOnNCVkeHUh?=
CGTH-W-1 NFqyZ|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTWRlF1UUN3ME2yOU4xPzJ|IN88US=> M1K5VXNCVkeHUh?=
LP-1 M{\4RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIT6VYRKSzVyPUK1MlY2PTFizszN NIXDV|ZUSU6JRWK=
NCI-H748 NULFclNYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\DTWM2OD1{Nj61NVM4KM7:TR?= MWfTRW5ITVJ?
PF-382 NW\4[odtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjtfYtKSzVyPUK3MlIzOjNizszN NX3HSJJkW0GQR1XS
ATN-1 MoP6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTJ5LkO3N|Ih|ryP NXuyTIhVW0GQR1XS
L-540 MmLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTLTWM2OD1{Nz62OFU6KM7:TR?= MmTSV2FPT0WU
LXF-289 NU[3SW1zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jZdGlEPTB;MkeuO|UyQSEQvF2= NEXuXYtUSU6JRWK=
LS-513 NF\1OVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHNS3pKSzVyPUK4MlE5ODdizszN M2PrfXNCVkeHUh?=
NCI-H1581 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnuUG45UUN3ME2zNE4{QTd4IN88US=> MUjTRW5ITVJ?
ES6 M2H2Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7hUm9TUUN3ME2zNE43QDl7IN88US=> MmCzV2FPT0WU
SW982 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2qwc2lEPTB;M{CuPFU3PiEQvF2= MoXuV2FPT0WU
DOHH-2 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{m3cGlEPTB;M{GuOVg6OyEQvF2= M4\GNHNCVkeHUh?=
DB NHq2d5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTN|Lkm0N|Eh|ryP NH3z[5pUSU6JRWK=
MPP-89 MmOyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLG[oFKSzVyPUO0MlE4PTZizszN MmnZV2FPT0WU
LB831-BLC Ml;3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofDTWM2OD1|ND61NVg1KM7:TR?= MX3TRW5ITVJ?
NB5 M2HZZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;zTWM2OD1|ND64OVM2KM7:TR?= MUfTRW5ITVJ?
GB-1 M1\wd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHKS5dKSzVyPUO1MlA1PjlizszN NE\ONWRUSU6JRWK=
TE-15 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7JRoZKSzVyPUO1MlIzOzhizszN M2DlS3NCVkeHUh?=
LC4-1 NH\pbW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH:xPHhKSzVyPUO1MlM5PDdizszN MYrTRW5ITVJ?
NCI-H747 NWfN[oY1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTN4LkGzOlkh|ryP MkDpV2FPT0WU
NTERA-S-cl-D1 NX;VOnVbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTN6LkezOFch|ryP MnLMV2FPT0WU
SK-MM-2 NUjuRVhlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvmU2ZxUUN3ME20NE4yOTR4IN88US=> NYPFcnNbW0GQR1XS
TGW M4HBTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWqyZod1UUN3ME20NU4xPTZ|IN88US=> M3X3WHNCVkeHUh?=
ONS-76 M{XsXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzITWM2OD12Mj60PFg{KM7:TR?= NUO1cXZqW0GQR1XS
CPC-N NHzIVJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjlfYxLUUN3ME20Nk46QTdzIN88US=> NHzjW5BUSU6JRWK=
ES4 NIrI[lRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnG1TWM2OD12ND60NVU{KM7:TR?= NYO5d3NMW0GQR1XS
Daudi NIXvS5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTR3LkC4Nlch|ryP NYXK[3JyW0GQR1XS
MOLT-4 MlvqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HsOGlEPTB;NEWuNFg2OyEQvF2= M4nqNnNCVkeHUh?=
HT-144 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TETmlEPTB;NE[uO|I3KM7:TR?= M3mwS3NCVkeHUh?=
SW872 M4\BRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmW2TWM2OD12OD6xPVM{KM7:TR?= M{Gzd3NCVkeHUh?=
D-283MED M2nJeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTR6LkO1OFIh|ryP NVizcJVzW0GQR1XS
NCI-H2126 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\CTWM2OD12OD64OFc3KM7:TR?= NX;lRW14W0GQR1XS
NCI-SNU-16 NV[3UnRRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTiTWJWUUN3ME20PU4zOTR|IN88US=> NEnuNYJUSU6JRWK=
CESS MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkH4TWM2OD12OT61NFg5KM7:TR?= M{W4ZnNCVkeHUh?=
A101D M3q1cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTR7Lkm3N|Yh|ryP NIfW[pNUSU6JRWK=

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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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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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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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