BMS-777607

For research use only. Not for use in humans.

目录号:S1561

BMS-777607 Chemical Structure

CAS No. 1025720-94-8

BMS-777607是一种Met相关的抑制剂,作用于c-MetAxlRonTyro3,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。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 2041.38 现货
RMB 976.53 现货
RMB 1706.13 现货
RMB 5498.71 现货
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客户使用Selleck生产的BMS-777607发表文献30篇:

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 BMS-777607是一种Met相关的抑制剂,作用于c-MetAxlRonTyro3,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。
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)
1.1 nM 1.8 nM 3.9 nM 4.3 nM 14 nM
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
GTL-16 Ml\QT4lv[XOnIHHzd4F6 M2LYRWROW09? M4rIO4lvcGmkaYTzJG1mfCCtaX7hd4Uhf2m2aDDJR|UxKG:oIEGwNEBvVQ>? M{PySFE6OjZyN{Gx
H1993 NWfhXoFVT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmDHglExKM7:TR?= M{fIdWROW09? NF3mVIpKSzVyPUG1NEBvVQ>? MXyxPVI3ODdzMR?=
U87 M33xSGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYnB[VBihjFyIN88US=> MmPRSG1UVw>? M13NRmlEPTB;MU[wJI5O M13kRVE6OjZyN{Gx
PC-3 MV;GeY5kfGmxbjDhd5NigQ>? MnfQNE4yKM7:TR?= NXPLSnJbTE2VTx?= MV\lfIhq[mm2czDpcohq[mm2b4L5JIVn\mWldDDvckBJT0ZvaX7keYNm\CClZXzsJJNk[XS2ZYLpcoc> Ml3GNlA2OTV7NEO=
DU145 NFrTTGFHfW6ldHnvckBie3OjeR?= MlvRNE4yKM7:TR?= MXnEUXNQ M1XVb4V5cGmkaYTzJIlvcGmkaYTvdpkh\W[oZXP0JI9vKEiJRj3pcoR2[2WmIHPlcIwhe2OjdITldolv\w>? M4T6NFIxPTF3OUSz
PC-3 MkSwSpVv[3Srb36gZZN{[Xl? NITPdXYxNjBzIN88US=> M4TxUWROW09? Mkntd5VxeHKnc4Pld{BJT0ZvaX7keYNm\CClZXzsJI1q\3KjdHnvci=> M4rs[VIxPTF3OUSz
DU145 NYL0VZo1TnWwY4Tpc44h[XO|YYm= NF7wV3ExNjBzIN88US=> NWO3W3VXTE2VTx?= MlnTd5VxeHKnc4Pld{BJT0ZvaX7keYNm\CClZXzsJI1q\3KjdHnvci=> NVz3W25EOjB3MUW5OFM>
PC-3 MVLGeY5kfGmxbjDhd5NigQ>? MnS2NE4yKM7:TR?= NXPzcVlLTE2VTx?= NEHZU3FqdXCjaYLzJGhITi2vZXTpZZRm\CClZXzsJIlvfmG|aX;u NFWzWYMzODVzNUm0Ny=>
DU145 MYnGeY5kfGmxbjDhd5NigQ>? NX[yeJBPOC5zIN88US=> MX7EUXNQ NFfmPXJqdXCjaYLzJGhITi2vZXTpZZRm\CClZXzsJIlvfmG|aX;u NEP2[nozODVzNUm0Ny=>
PC-3 NXrEWm53T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHXiWJp,OTBizszN M1joRWROW09? MX;y[YR2[2W|IHPlcIwheHKxbHnm[ZJifGmxbh?= MVGyNFUyPTl2Mx?=
KHT Ml;ET4lv[XOnIHHzd4F6 MXrEUXNQ MmT6Zoxw[2u|IITo[UBkNU2ndDDzbYdv[WyrbnegdIF1cHejeTD3bZRpKEmFNUCgc4YhOTBibl2= NWPwXIN4OjJ{OE[1NlM>
KHT M3fzR2Z2dmO2aX;uJIF{e2G7 MXX+NUDPxE1? NEnWSHpFVVOR NIDueIxxemW4ZX70d{B{eG:wdHHu[Y92eyCNSGSgZ4VtdCC|Y3H0eIVzcW6pIIfpeIghUUN3MDDv[kAxNjFvMD61JO69VQ>? MWeyNlI5PjV{Mx?=
KHT Ml3iSpVv[3Srb36gZZN{[Xl? M1;HNZ4xNjVizszN MW\EUXNQ NYHFXoNpcW6qaXLpeJMh[2WubDDtbYdz[XSrb36= MUGyNlI5PjV{Mx?=
KHT NIHBNphHfW6ldHnvckBie3OjeR?= NHHaflR,OC53IN88US=> NV7RdXdPTE2VTx?= NFHHVXpqdmirYnn0d{Bk\WyuIHnueoF{cW:w MmXHNlIzQDZ3MkO=
KHT NXfIRod5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2HFSZ4yOCEQvF2= NIDqUVRFVVOR NH25d3lqdmirYnn0d{BMUFRiY3XscEBxem:uaX\ldoF1cW:w NWriSmxNOjJ{OE[1NlM>
T-47D NX;wNndmT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEizOWV,PSEQvF2= NIPCZ5lFVVOR MVTpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= M1\jVlI{PDZ6NUK5
