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規(guī)格	價格	是否有貨
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	現(xiàn)貨	詢價
200 mg		詢價
500 mg		詢價

MCE 顧客使用本產(chǎn)品發(fā)表的 11 篇科研文獻

•ACS Nano. 2023 Sep 5. [Abstract]
•Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. [Abstract]
•Acta Pharmacol Sin. 2022 Nov 30. [Abstract]
•Liver Int. 2021 Mar 31. [Abstract]
•Cells. 2024 Nov 18;13(22):1902. [Abstract]
•Cancer Res Treat. 2020 Jul;52(3):973-986. [Abstract]

•World J Gastrointest Oncol. 2020 Nov 15;12(11):1216-1236. [Abstract]
•Exp Cell Res. 2019 Aug 1;381(1):50-56. [Abstract]
•Taiwan J Obstet Gynecol. 2019 Jan;58(1):145-152. [Abstract]
•Research Square Preprint. 2020 Jun.
•Harvard Medical School LINCS LIBRARY

WB

: 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 相關(guān)產(chǎn)品

•相關(guān)化合物庫:

•同靶點產(chǎn)品:

•同靶點蛋白產(chǎn)品:

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

細(xì)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]

體外研究
(In Vitro)

BMS 777607 是一種選擇性 ATP 競爭性 Met 激酶抑制劑，可有效阻斷 c-Met 的自磷酸化，在 GTL-16 細(xì)胞裂解物中的 IC₅₀ 為 20 nM，并在 Met 驅(qū)動的細(xì)胞中表現(xiàn)出選擇性增殖抑制作用腫瘤細(xì)胞系，如GTL-16細(xì)胞系、H1993 和 U87^[1]。BMS 777607 在 PC-3 和 DU145 前列腺癌細(xì)胞中抑制肝細(xì)胞生長因子 (HGF) 觸發(fā)的 c-Met 自磷酸化，IC₅₀< 1 nM。BMS 777607 對腫瘤細(xì)胞生長幾乎沒有影響，但對 HGF 誘導(dǎo)的 PC-3 和 DU145 細(xì)胞散射具有抑制作用，在 0.5 μM 時幾乎完全抑制。BMS 777607 還在兩種細(xì)胞系中以劑量依賴性方式抑制受刺激的細(xì)胞遷移和侵襲 (IC₅₀ < 0.1 μM)^[2]。將 BMS 777607 (約 10 μM) 應(yīng)用于高轉(zhuǎn)移性小鼠 KHT 細(xì)胞 2 小時，有效消除基礎(chǔ)水平的自磷酸化 c-Met，IC₅₀ 為 10 nM，而不影響總 c-Met，導(dǎo)致對下游信號分子磷酸化的劑量依賴性抑制，包括 ERK、Akt、p70S6K 和 S6。用 BMS 777607 (約 1 μM) 處理 24 小時，在納摩爾范圍內(nèi)的劑量下有效抑制 KHT 細(xì)胞分散、運動和侵襲，這包括 MET 基因敲低，并適度影響細(xì)胞增殖和集落形成^[3]。

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

體內(nèi)研究
(In Vivo)

口服 BMS 777607 (6.25-50 mg/kg) 可顯著減少無胸腺小鼠 GTL-16 人腫瘤異種移植物的腫瘤體積，且未觀察到毒性^[1]。BMS 777607 (25 mg/kg/day) 減少了 KHT 肺腫瘤結(jié)節(jié)的數(shù)量 (28.3%)，改善了形態(tài)學(xué)出血，顯著損害了注射的 6-8 周齡雌性 C3H/HeJ 小鼠的轉(zhuǎn)移表型。與對照相比，嚙齒動物纖維肉瘤 KHT 細(xì)胞沒有明顯的全身毒性。與對照相比，低劑量的 BMS 777607 (10 mg/kg) 也對肺結(jié)節(jié)形成產(chǎn)生輕微但不顯著的抑制作用^[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 號

1025720-94-8

性狀

固體

顏色

White to off-white

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

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

溶解性數(shù)據(jù)

細(xì)胞實驗：

DMSO 中的溶解度 : ≥ 39 mg/mL (76.04 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲備液

濃度溶劑體積質(zhì)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

查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

摩爾計算器
稀釋計算器

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

濃度 _(start)

C1

×

體積 _(start)

V1

=

濃度 _(final)

C2

×

體積 _(final)

V2

動物實驗：

請根據(jù)您的實驗動物和給藥方式選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

方案一

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.87 mM); 澄清溶液

此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水定容至 1 mL。
生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
方案二

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.87 mM); 澄清溶液

此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液中，混合均勻。
2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
方案三

請依序添加每種溶劑： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.87 mM); 澄清溶液

此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液，此方案實驗周期在半個月以上的動物實驗酌情使用。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中，混合均勻。

動物溶解方案計算器

請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只

由于實驗過程有損耗，建議您多配一只動物的量

請輸入您的動物體內(nèi)配方組成：

%

DMSO +

%

+

%

Tween-80 +

%

Saline

如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。

方案所需 助溶劑 包括：DMSO，，均可在 MCE 網(wǎng)站選購。，Tween 80，均可在 MCE 網(wǎng)站選購。

計算結(jié)果

工作液所需濃度 : mg/mL

儲備液配制方法 : mg 藥物溶于 μL DMSO（母液濃度為 mg/mL）。

您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。

動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。

連續(xù)給藥周期超過半月以上，請謹(jǐn)慎選擇該方案。

請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱（超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。

純度 & 產(chǎn)品資料

純度: 99.33%

選擇批次：

Data Sheet (658 KB) SDS (393 KB)

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

產(chǎn)品使用指南 (1538 KB)

參考文獻

[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.
參考文獻	[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 相關(guān)分類

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

可選溶劑	濃度溶劑體積質(zhì)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

Help & FAQs

Do most proteins show cross-species activity?
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 顧客使用本產(chǎn)品發(fā)表的 11 篇科研文獻

BMS 777607 相關(guān)產(chǎn)品

•相關(guān)化合物庫:

•同靶點產(chǎn)品:

•同靶點蛋白產(chǎn)品:

查看 TAM Receptor 亞型特異性產(chǎn)品:

生物活性

實驗參考方法

純度 & 產(chǎn)品資料

參考文獻

摩爾計算器

稀釋計算器

BMS 777607 相關(guān)分類

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BMS 777607 (Synonyms: BMS 817378)

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BMS 777607 相關(guān)抗體

MCE 顧客使用本產(chǎn)品發(fā)表的 11 篇科研文獻

BMS 777607 相關(guān)產(chǎn)品

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查看 TAM Receptor 亞型特異性產(chǎn)品:

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純度 & 產(chǎn)品資料

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BMS 777607 相關(guān)抗體:

摩爾計算器

稀釋計算器

BMS 777607 相關(guān)分類

完整儲備液配制表

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