BMS-777607

For research use only. Not for use in humans.

目录号：S1561

CAS No. 1025720-94-8

BMS-777607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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价格

库存

购买数量

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38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 )

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 )

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 )

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	MWrGeY5kfGmxbjDhd5NigQ>?	NXrIUJV7OC5zIN88US=>		MkjPSG1UVw>?	NFXpTpJmgGirYnn0d{BqdmirYnn0c5J6KGWoZnXjeEBwdiCKR1[tbY5lfWOnZDDj[YxtKHOlYYT0[ZJqdmd?	NX3UO45VRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC1NVU6PDNpPkKwOVE2QTR\|PD;hQi=>
DU145	NUHYR\|ZGTnWwY4Tpc44h[XO\|YYm=	Ml;0NE4yKM7:TR?=		NXXmXnEyTE2VTx?=	NFHhUFdmgGirYnn0d{BqdmirYnn0c5J6KGWoZnXjeEBwdiCKR1[tbY5lfWOnZDDj[YxtKHOlYYT0[ZJqdmd?	NWTIPWJoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC1NVU6PDNpPkKwOVE2QTR\|PD;hQi=>
PC-3	MWnGeY5kfGmxbjDhd5NigQ>?	MYGwMlAyKM7:TR?=		NHOwcIVFVVOR	NV36PFRRe3WycILld5NmeyCKR1[tbY5lfWOnZDDj[YxtKG2rZ4LheIlwdg>?	M{DzOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNUG1PVQ{Lz5{MEWxOVk1OzxxYU6=
DU145	NVvaTFZXTnWwY4Tpc44h[XO\|YYm=	Ml3oNE4xOSEQvF2=		NGHCW5BFVVOR	Mmntd5VxeHKnc4Pld{BJT0ZvaX7keYNm\CClZXzsJI1q\3KjdHnvci=>	NWi3OZpIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC1NVU6PDNpPkKwOVE2QTR\|PD;hQi=>
PC-3	MY\GeY5kfGmxbjDhd5NigQ>?	MoXaNE4yKM7:TR?=		MoHuSG1UVw>?	NEm2ZYpqdXCjaYLzJGhITi2vZXTpZZRm\CClZXzsJIlvfmG\|aX;u	NUjl[Yp7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC1NVU6PDNpPkKwOVE2QTR\|PD;hQi=>
DU145	NWnYW45STnWwY4Tpc44h[XO\|YYm=	MorGNE4yKM7:TR?=		MkDmSG1UVw>?	Mn;KbY1x[Wm{czDIS2YudWWmaXH0[YQh[2WubDDpcpZie2mxbh?=	MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODVzNUm0N{c,OjB3MUW5OFM9N2F-
PC-3	NYDSbFNzT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NI\3fZF,OTBizszN		MVXEUXNQ	NIDuU2Jz\WS3Y3XzJINmdGxicILvcIln\XKjdHnvci=>	MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODVzNUm0N{c,OjB3MUW5OFM9N2F-
KHT	NUHpWnN1U2mwYYPlJIF{e2G7			M1q3N2ROW09?	M{T4c4Jtd2OtczD0bIUh[y2PZYSgd4lodmGuaX7nJJBifGi5YYmge4l1cCCLQ{WwJI9nKDFyIH7N	NGLzZ3k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkK4OlUzOyd-MkKyPFY2OjN:L3G+
KHT	MWfGeY5kfGmxbjDhd5NigQ>?	Mn\zglEh\|ryP		MmfZSG1UVw>?	MWLwdoV3\W62czDzdI9vfGGwZX;1d{BMUFRiY3XscEB{[2G2dHXybY5oKHerdHigTWM2OCCxZjCwMlEuOC53IN88US=>	MlHpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{OE[1NlMoRjJ{Mki2OVI{RC:jPh?=
KHT	M2\mNGZ2dmO2aX;uJIF{e2G7	MlfsglAvPSEQvF2=		MoLPSG1UVw>?	MoK1bY5pcWKrdIOgZ4VtdCCvaXfyZZRqd25?	NY[zPFJDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyPFY2OjNpPkKyNlg3PTJ\|PD;hQi=>