ZR-75-1 MWjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUT+OUDPxE1? NHvJW5BFVVOR NXyzdGhQcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NHzaWW4zOzR4OEWyPS=>
T-47D NYq3bW9KTnWwY4Tpc44h[XO|YYm= NIDIXXAyOCEQvF2= M{nyUWROW09? M3zqOmlv\HWlZYOgdI9tgXCub3nkfUBjgSB6NjCl M1X4SlI{PDZ6NUK5
ZR-75-1 Mn3tSpVv[3Srb36gZZN{[Xl? NU\OXIh[OTBizszN M3LJcGROW09? NFP2d|dKdmS3Y3XzJJBwdHmybH;p[Jkh[nliOEil MYeyN|Q3QDV{OR?=
T-47D NXzCV3g3TnWwY4Tpc44h[XO|YYm= NGTvXJcyOCEQvF2= NVL5SoI1TE2VTx?= NIrVVXNqdmirYnn0d{BCXVKNLVKg[pVv[3Srb36gZY5lKGmwZIXj[ZMhcXS|IIDyc5RmcW5iZHXndoFl[XSrb36= NUHKVppIOjN2Nki1Nlk>
CHRF M{nxbGZ2dmO2aX;uJIF{e2G7 MWOxNEDPxE1? NXrYWHFYTE2VTx?= MXzpcohq[mm2czDj[YxtKGSrdnnzbY9v MVWyOVMxPDlyMB?=
HPDE NI\POJBHfW6ldHnvckBie3OjeR?= M2nlU|ExKM7:TR?= MYfEUXNQ NEjMcHdjdG:la4OgZ49ve3SrdIX0bZZmKGGldHn2ZZRqd25iYX7kJIRm[3KnYYPl[EBCU1Ric3nncoFtcW6p MWeyOlQ4PzNzNB?=
U118MG NIDWSmdMcW6jc3WgZZN{[Xl? NXXB[WlYhjNizszN NEnkN5pFVVOR M{nMNIJtd2OtczDBXGwheGixc4Doc5J6dGG2aX;u M{LVc|I3QDR6NUK0
SF126 NFrjfXJMcW6jc3WgZZN{[Xl? NEDhd2t,OyEQvF2= NVTtNpA3TE2VTx?= NE\QXVdjdG:la4OgRXhNKHCqb4PwbI9zgWyjdHnvci=> NUHGOG9qOjZ6NEi1NlQ>
U118MG Ml;2R5l1d3irY3n0fUBie3OjeR?= MoD6NVIvPSEQvF2= NGTJWIFFVVOR MnTY[IVkemWjc3XzJIdtcW:vYTDj[YxtKH[rYXLpcIl1gQ>? NEfGUnkzPjh2OEWyOC=>
SF126 NXW0TWNES3m2b4jpZ4l1gSCjc4PhfS=> NGr3WlMyOi53IN88US=> NFjzZoNFVVOR NFHHSJVl\WO{ZXHz[ZMh\2yrb33hJINmdGxidnnhZoltcXS7 NUnoNVZGOjZ6NEi1NlQ>
U118MG NUG3ZpBqSXCxcITvd4l{KGG|c3H5 NFzId5UyOi53IN88US=> M1\CWGROW09? NXm1XFZUcW6mdXPld{BodGmxbXGgZ4VtdCCjcH;weI9{cXN? M{PhZ|I3QDR6NUK0
SF126 NW\2RWZKSXCxcITvd4l{KGG|c3H5 NILWUmIyOi53IN88US=> NUC3ZnlpTE2VTx?= NXvBe|NzcW6mdXPld{BodGmxbXGgZ4VtdCCjcH;weI9{cXN? MoXSNlY5PDh3MkS=
U118MG MorkSpVv[3Srb36gZZN{[Xl? M{PjXFEzNjVizszN MnOxSG1UVw>? MXficI9kc3NiZ3zpc41iKGOnbHygcYloemG2aX;uJIFv\CCrbo\hd4l3\SCpcn;3eIgheGG2dHXyci=> MkLWNlY5PDh3MkS=
SF126 MY\GeY5kfGmxbjDhd5NigQ>? NULSfXVoOTJwNTFOwG0> NELRfIZFVVOR M2CyVIJtd2OtczDncIlwdWFiY3XscEBucWe{YYTpc44h[W6mIHnueoF{cX[nIHfyc5d1cCCyYYT0[ZJv MkP6NlY5PDh3MkS=

... 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     


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     


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     


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]

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)

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37oC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)

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

分子量 512.89
化学式

C25H19ClF2N4O4

CAS号 1025720-94-8
储存条件 粉状
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 g 每只动物给药体积 ul 动物数量
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

计算器

摩尔浓度计算器

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

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

  • 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

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

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

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操作手册

如果有其他问题,请给我们留言。

  • * 必填项

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID