BMS-906024|cas:1401066-79-2|西域试剂

BMS-906024,98.10%

产品编号：Bellancom-15670| CAS NO：1401066-79-2| 分子式：C₂₆H₂₆F₆N₄O₃| 分子量：556.50

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-15670		￥14500.00	杭州北京（现货）

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BMS-906024

产品介绍

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 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.

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

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
(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.

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

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 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.

体内研究

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

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 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.

体内研究

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

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 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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 9.5 mg/mL (17.07 mM; ultrasonic and warming and heat to 60°C)

配制储备液

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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式