CHIR-124 - CAS:405168-58-3

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CHIR-124

目录号 : KM6881 CAS No. : 405168-58-3 纯度 : 98%

Data Sheet 产品使用指南

CHIR-124 是一种有效的，选择性的 Chk1 抑制剂，IC₅₀ 值为 0.3 nM；同时可有效抑制 PDGFR 和 FLT3，IC₅₀ 值分别为 6.6 nM 和 5.8 nM。

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5mg		In-stock
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

CHIR-124 is a potent and selective Chk1 inhibitor with IC₅₀ of 0.3 nM, and also potently targets PDGFR and FLT3 with IC₅₀s of 6.6 nM and 5.8 nM.

体外研究

CHIR-124 is 500- to 5,000-fold less active against other cell cycle kinases, such as cyclin-dependent kinase 2/cyclin A (0.19 μM), cdc2/cyclin B (0.51 μM), and cyclin-dependent kinase 4/cyclin D (2.1 μM). CHIR-124 (≥0.9 nM) in combination with SN-38 (≥0.42 nM) causes significant synergy or >10% deviation from additivity in human cancer cell lines expressing mutant p53, and these values overlap and fall below the IC₅₀s for SN-38 (1.2×10 M) and CHIR-124 (2.2×10 M), respectively. Moreover, CHIR-124 (100 nM) abrogates the SN-38-induced S and G2-M phase cell cycle checkpoints. CHIR-124 (200 nM) leads to a 2.5-fold elevated level of cdc25A above that of the untreated HCT116 p53 cells. The down-regulation of cdc25A induced by SN-38 is completely restored by concurrent or sequential treatment with CHIR-124, proving that CHIR-124 inhibits the Chk1-mediated destruction of cdc25A in whole cells. CHIR-124 occupies the ATP-binding site, inhibits Chk1 (IC₅₀, 0.3 nM) 2,000-fold more potently than Chk2 (IC₅₀, 0.7 μM).

体内研究

CHIR-124 (10 or 20 mg/kg, p.o.) does not have a significant effect on tumor growth when compared with the vehicle-treated group, but it potentiates the growth inhibitory effect of CPT-11 in a human breast carcinoma xenograft model. The potentiation of the tumor growth inhibitory effect of CPT-11 by CHIR-124 is associated with an increase in apoptosis induction in the tumors. CHIR-124 reverses the suppression of phospho-H3 staining induced by CPT-11, indicating abrogation of the G2-M checkpoint by CHIR-124.

分子式

C₂₃H₂₂N₅OCl

分子量

419.91

CAS号

405168-58-3

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 : 7.14 mg/mL (17.00 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3815 mL	11.9073 mL	23.8146 mL
5 mM	0.4763 mL	2.3815 mL	4.7629 mL
10 mM	0.2381 mL	1.1907 mL	2.3815 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: ≥ 0.71 mg/mL (1.69 mM); Clear solution

此方案可获得 ≥ 0.71 mg/mL (1.69 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 7.1 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: ≥ 0.71 mg/mL (1.69 mM); Clear solution

此方案可获得 ≥ 0.71 mg/mL (1.69 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 7.1 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。