BMS 777607 (Synonyms: BMS 817378)

目录号: HY-12076 纯度: 99.33%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

BMS 777607 (BMS 817378) 是一种 Met-related 抑制剂，能够抑制 c-Met，Axl，Ron 和 Tyro3 的活性，IC₅₀ 值为 3.9 nM，1.1 nM，1.8 nM 和 4.3 nM。

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BMS 777607 Chemical Structure

CAS No. : 1025720-94-8

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥950	In-stock
1 mg	￥336	In-stock
5 mg	￥840	In-stock
10 mg	￥1440	In-stock
50 mg	￥4200	In-stock
100 mg	现货	询价
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

MCE 顾客使用本产品发表的 10 篇科研文献

: BMS 777607 purchased from MCE. Usage Cited in: Exp Cell Res. 2019 Aug 1;381(1):50-56. [Abstract]; Western analysis of the effect of BMS-777607 on the expression of osteogenic biomarkers during the osteoblastic differentiation of cultured preosteoblastic cells for 4 days.

: BMS 777607 purchased from MCE. Usage Cited in: Taiwan J Obstet Gynecol. 2019 Jan;58(1):145-152. [Abstract]; Western blot of cell cycle- and mitosis-associated proteins in SKOV3 cells treated with BMS-777607 for 48 h.

: BMS 777607 purchased from MCE. Usage Cited in: Taiwan J Obstet Gynecol. 2019 Jan;58(1):145-152. [Abstract]; Western blot of c-MET signaling-associated proteins of the SKOV3 cells treated with BMS-777607.

BMS 777607 相关产品

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Axl Mer Tyro3

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

BMS 777607 (BMS 817378) is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC₅₀s of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM, respectively, and 40-fold more selective for Met-related targets than Lck, VEGFR-2, and TrkA/B, with more than 500-fold greater selectivity versus all other receptor and non receptor kinases^[1].

IC₅₀ & Target

Axl

Tyro3

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	IC₅₀	> 10 μM Compound: BMS-777607	Cytotoxicity against human A549 cells after 48 hrs by MTT assay Cytotoxicity against human A549 cells after 48 hrs by MTT assay	[PMID: 24900830]
BaF3	IC₅₀	188.4 nM Compound: BMS-777607	Cytotoxicity against mouse BAF3 cells expressing TPR-Met assessed as growth inhibition after 72 hrs Cytotoxicity against mouse BAF3 cells expressing TPR-Met assessed as growth inhibition after 72 hrs	[PMID: 24792774]
DU-145	IC₅₀	200 nM Compound: BMS-777607	Antiinvasive activity in human DU145 cells assessed as inhibition of HGF-induced cell motility preincubated for 1 hr before HGF treatment measured after 24 hrs by cell scattering assay Antiinvasive activity in human DU145 cells assessed as inhibition of HGF-induced cell motility preincubated for 1 hr before HGF treatment measured after 24 hrs by cell scattering assay	[PMID: 24900830]
EBC-1	IC₅₀	162.3 nM Compound: BMS-777607	Antiproliferative activity against human EBC1 cells after 72 hrs by MTT assay Antiproliferative activity against human EBC1 cells after 72 hrs by MTT assay	[PMID: 28412159]
EBC-1	IC₅₀	99.4 nM Compound: BMS-777607	Antiproliferative activity against human EBC1 cells after 72 hrs by SRB assay Antiproliferative activity against human EBC1 cells after 72 hrs by SRB assay	[PMID: 27524312]
GTL 16 cell line	IC₅₀	100 nM Compound: 10, BMS-777607	Antiproliferative activity against Met-dependent human GTL16 cells after 72 hrs by MTS assay Antiproliferative activity against Met-dependent human GTL16 cells after 72 hrs by MTS assay	[PMID: 19260711]
HCC827	IC₅₀	> 10 μM Compound: BMS-777607	Cytotoxicity against human HCC827 cells after 48 hrs by MTT assay Cytotoxicity against human HCC827 cells after 48 hrs by MTT assay	[PMID: 24900830]
HepG2	IC₅₀	> 1000 nM Compound: BMS-777607	Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 28412159]
MKN-45	IC₅₀	285.8 nM Compound: BMS-777607	Cytotoxicity against human MKN45 cells assessed as growth inhibition after 72 hrs Cytotoxicity against human MKN45 cells assessed as growth inhibition after 72 hrs	[PMID: 24792774]
NCI-H1975	IC₅₀	> 10 μM Compound: BMS-777607	Cytotoxicity against human NCI-H1975 cells after 48 hrs by MTT assay Cytotoxicity against human NCI-H1975 cells after 48 hrs by MTT assay	[PMID: 24900830]
NCI-H1993	IC₅₀	1.108 μM Compound: BMS-777607	Cytotoxicity against human NCI-H1993 cells after 48 hrs by MTT assay Cytotoxicity against human NCI-H1993 cells after 48 hrs by MTT assay	[PMID: 24900830]
NCI-H1993	IC₅₀	150 nM Compound: 10, BMS-777607	Antiproliferative activity against Met-dependent human NCI-H1993 cells after 72 hrs by MTS assay Antiproliferative activity against Met-dependent human NCI-H1993 cells after 72 hrs by MTS assay	[PMID: 19260711]
NCI-N87	IC₅₀	> 10000 nM Compound: 10, BMS-777607	Antiproliferative activity against Met-independent human NCI-N87 cells after 72 hrs by MTS assay Antiproliferative activity against Met-independent human NCI-N87 cells after 72 hrs by MTS assay	[PMID: 19260711]
U-87MG ATCC	IC₅₀	160 nM Compound: 10, BMS-777607	Antiproliferative activity against Met-driven human U87 cells after 72 hrs by MTS assay Antiproliferative activity against Met-driven human U87 cells after 72 hrs by MTS assay	[PMID: 19260711]

