BMS-777607

For research use only. Not for use in humans.

目录号：S1561 别名： BMS 817378

CAS No. 1025720-94-8

BMS-777607 (BMS 817378)是一种Met相关的抑制剂，作用于c-Met，Axl，Ron和Tyro3，在无细胞试验中IC50分别为3.9 nM，1.1 nM，1.8 nM和4.3 nM，作用于Met相关靶点比作用于Lck， VEGFR-2，和TrkA/B选择性高40倍，比作用于其他受体和非受体激酶选择性高500多倍。Phase 1/2。

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10mM (1mL in DMSO)	RMB 2041.38	现货
5mg	RMB 976.53	现货
10mg	RMB 1706.13	现货
50mg	RMB 5498.71	现货
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客户使用Selleck生产的BMS-777607发表文献41篇：

Cell Metab, 2020, 4;31(2):406-421 e7

PubMed: 31839486 ( click the link to review the publication )

Nat Med, 2015, 21(12):1464-72

PubMed: 26523970 ( click the link to review the publication )

J Cell Mol Med, 2021, 10.1111/jcmm.16261

PubMed: 33410267 ( click the link to review the publication )

Cancer Res, 2020, canres.1992.2020

PubMed: 33203698 ( click the link to review the publication )

Cancer Sci, 2020, 112(1):133-143

PubMed: 33067904 ( click the link to review the publication )

Front Oncol, 2020, 12;10:700

PubMed: 32477943 ( click the link to review the publication )

PLoS Negl Trop Dis, 2020, 14(9):e0008602

PubMed: 32886656 ( click the link to review the publication )

Cancer Commun (Lond), 2020, 11

PubMed: 32525624 ( click the link to review the publication )

Mol Inform, 2020, 10.1002/minf.202000181

PubMed: 33274845 ( click the link to review the publication )

Genes Cancer, 2020, 11(3-4):106-121

PubMed: 33488949 ( click the link to review the publication )

Br J Cancer, 2020, 10.1038/s41416-020-01174-z

PubMed: 33257837 ( click the link to review the publication )

J Cancer Sci Clin Ther, 2020, 4(4):511-525

PubMed: 33283192 ( click the link to review the publication )

Mol Cell, 2019, 10.1016/j.molcel.2019.05.022

PubMed: 31230815 ( click the link to review the publication )

Cancer Res, 2019, 79(10):2669-2683

PubMed: 30877108 ( click the link to review the publication )

Breast Cancer Res, 2019, 21(1):43

PubMed: 30898150 ( click the link to review the publication )

Front Immunol, 2019, 10:2702

PubMed: 31824496 ( click the link to review the publication )

Front Oncol, 2019, 9:1138

PubMed: 31781483 ( click the link to review the publication )

Int J Mol Sci, 2019,

PubMed: 31752449 ( click the link to review the publication )

Front Endocrinol (Lausanne), 2019, 10:89

PubMed: 30863365 ( click the link to review the publication )

Oncotarget, 2019,

PubMed: 30863492 ( click the link to review the publication )

Cancer Res, 2018, 10.1158/0008-5472.CAN-18-1106

PubMed: 30413412 ( click the link to review the publication )

Mol Cancer Res, 2018, 16(2):333-344

PubMed: 29133594 ( click the link to review the publication )

NPJ Breast Cancer, 2018, 4:36

PubMed: 30456298 ( click the link to review the publication )

Oncotarget, 2018, 9(78):34735-34747

PubMed: 30410673 ( click the link to review the publication )
PLoS Biol, 2018, 16(8):e2005756

PubMed: 30157175 ( click the link to review the publication )

Mol Cancer Res, 2017,

PubMed: 28184013 ( click the link to review the publication )

Oncotarget, 2017,

PubMed: 28938607 ( click the link to review the publication )

J Med Chem, 2015, 58(1):466-79

PubMed: 25478866 ( click the link to review the publication )

J Pathol, 2015, 237(1):14-24

PubMed: 25965880 ( click the link to review the publication )

J Med Chem, 2015,

PubMed: ( click the link to review the publication )

Cell Death Dis, 2015, 6:e1646

PubMed: 25695599 ( click the link to review the publication )

Chem Biol, 2015, 22(4):504-515

PubMed: 25865310 ( click the link to review the publication )

J Clin Invest, 2014, 124(11):4737-52

PubMed: 25250573 ( click the link to review the publication )

Nat Commun, 2014, 5:5712

PubMed: 25502142 ( click the link to review the publication )

Mol Cancer Ther, 2014, 13(1):37-48

PubMed: 24233399 ( click the link to review the publication )

Hum Cell, 2014, 10.1007/s13577-014-0102-2

PubMed: 25304900 ( click the link to review the publication )

Nat Immunol, 2014, 15(10):920-8

PubMed: 25194421 ( click the link to review the publication )

Mol Cancer Ther, 2013, 12(5):725-36

PubMed: 23468529 ( click the link to review the publication )

Mol Oncol, 2013, 8(3):469-82

PubMed: 24444656 ( click the link to review the publication )

Neoplasia, 2013, 15(3):296-304

PubMed: 23479507 ( click the link to review the publication )

Eur J Med Chem, 2013, 70:789-801

PubMed: 24239626 ( click the link to review the publication )

产品安全说明书

c-Met抑制剂选择性比较

生物活性

产品描述

特性

BMS 777607是有效的Met家族成员抑制剂，比作用于Lck, VEGFR-2,和TrkA/B的选择性高40多倍，比作用同样其他受体和非受体激酶选择性高500多倍。

靶点

Axl ^[1] (Cell-free assay)	RON ^[1] (Cell-free assay)	Met ^[1] (Cell-free assay)	Tyro3 ^[1] (Cell-free assay)	Mer ^[1] (Cell-free assay)	点击更多
1.1 nM	1.8 nM	3.9 nM	4.3 nM	14 nM	点击更多