KHT	MV\GeY5kfGmxbjDhd5NigQ>?	NEXDUIJ,OC53IN88US=>		MWXEUXNQ	NYPBWoIxcW6qaXLpeJMh[2WubDDpcpZie2mxbh?=	Mn[3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{OE[1NlMoRjJ{Mki2OVI{RC:jPh?=
KHT	MUTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NHPSbVd,OTBizszN		NIXtfmJFVVOR	NELSXm5qdmirYnn0d{BMUFRiY3XscEBxem:uaX\ldoF1cW:w	NFTJfpo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkK4OlUzOyd-MkKyPFY2OjN:L3G+
T-47D	NI[4WJlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	MYD+OUDPxE1?		MoXpSG1UVw>?	NGnmfFJqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44>	MorZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2Nki1NlkoRjJ\|NE[4OVI6RC:jPh?=
ZR-75-1	MoDwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	NGfme2R,PSEQvF2=		NVXoVIUzTE2VTx?=	M3XHS4lvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=>	MnHXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2Nki1NlkoRjJ\|NE[4OVI6RC:jPh?=
T-47D	NGj5fXpHfW6ldHnvckBie3OjeR?=	NH7oV24yOCEQvF2=		MWrEUXNQ	M1OxcWlv\HWlZYOgdI9tgXCub3nkfUBjgSB6NjCl	NGXQXFc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S2PFUzQSd-MkO0Olg2Ojl:L3G+
ZR-75-1	NWG1VZU1TnWwY4Tpc44h[XO\|YYm=	M2jiW\|ExKM7:TR?=		NYHsdmhGTE2VTx?=	NIrxcJBKdmS3Y3XzJJBwdHmybH;p[Jkh[nliOEil	M2TxOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|NE[4OVI6Lz5{M{S2PFUzQTxxYU6=
T-47D	M13UTmZ2dmO2aX;uJIF{e2G7	MXOxNEDPxE1?		MX;EUXNQ	MYPpcohq[mm2czDBWXJMNUJiZoXuZ5Rqd25iYX7kJIlv\HWlZYOgbZR{KHC{b4TlbY4h\GWpcnHkZZRqd25?	M1T1XFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|NE[4OVI6Lz5{M{S2PFUzQTxxYU6=
CHRF	M1PScWZ2dmO2aX;uJIF{e2G7	NGHUR5QyOCEQvF2=		MnLxSG1UVw>?	MUTpcohq[mm2czDj[YxtKGSrdnnzbY9v	NIewSVQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOwOFkxOCd-MkWzNFQ6ODB:L3G+
HPDE	MYXGeY5kfGmxbjDhd5NigQ>?	NW\IeJZ5OTBizszN		MYnEUXNQ	MlfDZoxw[2u\|IHPvcpN1cXS3dHn2[UBi[3SrdnH0bY9vKGGwZDDk[YNz\WG\|ZXSgRWtVKHOrZ37hcIlv\w>?	NVzH[4p3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[0O\|c{OTRpPkK2OFc4OzF2PD;hQi=>
U118MG	MVvLbY5ie2ViYYPzZZk>	M2fXUJ4{KM7:TR?=		MVHEUXNQ	MkjxZoxw[2u\|IFHYUEBxcG:\|cHjvdplt[XSrb36=	MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh2OEWyOEc,OjZ6NEi1NlQ9N2F-
SF126	MkKyT4lv[XOnIHHzd4F6	MVv+N{DPxE1?		M4HwRmROW09?	MkG4Zoxw[2u\|IFHYUEBxcG:\|cHjvdplt[XSrb36=	NELlPJM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nki0PFUzPCd-Mk[4OFg2OjR:L3G+
U118MG	NVTOPZZYS3m2b4jpZ4l1gSCjc4PhfS=>	MnfUNVIvPSEQvF2=		NX3wbI1LTE2VTx?=	NFjoTFRl\WO{ZXHz[ZMh\2yrb33hJINmdGxidnnhZoltcXS7	M1jn[\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OES4OVI1Lz5{Nki0PFUzPDxxYU6=