体外研究
(In Vitro)

BMS 777607 是一种选择性 ATP 竞争性 Met 激酶抑制剂，可有效阻断 c-Met 的自磷酸化，在 GTL-16 细胞裂解物中的 IC₅₀ 为 20 nM，并在 Met 驱动的细胞中表现出选择性增殖抑制作用肿瘤细胞系，如GTL-16细胞系、H1993 和 U87^[1]。BMS 777607 在 PC-3 和 DU145 前列腺癌细胞中抑制肝细胞生长因子 (HGF) 触发的 c-Met 自磷酸化，IC₅₀< 1 nM。BMS 777607 对肿瘤细胞生长几乎没有影响，但对 HGF 诱导的 PC-3 和 DU145 细胞散射具有抑制作用，在 0.5 μM 时几乎完全抑制。BMS 777607 还在两种细胞系中以剂量依赖性方式抑制受刺激的细胞迁移和侵袭 (IC₅₀ < 0.1 μM)^[2]。将 BMS 777607 (约 10 μM) 应用于高转移性小鼠 KHT 细胞 2 小时，有效消除基础水平的自磷酸化 c-Met，IC₅₀ 为 10 nM，而不影响总 c-Met，导致对下游信号分子磷酸化的剂量依赖性抑制，包括 ERK、Akt、p70S6K 和 S6。用 BMS 777607 (约 1 μM) 处理 24 小时，在纳摩尔范围内的剂量下有效抑制 KHT 细胞分散、运动和侵袭，这包括 MET 基因敲低，并适度影响细胞增殖和集落形成^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

口服 BMS 777607 (6.25-50 mg/kg) 可显著减少无胸腺小鼠 GTL-16 人肿瘤异种移植物的肿瘤体积，且未观察到毒性^[1]。BMS 777607 (25 mg/kg/day) 减少了 KHT 肺肿瘤结节的数量 (28.3%)，改善了形态学出血，显著损害了注射的 6-8 周龄雌性 C3H/HeJ 小鼠的转移表型。与对照相比，啮齿动物纤维肉瘤 KHT 细胞没有明显的全身毒性。与对照相比，低剂量的 BMS 777607 (10 mg/kg) 也对肺结节形成产生轻微但不显著的抑制作用^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

512.89

Formula

C₂₅H₁₉ClF₂N₄O₄

CAS 号

1025720-94-8

性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : ≥ 39 mg/mL (76.04 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9497 mL	9.7487 mL	19.4974 mL
5 mM	0.3899 mL	1.9497 mL	3.8995 mL
10 mM	0.1950 mL	0.9749 mL	1.9497 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.87 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.87 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.87 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.33%

选择批次：

Data Sheet (658 KB) SDS (393 KB)

COA (191 KB) HNMR (284 KB) LCMS (96 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Schroeder GM, et al. Discovery of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a selective and orally efficacious inhibitor of the Met kinase superfamily. J Med Chem. 2009 Mar 12;52(5):1251-4. [Content Brief]

[2]. Dai Y, et al. BMS-777607, a small-molecule met kinase inhibitor, suppresses hepatocyte growth factor-stimulated prostate cancer metastatic phenotype in vitro. Mol Cancer Ther, 2010, 9(6), 1554-1561. [Content Brief]

[3]. Dai Y, et al. Impact of the small molecule Met inhibitor BMS-777607 on the metastatic process in a rodent tumor model with constitutive c-Met activation. Clin Exp Metastasis, 2012, 29, 253-261. [Content Brief]