体外研究

BMS-777607是ATP竞争性Met激酶选择性抑制剂，有效抑制c-Met自磷酸化，作用于GTL-16细胞裂解物， IC50为20 nM，且选择性抑制Met驱动的肿瘤细胞系如GTL-16细胞系, H1993和 U87增殖。^[1] BMS-777607 作用于DU145前列腺癌细胞，抑制肝细胞生长因子 (HGF)引起的c-Met自磷酸化， IC50<1 nM 。BMS 777607对肿瘤细胞生长作用效果不大，但是作用于PC-3 和DU145 细胞，抑制HGF诱导的细胞分散。BMS 777607作用于这两种细胞，也抑制刺激的细胞迁移和入侵，IC50<0.1 μM，这种作用存在剂量依赖性。^[2] BMS 777607(~10 μM)作用于高度转移性鼠科KHT细胞2小时，有效清除自磷酸化的c-Met水平，IC50为10 nM，不影响全部 c-Met,导致下游信号分子包括 ERK, Akt, p70S6K 和 S6受抑制，这种作用存在剂量依赖性。纳摩尔级BMS-777607(~1 μM)处理24小时,有效抑制KHT细胞分散，活动，和入侵，这与MET基因抑制相关,适当影响细胞增殖和集落形成。^[3]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
PC-3	MUfGeY5kfGmxbjDhd5NigQ>?	NVnlU2F[OC5zIN88US=>		NIDZeZBFVVOR	M4Gy[IV5cGmkaYTzJIlvcGmkaYTvdpkh\W[oZXP0JI9vKEiJRj3pcoR2[2WmIHPlcIwhe2OjdITldolv\w>?	NEG4Wmk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEWxOVk1Oyd-MkC1NVU6PDN:L3G+
DU145	NITqbG1HfW6ldHnvckBie3OjeR?=	NFzsU2cxNjFizszN		NY\MfnRwTE2VTx?=	NYS4d\|A1\XiqaXLpeJMhcW6qaXLpeI9zgSCnZn\lZ5Qhd25iSFfGMYlv\HWlZXSgZ4VtdCC\|Y3H0eIVzcW6p	NGTBcZA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEWxOVk1Oyd-MkC1NVU6PDN:L3G+
PC-3	NHjlXGxHfW6ldHnvckBie3OjeR?=	M4X6RVAvODFizszN		M2joNWROW09?	MYrzeZBxemW\|c3XzJGhITi2rbnT1Z4VlKGOnbHygcYloemG2aX;u	MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODVzNUm0N{c,OjB3MUW5OFM9N2F-
DU145	MXnGeY5kfGmxbjDhd5NigQ>?	NGjUS3gxNjBzIN88US=>		NH;4WpJFVVOR	M4H0[5N2eHC{ZYPz[ZMhUEeILXnu[JVk\WRiY3XscEBucWe{YYTpc44>	NFjzU3o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEWxOVk1Oyd-MkC1NVU6PDN:L3G+
PC-3	NIrtT5JHfW6ldHnvckBie3OjeR?=	NVLHdodDOC5zIN88US=>		NUTTTmVDTE2VTx?=	M{jWdIlueGGrcoOgTGdHNW2nZHnheIVlKGOnbHygbY53[XOrb36=	MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODVzNUm0N{c,OjB3MUW5OFM9N2F-
DU145	NIDqSlFHfW6ldHnvckBie3OjeR?=	M2LuelAvOSEQvF2=		M4Pk[2ROW09?	MYDpcZBicXK\|IFjHSk1u\WSrYYTl[EBk\WyuIHnueoF{cW:w	MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODVzNUm0N{c,OjB3MUW5OFM9N2F-
PC-3	M3PnVmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	M4mwPZ4yOCEQvF2=		NIe5ZYlFVVOR	MYfy[YR2[2W\|IHPlcIwheHKxbHnm[ZJifGmxbh?=	MlLSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB3MUW5OFMoRjJyNUG1PVQ{RC:jPh?=
KHT	NYC5SWlNU2mwYYPlJIF{e2G7			NXHCOlQyTE2VTx?=	NXmxdlZQ[myxY3vzJJRp\SClLV3leEB{cWewYXzpcocheGG2aIfhfUB4cXSqIFnDOVAhd2ZiMUCgcm0>	Mmf0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{OE[1NlMoRjJ{Mki2OVI{RC:jPh?=
KHT	MnrSSpVv[3Srb36gZZN{[Xl?	NEjRSXF,OSEQvF2=		M2\X[GROW09?	MUPwdoV3\W62czDzdI9vfGGwZX;1d{BMUFRiY3XscEB{[2G2dHXybY5oKHerdHigTWM2OCCxZjCwMlEuOC53IN88US=>	MnW1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{OE[1NlMoRjJ{Mki2OVI{RC:jPh?=
KHT	Mn3CSpVv[3Srb36gZZN{[Xl?	MnXtglAvPSEQvF2=		MkDWSG1UVw>?	MWTpcohq[mm2czDj[YxtKG2rZ4LheIlwdg>?	NEHYRng9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkK4OlUzOyd-MkKyPFY2OjN:L3G+
KHT	M3Ox[WZ2dmO2aX;uJIF{e2G7	M{LHVZ4xNjVizszN		MYPEUXNQ	Mn60bY5pcWKrdIOgZ4VtdCCrbo\hd4lwdg>?	MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJ6NkWyN{c,OjJ{OE[1NlM9N2F-
KHT	NILhUJJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MYf+NVAh\|ryP		NVSzZ2UyTE2VTx?=	NGXpWppqdmirYnn0d{BMUFRiY3XscEBxem:uaX\ldoF1cW:w	NWW3UoZ2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyPFY2OjNpPkKyNlg3PTJ\|PD;hQi=>
T-47D	NF3uPGtIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	M1SxeJ42KM7:TR?=		NUHNe\|BjTE2VTx?=	MXTpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36=	M3\hUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|NE[4OVI6Lz5{M{S2PFUzQTxxYU6=
ZR-75-1	MX3Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	M{i3[542KM7:TR?=		NF\RcWNFVVOR	NWj3T3ZucW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v	MkK0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2Nki1NlkoRjJ\|NE[4OVI6RC:jPh?=
T-47D	MXHGeY5kfGmxbjDhd5NigQ>?	MYSxNEDPxE1?		MmnwSG1UVw>?	NXr3c3NtUW6mdXPld{Bxd2y7cHzvbYR6KGK7IEi2JEU>	NVf4bHlRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0Olg2OjlpPkKzOFY5PTJ7PD;hQi=>
ZR-75-1	MlnnSpVv[3Srb36gZZN{[Xl?	MVmxNEDPxE1?		NEjQWmZFVVOR	MnrjTY5lfWOnczDwc4x6eGyxaXT5JIJ6KDh6JR?=	NXWyXmJwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0Olg2OjlpPkKzOFY5PTJ7PD;hQi=>
T-47D	MlHPSpVv[3Srb36gZZN{[Xl?	NFnGblIyOCEQvF2=		M1\CfGROW09?	MVPpcohq[mm2czDBWXJMNUJiZoXuZ5Rqd25iYX7kJIlv\HWlZYOgbZR{KHC{b4TlbY4h\GWpcnHkZZRqd25?	MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR4OEWyPUc,OjN2Nki1Nlk9N2F-
CHRF	NUnWZoNtTnWwY4Tpc44h[XO\|YYm=	NWWxb5Y1OTBizszN		NH3MPFRFVVOR	NFvXTnJqdmirYnn0d{Bk\WyuIHTpeol{cW:w	NEHibXc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOwOFkxOCd-MkWzNFQ6ODB:L3G+
