BRD0705 - CAS:2056261-41-5

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BRD0705

目录号 : KM5994 CAS No. : 2056261-41-5 纯度 : 98%

Data Sheet 产品使用指南

BRD0705 是一种有效的，具有旁系选择性和口服活性的 GSK3α 抑制剂，IC₅₀ 为 66 nM，K_d 为 4.8 μM。 BRD0705 与 GSK3β (IC₅₀ 为 515 nM) 相比，对 GSK3α 的选择性更高 (8 倍)。BRD0705 可用于急性髓细胞性白血病的研究。

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10mg		In-stock
50mg	询价	In-stock
100mg	询价	In-stock

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生物活性

BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC₅₀ of 66 nM and a K_d of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC₅₀ of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML) research.

体外研究

BRD0705 displays excellent selectivity in a penal of 311 kinases, the CDK family of kinases (CDK2, 3 and 5) are next most potently inhibits at values of 6.87 μM, 9.74 μM and 9.20 μM (87-fold, 123-fold and 116-fold selectivity relative to GSK3α).
BRD0705 (10-40 μM; 2-24 hours; U937 cells) treatment impairs GSK3α Tyr279 phosphorylation in a time-and concentration-dependent manner without affecting GSK3β Tyr216 phosphorylation.
Using a β-catenin dependent TCF/LEF luciferase reporter assay, the absence of β-catenin induced target activation after treatment with BRD0705 in AML cell lines.
BRD0705 impairs AML colony formation in all six tested cell lines, MOLM13, TF-1, U937, MV4-11, HL-60 and NB4, in a concentration-dependent manner, as opposed to BRD3731 which impairs colony formation in TF-1 while increasing colony forming ability in the MV4-11 cell line.

Western Blot Analysis

Cell Line:	U937 cells
Concentration:	10 μM, 20 μM and 40 μM
Incubation Time:	2 hours, 4 hours, 8 hours and 24 hours
Result:	Impaired GSK3α Tyr279 phosphorylation in a time-and concentration-dependent manner without affecting GSK3β Tyr216 phosphorylation.

体内研究

BRD0705 (30 mg/kg; oral gavage; twice daily; NSG mice) treatment impairs leukemia initiation and prolongs survival in AML mouse models.

Animal Model:	8-week-old male NSG mice injected with MLL-AF9 AML cells
Dosage:	30 mg/kg
Administration:	Oral gavage; twice daily
Result:	Mice survival was significantly improved.

分子式

C₁₆H₁₂ClNO₄S

分子量

321.42

CAS号

2056261-41-5

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 : 300 mg/mL (933.36 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.1112 mL	15.5560 mL	31.1119 mL
5 mM	0.6222 mL	3.1112 mL	6.2224 mL
10 mM	0.3111 mL	1.5556 mL	3.1112 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: ≥ 7.5 mg/mL (23.33 mM); Clear solution

此方案可获得 ≥ 7.5 mg/mL (23.33 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 75.0 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: ≥ 7.5 mg/mL (23.33 mM); Clear solution

此方案可获得 ≥ 7.5 mg/mL (23.33 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 75.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。