BMS-536924 - CAS:468740-43-4

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BMS-536924

目录号 : KM6183 CAS No. : 468740-43-4 纯度 : 98%

Data Sheet 产品使用指南

BMS-536924 是一种具有口服活性，竞争性和选择性的胰岛素样生长因子受体 (IGF-1R) 激酶和胰岛素受体 (IR) 抑制剂，IC₅₀ 分别为 100 nM 和 73 nM。BMS-536924 具有抗癌活性。

规格	价格	是否有货
5mg		In-stock
10mg		In-stock
50mg		In-stock
100mg	询价	In-stock
200mg	询价	In-stock

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生物活性

BMS-536924 is an orally active, competitive and selective insulin-like growth factor receptor (IGF-1R) kinase and insulin receptor (IR) inhibitor with IC₅₀s of 100 nM and 73 nM, respectively. BMS-536924 has anti-cancer activity.

体外研究

BMS-536924 inhibits FAK and Lck with IC₅₀s of 150 nM and 341 nM, respectively.
BMS-536924 (1 μM; every four days for 12 days) blocks pBabe-MCF10A and CD8-IGF-IR-MCF10A acinar proliferation.
BMS-536924 (0.01-1 μM; 24 hours) inhibits growth of CD8-IGF-IR-MCF10A cells and has an IC₅₀ of 0.48 μM.
BMS-536924 (1 μM; for 4 days) induces apoptosis in CD8-IGF-IR-MCF10A acini.
BMS-536924 (0.1-1 μM; for 24 hours) decreases in S-phase cells and causes a G0/G1 block.
BMS-536924 (1 μM; 10 min, 1, 8, 24, 48 hours) inhibits IGF-IR signaling in pBabe-MCF10A cells and inhibits phosphorylation of CD8-IGF-IR. BMS-536924 time-dependently inhibits AKT phosphorylation.

Cell Proliferation Assay

Cell Line:	pBabe-MCF10A and CD8-IGF-IR-MCF10A acini
Concentration:	1 μM
Incubation Time:	Every four days for 12 days
Result:	Blocked acinar proliferation.

Cell Viability Assay

Cell Line:	CD8-IGF-IR-MCF10A cells
Concentration:	0.01, 0.1, 1 μM
Incubation Time:	24 hours
Result:	Has an IC50 of 0.48 μM.

Apoptosis Analysis

Cell Line:	CD8-IGF-IR-MCF10A acini
Concentration:	1 μM
Incubation Time:	For 4 days
Result:	Resulted in a dramatic induction of apoptosis.

Cell Cycle Analysis

Cell Line:	CD8-IGF-IR-MCF10A cells and pBabe-MCF10A control cells
Concentration:	0.1, 0.5, 1 μM
Incubation Time:	For 24 hours
Result:	Decreased in S-phase cells and caused a G0/G1 block.

Western Blot Analysis

Cell Line:	CD8-IGF-IR-MCF10A cells
Concentration:	1 μM
Incubation Time:	10 min, 1, 8, 24, 48 hours
Result:	Caused maximal inhibition of phosphorylated IGF-IR at 10 min and retained its ability to inhibit IGF-IR phosphorylation for up to 48 hours.

体内研究

BMS-536924 (100 mg/kg; gavage; daily; for 35 days) causes regression of xenografts in vivo and an average reduction of 76% tumor volume after 2 weeks.

Animal Model:	Athymic nude mice with CD8-IGF-IRMCF10A cells
Dosage:	100 mg/kg
Administration:	Gavage; daily; for 35 days
Result:	Caused an average reduction of 76% tumor volume after 2 weeks.

分子式

C₂₅H₂₆N₅O₃Cl

分子量

479.96

CAS号

468740-43-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 50 mg/mL (104.18 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0835 mL	10.4175 mL	20.8351 mL
5 mM	0.4167 mL	2.0835 mL	4.1670 mL
10 mM	0.2084 mL	1.0418 mL	2.0835 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 (5.21 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.21 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 (5.21 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.21 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。
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.25 mg/mL (4.69 mM); Clear solution

此方案可获得 ≥ 2.25 mg/mL (4.69 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 22.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。