HPDE	Mn76SpVv[3Srb36gZZN{[Xl?	NX36UYZ4OTBizszN		NHHVd4JFVVOR	M{LCb4Jtd2OtczDjc45{fGm2dYTpeoUh[WO2aY\heIlwdiCjbnSg[IVkemWjc3XkJGFMXCC\|aXfuZYxqdmd?	NYDZNnBFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[0O\|c{OTRpPkK2OFc4OzF2PD;hQi=>
U118MG	NH30e4lMcW6jc3WgZZN{[Xl?	NHT3[\|Z,OyEQvF2=		Mm\MSG1UVw>?	MnK1Zoxw[2u\|IFHYUEBxcG:\|cHjvdplt[XSrb36=	NYrpeZRERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4OFg2OjRpPkK2PFQ5PTJ2PD;hQi=>
SF126	MYDLbY5ie2ViYYPzZZk>	NFvqNo9,OyEQvF2=		NXfxPXBqTE2VTx?=	Ml7xZoxw[2u\|IFHYUEBxcG:\|cHjvdplt[XSrb36=	M32wfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OES4OVI1Lz5{Nki0PFUzPDxxYU6=
U118MG	NUC3elc5S3m2b4jpZ4l1gSCjc4PhfS=>	NVHYeoNNOTJwNTFOwG0>		NVr3O4tVTE2VTx?=	NXjabYU3\GWlcnXhd4V{KGeuaX;tZUBk\WyuII\pZYJqdGm2eR?=	MknMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ6NEi1NlQoRjJ4OES4OVI1RC:jPh?=
SF126	NYP4PVEzS3m2b4jpZ4l1gSCjc4PhfS=>	NXXkb2VlOTJwNTFOwG0>		NFXucJJFVVOR	MY\k[YNz\WG\|ZYOg[4xqd22jIHPlcIwhfmmjYnnsbZR6	M3PJRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OES4OVI1Lz5{Nki0PFUzPDxxYU6=
U118MG	MUfBdI9xfG:\|aYOgZZN{[Xl?	Mn7tNVIvPSEQvF2=		Ml[ySG1UVw>?	NIrMUZlqdmS3Y3XzJIdtcW:vYTDj[YxtKGGyb4D0c5Nqew>?	MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh2OEWyOEc,OjZ6NEi1NlQ9N2F-
SF126	MVfBdI9xfG:\|aYOgZZN{[Xl?	Mn\GNVIvPSEQvF2=		NUnkTW1uTE2VTx?=	NYHzZmM3cW6mdXPld{BodGmxbXGgZ4VtdCCjcH;weI9{cXN?	MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh2OEWyOEc,OjZ6NEi1NlQ9N2F-
U118MG	MmHZSpVv[3Srb36gZZN{[Xl?	MnfzNVIvPSEQvF2=		NICzXJBFVVOR	MWTicI9kc3NiZ3zpc41iKGOnbHygcYloemG2aX;uJIFv\CCrbo\hd4l3\SCpcn;3eIgheGG2dHXyci=>	NV\xUYlNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4OFg2OjRpPkK2PFQ5PTJ2PD;hQi=>
SF126	MoLuSpVv[3Srb36gZZN{[Xl?	MnzWNVIvPSEQvF2=		MVvEUXNQ	MVvicI9kc3NiZ3zpc41iKGOnbHygcYloemG2aX;uJIFv\CCrbo\hd4l3\SCpcn;3eIgheGG2dHXyci=>	MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh2OEWyOEc,OjZ6NEi1NlQ9N2F-
GTL16	MnfMSpVv[3Srb36gZZN{[Xl?		NHPwXFI{OCCvaX7z		MWnJcohq[mm2aX;uJI9nKE2ndDDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iR2TMNVYh[2WubIOgZYZ1\XJiM{CgcYlveyxiSVO1NEA:KDBwMEKg{txONg>?	M{HDV\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7Mk[wO\|EyLz5zOUK2NFcyOTxxYU6=
GTL16	NVTtbYJkSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		MoXWO\|IhcHK\|		MmSxRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDN[ZQu\GWyZX7k[Y51KGi3bXHuJGdVVDF4IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFNiYYPzZZktKEmFNUCgQUAxNjFizszNMi=>	NHzrZnU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUK2NFcyOSd-MUmyOlA4OTF:L3G+
NCI-H1993	MWrBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		Mn7sO\|IhcHK\|		MoX1RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDN[ZQu\GWyZX7k[Y51KGi3bXHuJG5EUS2KMUm5N{Bk\WyuczDh[pRmeiB5MjDodpMh[nliTWTTJIF{e2G7LDDJR\|UxKD1iMD6xOUDPxE1w	NFnveGc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUK2NFcyOSd-MUmyOlA4OTF:L3G+
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OHS-50	NULOTJNkeUiWUzDhd5NigQ>?				MVzxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhV0iVLUWwJINmdGy\|	MkLmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
A673	NHTIe4VyUFSVIHHzd4F6				NYDmRphUeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhSTZ5MzDj[Yxteyl?	MnrxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC	NV7UPJZFeUiWUzDhd5NigQ>?				MkPFdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgV2suVi2PQzDj[Yxtew>?	M3XiZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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MG 63 (6-TG R)	NYXyVWY1eUiWUzDhd5NigQ>?				NFzLWlFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBOTyB4MzCoOk1VTyCUKTDj[Yxtew>?	NX:wTZFpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
MGHU3	NIDkdZlCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		M1\BVVczKGi{cx?=		MYXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2JSGWzJINmdGy\|IHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvR3zvJIF{e2G7	NH[4c2k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|MEOwPVY4OSd-M{CzNFk3PzF:L3G+
RT112	NETLVmtCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		MVy3NkBpenN?		MnzTRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCUVEGxNkBk\WyuczDh[pRmeiB5MjDodpMh[nliQ3XscHRqfGW{LVfsc{Bie3OjeR?=	MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODNyOU[3NUc,OzB\|MEm2O\|E9N2F-

