BMS-906024|1401066-79-2|-陌孚医药/Medlife

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BMS-906024

目录号: PL07868 纯度: ≥98%

CAS No. :1401066-79-2

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中文名称	BMS-906024
中文别名	(2R,3S)-N1-[(3S)-2,3-二氢-1-甲基-2-氧代-5-苯基-1H-1,4-苯并二氮杂卓-3-基]-2,3-二(3,3,3-三氟丙基)丁二酰胺
英文名称	BMS-906024
英文别名	Bms-906024;(2S,3R)-N'-[(3S)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]-2,3-bis(3,3,3-trifluoropropyl)butanediamide;(2R,3S)-N1-[(3S)-2,3-Dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-2,3-bis(3,3,3-trifluoropropyl)-butanediamide;BMS 906024;BMS-906024
Cas No.	1401066-79-2
分子式	C₂₆H₂₆F₆N₄O₃
分子量	556.50
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

BMS-906024 是一种口服有效，选择性的 γ 分泌酶 (γ-secretase; gamma secretase) 抑制剂。BMS-906024 是有效的，泛 Notch 受体抑制剂，对 Notch1，-2，-3 和 -4 受体的 IC₅₀ 值分别为 1.6 nM，0.7 nM，3.4 nM 和 2.9 nM。BMS-906024 表现广谱抗肿瘤活性。

生物活性

BMS-906024 is an orally active and selective γ-secretase (gamma secretase) inhibitor. BMS-906024 is a potent pan-Notch receptors inhibitor with IC 50 s of 1.6 nM, 0.7 nM, 3.4 nM, and 2.9 nM for Notch1, -2, -3, and -4 receptors, respectively. BMS-906024 demonstrates broad-spectrum antineoplastic activity.

性状

Solid

IC50 & Target[1][2]

IC50: 1.6 nM (Notch1), 0.7 nM (Notch2), 3.4 nM (Notch3) and 2.9 nM (Notch4)

体外研究(In Vitro)

BMS-906024 (5-100 nM; 72 hours) reduces Notch1 ICD levels in all six lung cancer cell lines. BMS-906024 at 100 nM, has no effect on total Notch1, and down-regulated Hes1 transcript.
In cancer cell proliferation assays, BMS-906024 inhibits both leukemia (TALL-1) and triple-negative breast cancer (MDA-MB-468) cells with IC50 of ～4 nM.
BMS-906024 (100 nM; for 72 hours) enhances the anti-tumor activity of Paclitaxel in vitro.
has not independently confirmed the accuracy of these methods. They are for reference only."

体内研究(In Vivo)

BMS-906024 (8.5 mg/kg; oral gavage; days 1 through 4 of each week for 3 weeks) significantly enhances the tumor growth inhibition of Paclitaxel (36 mg/kg). BMS-906024 enhances Paclitaxel-mediated cytotoxicity in vivo in NSCLC through a combination of inhibiting proliferation and promoting apoptosis, in a p21 and p57-independent manner.
BMS-906024 has a T 1/2 of 4.6/5.3 hours, a C max of 1/0.3 μM and an AUC of 3.4/1.9 μM?hour for IV/PO.
has not independently confirmed the accuracy of these methods. They are for reference only.

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

ClinicalTrial

参考文献

[1]. Morgan KM, et al. Gamma Secretase Inhibition by BMS-906024 Enhances Efficacy of Paclitaxel in Lung Adenocarcinoma. Mol Cancer Ther. 2017 Dec;16(12):2759-2769.
[2]. Gavai AV, et al. Discovery of Clinical Candidate BMS-906024: A Potent Pan-Notch Inhibitor for the Treatment of Leukemia and Solid Tumors. ACS Med Chem Lett. 2015 Mar 11;6(5):523-7.

溶解度数据	In Vitro: DMSO : 9.5 mg/mL (17.07 mM; ultrasonic and warming and heat to 60°C)配制储备液

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产品使用指南

Data Sheet

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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