PHA-665752 - CAS:477575-56-7

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PHA-665752

目录号 : KM6053 CAS No. : 477575-56-7 纯度 : 98%

Data Sheet 产品使用指南

PHA-665752 是一种选择性的 ATP 竞争活性位点 c-Met 激酶抑制剂，K_i 为 4 nM，IC₅₀为 9 nM。PHA-665752 对 c-Met 的选择性比一组不同的酪氨酸和丝氨酸苏氨酸激酶高 50 倍。PHA-665752 诱导细胞凋亡和细胞周期阻滞，具有细胞还原性抗肿瘤活性。

规格	价格	是否有货
10mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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生物活性

PHA-665752 is a selective, ATP-competitive, and active-site inhibitor of the catalytic activity of c-Met kinase (K_i=4 nM; IC₅₀=9 nM). PHA-665752 exhibits >50-fold selectivity for c-Met compared with a panel of diverse tyrosine and serine-threonine kinases. PHA-665752 induces apoptosis and cell cycle arrest, and exhibits cytoreductive antitumor activity.

IC₅₀&Target

Ki: 4 nM
IC50: 9 nM (c-Met)

体外研究

PHA-665752 is a potent and ATP-competitive inhibitor of c-Met kinase activity with a K_i of 4 nM and an IC₅₀ of 9 nM.
PHA-665752 exhibits >50-fold selectivity for c-Met enzyme compared with the majority of kinases evaluated.
PHA-665752 shows potent inhibition of c-Met RTK autophosphorylation in NIH3T3 cells engineered to express high levels of c-Met and hepatocyte growth factor (HGF).
PHA-665752 inhibits HGF-stimulated or constitutive phosphorylation of mediators of downstream of c-Met such as Gab-1, ERK, Akt, STAT3, PLC-γ, and FAK in multiple tumor cell lines.
PHA-665752 (0-1.25 μM; 18 hours) potently inhibits HGF and c-Met-driven phenotypes such as cell growth (proliferation and survival), cell motility, invasion, and/or morphology of a variety of tumor cells.
PHA-665752 (0-1.25 μM; 72 hours) induces apoptosis in both the presence and absence of HGF at concentrations that inhibited tyrosine phosphorylation of c-Met in GTL-16 cells.
PHA-665752 (0.0125-0.2 μM; 4 hours) potent inhibits HGF-induced c-Met phosphorylation in A549 cells.

Cell Proliferation Assay

Cell Line:	S114 cells, GTL-16 cells, NCI-H441 cells, or BxPC-3 cells
Concentration:	0 μM, 0.002 μM, 0.01 μM, 0.05 μM, 0.25 μM, 1.25 μM
Incubation Time:	18 hours
Result:	Potently inhibited HGF and c-Met-driven cell growth.

Apoptosis Analysis

Cell Line:	GTL-16 cells
Concentration:	0 μM, 0.002 μM, 0.01 μM, 0.05 μM, 0.25 μM, 1.25 μM
Incubation Time:	72 hours
Result:	Induced apoptosis in both the presence and absence of HGF at concentrations that inhibited tyrosine phosphorylation of c-Met in GTL-16 cells. Immunoblot Analysis.

Western Blot Analysis

Cell Line:	A549 cells
Concentration:	0.0125 μM, 0.025 μM,0.05 μM,0.1 μM,0.2 μM
Incubation Time:	4 hours
Result:	Potent inhibited HGF-induced c-Met phosphorylation in A549 cells.

体内研究

PHA-665752 (7.5-30 mg/kg/day; i.v. ; for 9 days) exhibits statistically significant dose-dependent tumor growth inhibition of 68%, 39%, and 20% of vehicle control at the 30 mg/kg/day, 15 mg/kg/day, and 7.5 mg/kg/day doses, respectively.
PHA-665752 shows a potent cytoreductive activity in a gastric carcinoma xenograft model.

Animal Model:	Female athymic mice (nu/nu, 8–12 weeks) bearing S114 or GTL-16 tumor xenografts
Dosage:	7.5 mg/kg/day, 15 mg/kg/day, 30 mg/kg/day
Administration:	Intravenous injection; for 9 days
Result:	Demonstrated statistically significant dose-dependent tumor growth inhibition.

分子式

C₃₂H₃₄Cl₂N₄O₄S

分子量

641.61

CAS号

477575-56-7

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	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 50 mg/mL (77.93 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5586 mL	7.7929 mL	15.5858 mL
5 mM	0.3117 mL	1.5586 mL	3.1172 mL
10 mM	0.1559 mL	0.7793 mL	1.5586 mL

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, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

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

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (3.90 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (3.90 mM，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；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (3.90 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (3.90 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
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。

科研文献

纯度： 98%

Data Sheet

产品使用指南

暂无相关参考文献

The molarity calculator equation

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

质量

浓度

体积

分子量*

重置计算

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

重置计算

动物实验计算换算器

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，请联系客服为您提供正确的澄清溶液配方）

% DMSO

% Tween 80

% ddH₂O

% DMSO

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，请先联系客服）；

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。

配置后的溶液总体积：

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。

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KKL 顾客使用本产品发表的 9 篇科研文献

The molarity calculator equation

The dilution calculator equation

动物实验计算换算器