BTSA1|cas:314761-14-3|西域试剂

BTSA1,99.49%

产品编号：Bellancom-123054| CAS NO：314761-14-3| 分子式：C₂₁H₁₄N₆OS₂| 分子量：430.51

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货号	价格	库存与货期
Bellancom-123054	￥1300.00	杭州北京（现货）
Bellancom-123054	￥2080.00	杭州北京（现货）
Bellancom-123054	￥6500.00	杭州北京（现货）
Bellancom-123054	￥10500.00	杭州北京（现货）

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BTSA1

产品介绍

BTSA1 是一种有效的，高亲和力和口服活性的 BAX 激活剂，IC₅₀ 为 250 nM，EC₅₀ 为 144 nM。BTSA1 以高亲和力和特异性与 N 末端激活位点结合，并诱导 BAX 发生构象变化，从而导致 BAX 介导的细胞凋亡。

生物活性

BTSA1 is a potent, high affinity and orally active BAX activator with an IC₅₀ of 250 nM and an EC₅₀ of 144 nM. BTSA1 binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis.

体外研究

BTSA1 (5 μM; 6-24 hours; human AML cell lines) treatment reduced viability of all AML cell lines and displays substantial cell death activity within 6 hours.
BTSA1 (2.5-10 μM; 6 hours; NB4 cells) treatment induces BAX translocation coincided with the release of cytochrome c from the mitochondria to the cytosol. Significant BAX mitochondrial translocation is induced in a BTSA1 dose-dependent manner.
BTSA1 (0.15625-10 μM; 4-24 hours; OCI-AML3 cells) treatment induces dose-dependent caspase-3/7 activation in OCI-AML3 cells. Caspase-3/7 activation is monitored within 4-24 hours and maximal caspase-3/7 activation is detected in 4 hours.

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

Cell Viability Assaysup>

Cell Line:	Human AML cell lines<
Concentration:	5 μM
Incubation Time:	6 hours, 12 hours, 24 hours
Result:	Reduced viability of all AML cell lines. Displayed substantial cell death activity within 6 hours.

Western Blot Analysis

Cell Line:	NB4 cells
Concentration:	2.5 μM, 5 μM, 10 μM
Incubation Time:	6 hours
Result:	Significant BAX mitochondrial translocation was induced in a dose-dependent manner.

Apoptosis Analysis

Cell Line:	OCI-AML3 cells
Concentration:	0.15625 μM, 0.3125 μM, 0.625 μM, 1.25 μM, 2.5 μM, 5 μM, 10 μM
Incubation Time:	4 hours, 6 hours, 8 hours, 12 hours, 24 hours
Result:	Induced dose-dependent caspase-3/7 activation in OCI-AML3 cells. Caspase-3/7 activation was monitored within 4-24 hr and maximal caspase-3/7 activation was detected in 4 hr.

体内研究
(In Vivo)

BTSA1 (10 mg/kg; intraperitoneal injection; every two days; NOD-SCID IL2Rγ null (NSG) mice) treatment significantly increases survival when compared to vehicle-treated mice. BTSA1 treatment induces significant suppression of leukemia growth.

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

Animal Model:	NOD-SCID IL2Rγ null (NSG) mice (6-8 weeks old) with THP-1 cells
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection; every two days
Result:	Significantly increased survival when compared to vehicle-treated mice.

体内研究

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

Animal Model:	NOD-SCID IL2Rγ null (NSG) mice (6-8 weeks old) with THP-1 cells
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection; every two days
Result:	Significantly increased survival when compared to vehicle-treated mice.

体内研究

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

Animal Model:	NOD-SCID IL2Rγ null (NSG) mice (6-8 weeks old) with THP-1 cells
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection; every two days
Result:	Significantly increased survival when compared to vehicle-treated mice.

性状

Solid

溶解性数据

In Vitro:

DMSO : 25 mg/mL (58.07 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3228 mL	11.6141 mL	23.2283 mL
5 mM	0.4646 mL	2.3228 mL	4.6457 mL
10 mM	0.2323 mL	1.1614 mL	2.3228 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