A-1331852

产品编号 T6749Cas号 1430844-80-6

别名

A1331852是一种具有口服活性的BCL-XL 选择性抑制剂，Ki 值小于10 pM。它可用于治疗癌症、免疫和自身免疫疾病。

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A-1331852

产品编号 T6749Cas号 1430844-80-6

A1331852是一种具有口服活性的BCL-XL 选择性抑制剂，Ki 值小于10 pM。它可用于治疗癌症、免疫和自身免疫疾病。

规格	价格	库存
1 mg	¥ 348	现货
2 mg	¥ 491	现货
5 mg	¥ 828	现货
10 mg	¥ 1,330	现货
25 mg	¥ 2,820	现货
50 mg	¥ 4,220	现货
100 mg	¥ 5,900	现货
1 mL x 10 mM (in DMSO)	¥ 1,180	现货

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产品介绍

生物活性

产品描述	A-1331852 is a potent and selectiveBCL-XL inhibitor and may be useful in the treatment of cancer, immune and autoimmune diseases.
靶点活性	BCL-XL:0.01 nM (Ki), BCL2:6 nM (Ki), MCL1:142 nM (Ki), BCL-W:4 nM (Ki)
体外活性	A-1331852 在作为单一化合物以及与TKIs联合应用时，对原发性CD34+ CML细胞具有显著的杀伤效力。此外，它能在低纳摩尔浓度下，治疗后最早于1小时内诱导这些细胞发生凋亡，表现出显著的效力[2]。
体内活性	A-1331852在Molt-4异种移植模型中显示了抗肿瘤效果，作为单一化合物诱导肿瘤退缩[1]。
激酶实验	Rabbit or mouse E1 (apper 250 ng) is incubated with 32P-ubiquitin in 1× reaction buffer [50 mM Tris (pH 7.4), 0.2 mM ATP, 0.5 mM MgCl2] at room temperature for 15 min. In some experiments, the His-tagged mouse E1 is bound to TALON cobalt affinity resin before carrying out incubations and reactions. Mouse E1 and 32P-ubiquitin are added to the beads in 1× reaction buffer and incubated as for E1 reactions. Samples are heated in nonreducing SDS-PAGE sample buffer and resolved by SDS-PAGE. Thioesters with ubiquitin are visualized by Storm PhosphoImager.
细胞实验	Immunoprecipitation of BCL-XL is carried out in K562 cells, exposed to A-1331852 (100 nM) for 0-2 h, and the eluted complexes are immunoblotted for the indicated proteins. The input cell lysates and the immunodepleted supernatant (labeled as Flow-through) are immunoblotted to check the efficiency of the immunoprecipitation. (Only for Reference)
动物实验	Mice: The growth inhibition of established tumors in SCID-bg mice is studied. A-1331852 is administered orally daily for 14 days at 25 mg/kg and docetaxel is administered intravenously at 7.5 mg/kg. The change of tumor volume is monitored daily. They are for reference only.

偶联与修饰

抗原信息

存储 & 运输

化学信息

分子量	658.81
分子式	C₃₈H₃₈N₆O₃S
CAS No.	1430844-80-6

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

溶解度信息

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 93 mg/mL (141.2 mM)

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.5179 mL	7.5894 mL	15.1789 mL	75.8944 mL
5 mM	0.3036 mL	1.5179 mL	3.0358 mL	15.1789 mL
10 mM	0.1518 mL	0.7589 mL	1.5179 mL	7.5894 mL
20 mM	0.0759 mL	0.3795 mL	0.7589 mL	3.7947 mL
50 mM	0.0304 mL	0.1518 mL	0.3036 mL	1.5179 mL
100 mM	0.0152 mL	0.0759 mL	0.1518 mL	0.7589 mL