BMS-906024
目录号 : KM11214 CAS No. : 1401066-79-2 纯度 : 98%

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。

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

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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 IC50s 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.

体外研究

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.

Western Blot Analysis

Cell Line: NSCLC cell lines (A549, H358, H1975, H2444, H1792, HCC44)
Concentration: 5, 10, 25, 50, 100 nM
Incubation Time: 72 hours
Result: Reduced Notch1 ICD levels in all six lung cancer cell lines tested at concentrations as low as 5 nM, with maximal depletion at 50-100 nM.
体内研究

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 T1/2 of 4.6/5.3 hours, a Cmax of 1/0.3 μM and an AUC of 3.4/1.9 μM•hour for IV/PO.

Animal Model: Six to 12-week-old female NOD scid gamma (NSG) mice with KRAS- and BRAF-WT PDX-T42 xenografts
Dosage: 8.5 mg/kg
Administration: oral gavage; days 1 through 4 of each week for 3 weeks
Result: Significantly enhanced the tumor growth inhibition of Paclitaxel (36 mg/kg), but had no significant effect on Cisplatin (2 mg/kg) treatment.
Animal Model: Mouse
Dosage: 1 mg/kg (Pharmacokinetic Analysis)
Administration: IV or PO
Result: Had a T1/2 of 4.6/5.3 hours, a Cmax of 1/0.3 μM and an AUC of 3.4/1.9 μM•hour for IV/PO.
分子式
C26H26F6N4O3
分子量
556.50
CAS号
1401066-79-2
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 : 260 mg/mL (467.21 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7969 mL 8.9847 mL 17.9695 mL
5 mM 0.3594 mL 1.7969 mL 3.5939 mL
10 mM 0.1797 mL 0.8985 mL 1.7969 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。

临床试验
科研文献
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