CGP77675 - CAS:234772-64-6

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CGP77675

目录号 : KM19834 CAS No. : 234772-64-6 纯度 : ≥98%

Data Sheet SDS 产品使用指南

CGP77675 是一种口服有效的 Src 家族激酶抑制剂。CGP77675 抑制肽底物的磷酸化和纯化 Src 的自磷酸化 (IC₅₀ 分别为 5-20 和 40 nM)，并且还抑制 Src，EGFR，KDR，v-Abl 和 Lck，IC₅₀ 分别为 20、150、1000、310 和 290 nM。具有抗肿瘤活性。

规格	价格	是否有货	数量
5mg		In-stock
10mg		In-stock

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生物活性

CGP77675 is an orally active and potent inhibitor of Src family kinases. CGP77675 inhibits phosphorylation of peptide substrates and autophosphorylation of purified Src (IC₅₀s of 5-20 and 40 nM, respectively), and also inhibits Src, EGFR, KDR, v-Abl, and Lck with IC₅₀s of 5-20, 40, 20, 150, 1000, 310, and 290 nM, respectively. Anticancer activity.

IC₅₀&Target

IC50: 0.02 μM (Src), 0.15 μM (EGFR), 1.0 μM (KDR), 0.31 μM (v-Abl), 0.29 μM (Lck)

体外研究

CGP77675 dose dependently inhibits phosphorylation of poly-Glu-Tyr with an IC₅₀ value of 5.5 nM, and of the optimal Src substrate (OSS) peptide with an IC₅₀ value of 16.7 nM. These IC₅₀ values are similar to the value obtained with chicken Src (20 nM).
CGP77675 inhibits the parathyroid hormone-induced bone resorption in rat fetal long bone cultures with an IC₅₀ of 0.8 μM.
CGP77675 (0.04-10 μM; 2 hours) potently inhibits tyrosine phosphorylation of the Src substrates Fak and paxillin, but has much less effect on Src (IC₅₀ values 0.2, 0.5, and 5.7μM) in IC8.1 cells.

Cell Viability Assay

Cell Line:	MC3T3-E1 cells
Concentration:	0.2, 1, and 5 μM
Incubation Time:	3 days
Result:	Did not influence cell viability for up to 3 days of treatment.

Western Blot Analysis

Cell Line:	Src-overexpressing IC8.1 cells
Concentration:	0.04, 0.2, 1, 5, and 10 μM
Incubation Time:	2 hours
Result:	Dose dependently inhibited phosphorylation of Fak and paxillin, but not of Src.

体内研究

CGP77675 (1, 5, and 25 mg/kg; injected s.c.; twice a day) inhibits IL-1β-induced hypercalcemia in Mice.
CGP77675 (10 and 50 mg/kg; administered orally; twice a day for 6 weeks) partially prevents bone loss and rescues bone microarchitectural features in young ovx rats.

Animal Model:	Male mice (Tif:MAGf; Novartis Animal Farm) of 25-30 g body
Dosage:	1, 5, and 25 mg/kg
Administration:	Injected s.c.; twice a day
Result:	Prevented IL-1β-induced hypercalcemia in mice without affecting serum amyloid protein levels.

Animal Model:	Eight-week-old (175-209 g) female rats of the Sprague-Dawley-derived strain Tif:RAlf
Dosage:	10 and 50 mg/kg
Administration:	Administered orally; twice a day for 6 weeks
Result:	Partly prevented bone loss.

分子式

C₂₆H₂₉N₅O₂

分子量

443.54

CAS号

234772-64-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

纯度： ≥98%

Data Sheet

SDS

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*

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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。

Other Forms of Rapamycin:

KKL 顾客使用本产品发表的 0 篇科研文献

The molarity calculator equation

The dilution calculator equation

动物实验计算换算器