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	p-c-Met / c-Met / p-FAK / p-c-Src / p-Akt / p-S6K / p-S6; PubMed: 22639908 BMC Cancer Effect of BMS-777607 on c-Met signaling in PC-3 cells PC-3 cells were treated with indicated doses of BMS-777607 for 1 h (A) or with BMS-777607 (1 μM) for indicated times (B). Whole cell lysates were harvested and analyzed by Western blot, with actin as a loading control. Data represent 1 of 2 independent experiments. p53 / p21 / Survivin / p-Rb / Rb ; PubMed: 24444656 Mol Oncol BMS-777607 increases p21/WAF1 and survivin expression but down-regulates Rb expression. T-47D and ZR-75-1 cells were treated with 5 μM BMS-777607 for different time intervals. Cellular proteins (50 μg per sample) from cell lysates were subjected to Western blot analysis using individual antibodies specific to p53, p21/WAF1, survivin, regular and phospho-Rb. B-actin was used as the loading control.	22639908 24444656
Immunofluorescence	α-tubulin / survivin; PubMed: 24444656 Mol Oncol Abnormal accumulation of survivin and its disassociation with condensed DNA and mitotic spindle. Both T-47D and ZR-75-1 cells were treated with 5 μM BMS-777607 for 72 h followed by immunofluorescent analysis using antibodies specific to survivin and α-tubulin. Cells were also stained with DAPI for nuclear DNA. Images shown here are from one of two experiments with similar results.	24444656