Cell Assay ^[3]	KHT cells are exposed to serial dilution of BMS 777607 for 96 hours, then the MTT assay and trypan blue exclusion are used for the determination of cell proliferation and cell death, respectively. KHT cell colonies are incubated with BMS 777607 for 24 hours and then stained with crystal violet (0.1%) and photographed for the assessment of cell scattering. 2 mm scratch on the confluent KHT cell monolayer is made using a sterilized 1 mL pipette tip followed by treated with BMS 777607 for 24 hours, then the number of cells that have migrated into the denuded area is counted on 4 random fields for the evaluation of cell migration. For the examination of cell invasion, the commercial transwell inserts (8 μM pore membrane) pre-loaded with Matrigel are incubated with serum-free medium in the presence or absence of BMS 777607 at 37°C for 2 hours to allow rehydration of Matrigel. Then cells suspended in serum-free medium are loaded onto the top chamber (5×10³/insert) and complete medium (containing 10% FBS) is used in the lower chamber as a chemoattractant. After incubation for 24 hours, the Matrigel is removed and the inserts are stained with crystal violet. Invaded cells on the underside of the filter are photographed and counted. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	The pharemacokinetics of BMS 777607 are characterized in male Balb/C mice. Two groups of animals (N=6 per group, 20-25 g) are fasted overnight and receive BMS 777607 either as an intravenous (IV) bolus dose (5 mg/kg) via the tail vein or by gavage (10 mg/kg). The mice are fed 6 h after dosing. Blood samples (appr 0.2 mL) are obtained by retro-orbital bleeding at 0.05 (or 0.25 for oral), 0.5, 1, 3, 6, 8 and 24 h post dose. Within each group, half of the animals are bled at 0.05 (or 0.25 for oral), 1, 6 and 24 h, the other half are bled at 0.5, 3, and 8 h, resulting in a composite pharmacokinetic profile (3 mice per time point). Blood samples are allowed to coagulate and centrifuged at 4°C (1500-2000 ×g) to obtain serum. Serum samples are stored at appr 20°C until analysis by LC/MS/MS. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Schroeder GM, et al. Discovery of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a selective and orally efficacious inhibitor of the Met kinase superfamily. J Med Chem. 2009 Mar 12;52(5):1251-4. [Content Brief] [2]. Dai Y, et al. BMS-777607, a small-molecule met kinase inhibitor, suppresses hepatocyte growth factor-stimulated prostate cancer metastatic phenotype in vitro. Mol Cancer Ther, 2010, 9(6), 1554-1561. [Content Brief] [3]. Dai Y, et al. Impact of the small molecule Met inhibitor BMS-777607 on the metastatic process in a rodent tumor model with constitutive c-Met activation. Clin Exp Metastasis, 2012, 29, 253-261. [Content Brief]

BMS 777607 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.9497 mL	9.7487 mL	19.4974 mL	48.7434 mL
	5 mM	0.3899 mL	1.9497 mL	3.8995 mL	9.7487 mL
	10 mM	0.1950 mL	0.9749 mL	1.9497 mL	4.8743 mL
	15 mM	0.1300 mL	0.6499 mL	1.2998 mL	3.2496 mL
	20 mM	0.0975 mL	0.4874 mL	0.9749 mL	2.4372 mL
	25 mM	0.0780 mL	0.3899 mL	0.7799 mL	1.9497 mL
	30 mM	0.0650 mL	0.3250 mL	0.6499 mL	1.6248 mL
	40 mM	0.0487 mL	0.2437 mL	0.4874 mL	1.2186 mL
	50 mM	0.0390 mL	0.1950 mL	0.3899 mL	0.9749 mL
	60 mM	0.0325 mL	0.1625 mL	0.3250 mL	0.8124 mL

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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BMS 7776071025720-94-8BMS 817378BMS777607BMS-777607BMS817378BMS-817378c-Met/HGFRTAM ReceptorTyro3AxlMerInhibitorinhibitorinhibit

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BMS 777607 (Synonyms: BMS 817378)

Customer Review

MCE 顾客使用本产品发表的 10 篇科研文献

BMS 777607 相关产品

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实验参考方法

纯度 & 产品资料

参考文献

摩尔计算器

稀释计算器

BMS 777607 相关分类

完整储备液配制表

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BMS 777607 (Synonyms: BMS 817378)

Customer Review

BMS 777607 相关抗体

MCE 顾客使用本产品发表的 10 篇科研文献

BMS 777607 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 TAM Receptor 亚型特异性产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

BMS 777607 相关抗体:

摩尔计算器

稀释计算器

BMS 777607 相关分类

完整储备液配制表

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