SF126	MVzDfZRwgGmlaYT5JIF{e2G7	MXqxNk42KM7:TR?=		MVLEUXNQ	M4TtNIRm[3KnYYPld{BodGmxbXGgZ4VtdCC4aXHibYxqfHl?	M2\5bVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OES4OVI1Lz5{Nki0PFUzPDxxYU6=
U118MG	MljQRZBweHSxc3nzJIF{e2G7	NFu2UGoyOi53IN88US=>		NUHkVWw4TE2VTx?=	M4XGR4lv\HWlZYOg[4xqd22jIHPlcIwh[XCxcITvd4l{	NFLUdIY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nki0PFUzPCd-Mk[4OFg2OjR:L3G+
SF126	M2P0NmFxd3C2b4Ppd{Bie3OjeR?=	MV[xNk42KM7:TR?=		MnvqSG1UVw>?	M4XoPIlv\HWlZYOg[4xqd22jIHPlcIwh[XCxcITvd4l{	MkTqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ6NEi1NlQoRjJ4OES4OVI1RC:jPh?=
U118MG	NFf4[XpHfW6ldHnvckBie3OjeR?=	Mnn5NVIvPSEQvF2=		MlfwSG1UVw>?	NV\LemFH[myxY3vzJIdtcW:vYTDj[YxtKG2rZ4LheIlwdiCjbnSgbY53[XOrdnWg[5Jwf3SqIIDheJRmem5?	NGfVWng9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nki0PFUzPCd-Mk[4OFg2OjR:L3G+
SF126	MUHGeY5kfGmxbjDhd5NigQ>?	MVixNk42KM7:TR?=		M2rmcGROW09?	M13hcoJtd2OtczDncIlwdWFiY3XscEBucWe{YYTpc44h[W6mIHnueoF{cX[nIHfyc5d1cCCyYYT0[ZJv	MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh2OEWyOEc,OjZ6NEi1NlQ9N2F-
GTL16	MY\GeY5kfGmxbjDhd5NigQ>?		M1\OVFMxKG2rboO=		NVLhSVhMUW6qaXLpeIlwdiCxZjDN[ZQheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJGdVVDF4IHPlcIx{KGGodHXyJFMxKG2rboOsJGlEPTBiPTCwMlAzKM7:TT6=	NYTKNnZORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmyOlA4OTFpPkG5NlYxPzFzPD;hQi=>
GTL16	NVvvOoVwSW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		MUC3NkBpenN?		MomyRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDN[ZQu\GWyZX7k[Y51KGi3bXHuJGdVVDF4IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFNiYYPzZZktKEmFNUCgQUAxNjFizszNMi=>	MlziQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl{NkC3NVEoRjF7Mk[wO\|EyRC:jPh?=
NCI-H1993	NGf6PWFCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		NHPhUoc4OiCqcoO=		MmnmRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDN[ZQu\GWyZX7k[Y51KGi3bXHuJG5EUS2KMUm5N{Bk\WyuczDh[pRmeiB5MjDodpMh[nliTWTTJIF{e2G7LDDJR\|UxKD1iMD6xOUDPxE1w	NH3TNmk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUK2NFcyOSd-MUmyOlA4OTF:L3G+
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MGHU3	MYfBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		Mnn3O\|IhcHK\|		MYXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2JSGWzJINmdGy\|IHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1\XJvR3zvJIF{e2G7	M2q1Z\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{C5OlcyLz5\|MEOwPVY4OTxxYU6=
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... 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	N/A

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38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