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BMS-536924
目录号: PC16005 纯度: ≥98%
CAS No. :468740-43-4
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中文名称
BMS-536924
中文别名
胰岛素样生长因子-1 受体拮抗剂
英文名称
BMS-536924
英文别名
4-[[(2S)-2-(3-Chlorophenyl)-2-hydroxyethyl]amino]-3-[7-methyl-5-(4-morpholinyl)-1H-benzimidazol-2-yl]-2(1H)-pyridinone;BMS-536924;(S)-4-[2-(3-Chloro-phenyl)-2-hydroxy-ethylamino]-3-(4-methyl-6-morpholin-4-yl-1H-benzoimidazol-2-yl)-1H-pyridin-2-one;BMS 536924;BMS-536924 (BMS536924, BMS 536924);CDK inhibitor;CHEMBL401930;INSULIN-LIKE GROWTH FACTOR-1 RECEPTOR INHIBITOR
Cas No.
468740-43-4
分子式
C25H26N5O3Cl
分子量
479.96
包装储存
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
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.

性状

Solid

IC50 & Target[1][2]

IC50: 100 nM (IGF-1R) and 73 nM (IR)

体外研究(In Vitro)

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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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(In Vivo)

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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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.
运输条件

Room temperature or refrigerated transportation.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
参考文献
溶解度数据
体外研究: 

DMSO : 10 mg/mL (20.84 mM; ultrasonic and warming and heat to 60°C)

配制储备溶液
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
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,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,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

    建议依照次序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 3.75 mg/mL (7.81 mM); Clear solution

    此方案可获得 ≥ 3.75 mg/mL (7.81 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 37.5 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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH?O 中,得到澄清透明的生理盐水溶液
  • 2.

    建议依照次序添加每种溶剂: 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.

    建议依照次序添加每种溶剂: 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。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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