体内研究

BMS 777607按6.25-50 mg/kg剂量口服处理给药携带GTL-16人类移植瘤的无胸腺小鼠，明显降低肿瘤体积，且没有毒性。^[1] BMS 777607按25 mg/kg剂量每天处理6-8周大的注射啮齿类纤维肉瘤KHT细胞的雌性C3H/HeJ小鼠，降低 KHT肺肿瘤结节数量,提高形态出血, 且明显修复损害转移表型，与对照组相比，没有明显毒性。BMS 777607按 10 mg/kg 低剂量处理，也适度但不显著抑制肺结节形成。^[3]

激酶实验：^[4]	- 合并 Met Kinase Assay: The kinase reaction consists of baculovirus expressed GST-Met, 3 μg of poly(Glu/Tyr), 0.12 μCi ³³P γ-ATP, 1 μM ATP in 30 μL of kinase buffer (20 mM Tris-Cl, 5 mM MnCl2, 0.1 mg/mL BSA, 0.5 mM DTT). Reactions are incubated for 1 hour at 30 °C and stopped by the addition of cold trichloroacetic acid (TCA) to a final concentration of 8%. TCA precipitates are collected onto GF/C unifilter plates using a Filtermate universal harvester, and the filters are quantitated using a TopCount 96-well liquid scintillation counter. Dose response curves are generated to determine the concentration required to inhibit 50% of substrate phosphorylation (IC50). BMS 777607 is dissolved at 10 mM in dimethylsulfoxide (DMSO) and evaluated at 10 concentrations, in duplicate.
细胞实验：^[3]	- 合并 Cell lines: 啮齿类纤维肉瘤KHT细胞 Concentrations: 溶于DMSO，作为储存液(10 mM), 终浓度为10 μM 左右 Incubation Time: 2, 24和96小时 Method: 用连续稀释的BMS 777607 处理KHT细胞96小时，然后进行MTT实验和台酚蓝排除，分别测定细胞增殖和细胞死亡。KHT细胞集落和BMS 777607温育24小时，然后用结晶紫(0.1%)染色，然后显影，测定细胞分散情况。使用无菌的1 ml吸管端在融合的KHT单层细胞上划2 mm 痕，随后用BMS-777607处理24小时，在4块随机区域中计数迁移到剥蚀地细胞数，用于测定细胞迁移情况。为了测定细胞入侵，用Matrigel预包被的转移嵌入板(8 μm 孔膜)，和无血清培养基在有或无BMS 777607存在时，在37^oC下温育2小时,使Matrigel再水化。悬浮在无血清培养基上的细胞装到小室顶端，悬浮在含10% FBS的完全培养基上的细胞装到小室底端，作为化学引诱物。温育24小时，移除 Matrigel，用结晶紫染色。显影并计数在滤液下面的入侵细胞。 (Only for Reference)
动物实验：^[3]	- 合并 Animal Models: 携带啮齿类纤维肉瘤KHT细胞的雌性C3H/HeJ小鼠 Dosages: 10-25 mg/kg Administration: 饲喂处理，每天一次 (Only for Reference)

参考文献

[4] Kim KS, et al. J Med Chem, 2008, 51(17), 5330-5341.

- 合并

溶解度 (25°C)

体外	DMSO	47 mg/mL (91.63 mM)
	Water	Insoluble
	Ethanol	Insoluble
体内	从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)： 4% DMSO+45% PEG 300+5% Tween 80+ddH2O	5mg/mL

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据 Download BMS-777607 SDF

分子量	512.89
化学式	C₂₅H₁₉ClF₂N₄O₄
CAS号	1025720-94-8
储存条件	3年-20°C 粉状 2年-80°C 溶于溶剂
别名	BMS 817378

动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO+ % + % Tween 80+ % ddH₂O

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

质量

浓度

体积

分子量
=

×

×

*在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入输出 )

C1

V1

C2

V2
×

=

×

在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

分子量计算器

通过输入化合物的化学式来计算其分子量：

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×
计算

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

常见问题及建议解决方法

问题 1：
What formulation can we use to dissolve S1561 for mice in vivo study?
回答：
S1561 BMS-777607 in 1% DMSO+30% polyethylene glycol+1% Tween 80 at 30 mg/ml is a suspension. It is fine for oral gavage. If you are going to use it for injection, please try the following vehicle: 4% DMSO+30% PEG 300+ddH2O. BMS-777607 can be dissolved in it at 5 mg/ml as a clear solution.

c-Met Signaling Pathway Map

c-Met Inhibitors with Unique Features

选择性强的c-Met抑制剂

PF-04217903 : C-Met-selective, IC50=4.8 nM.
活性最高的c-Met抑制剂

INCB28060 : C-Met, IC50=0.13 nM.
FDA批准的c-Met抑制剂

Crizotinib (PF-02341066) : Approved by FDA for non-small cell lung carcinoma (NSCLC).
最新的c-Met抑制剂

EMD 1214063 ^New : Potent and selective c-Met inhibitor with IC50 of 4 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer.

研究领域

产品类型

定制您的化合物库

BMS-777607

客户使用Selleck生产的BMS-777607发表文献41篇：

产品安全说明书

c-Met抑制剂选择性比较

生物活性

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

参考文献

溶解度 (25°C)

化学数据 Download BMS-777607 SDF

动物体内配方计算器 (澄清溶液)

计算器

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

稀释计算器

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

连续稀释计算器方程

连续稀释

计算结果

分子量计算器

总分子量：g/mol

摩尔浓度计算器

技术支持

常见问题及建议解决方法

c-Met Signaling Pathway Map

c-Met Inhibitors with Unique Features

相关c-Met产品