BAP1-IN-1|cas:353495-21-3|西域试剂

BAP1-IN-1,99.52%

产品编号：Bellancom-W327122| CAS NO：353495-21-3| 分子式：C₁₈H₁₆N₂O₂| 分子量：292.33

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-W327122		￥370.00	杭州北京（现货）
Bellancom-W327122		￥590.00	杭州北京（现货）

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BAP1-IN-1

产品介绍

BAP1-IN-1 (Compound 8) 是一种 BRCA1 相关蛋白 1 (BAP1) 催化活性抑制剂，其 IC₅₀ 为 0.1-1μM。

生物活性

BAP1-IN-1 (Compound 8) is a BRCA1 associated protein 1 (BAP1) catalytic activity inhibitor with an IC₅₀ of 0.1-1 μM.

体外研究

BAP1-IN-1 (Compound 8) (1 μM; 30 min) specifically inhibits BAP1 not just in vitro but also within the cellular context.
BAP1-IN-1 (0.1 μM; 24 h) significantly alters 240 genes in BAP1-WT cells, whereas only 33 transcripts are changed in BAP1-KO cells, demonstrating that the gene expression changes mainly depend on the presence of BAP1 protein.
BAP1-IN-1 (0-10 μM; 72 h) selectively inhibits cells with ASXL1 GOF mutations.

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

Western Blot Analysis

Cell Line:	CAL51 cells
Concentration:	1 μM
Incubation Time:	30 min
Result:	Remarkably inhibited BAP1 catalytic activity.

Cell Viability Assay

Cell Line:	THP1, MOML13, K562, THP1-ASXL1-WT and THP1-ASXL1-Y591fs cells
Concentration:	0, 0.1, 0.3, 1, 3 and 10 μM
Incubation Time:	72 h
Result:	K562 cells (ASXL1-Y591^*) were significantly more sensitive to the treatment. Cells with ASXL1fs mutations were ten times more sensitive to the treatment.

体内研究
(In Vivo)

BAP1-IN-1 (Compound 8) (50 mg/kg/d; i.p.; 4 weeks) delays the progression of ASXL1-mutant leukemia and improves survival in mice.

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

Animal Model:	NSGS mice, K562 (ASXL1-WT/Y591^) xenograft model and patient-derived tumor cells (ASXL1-WT/Q588^) model
Dosage:	50 mg/kg/d
Administration:	Intraperitoneal injection, drug treatments were started at day 28 after transplantation
Result:	Significantly delayed progression of disease in both models.

体内研究

BAP1-IN-1 (Compound 8) (50 mg/kg/d; i.p.; 4 weeks) delays the progression of ASXL1-mutant leukemia and improves survival in mice.

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

Animal Model:	NSGS mice, K562 (ASXL1-WT/Y591^) xenograft model and patient-derived tumor cells (ASXL1-WT/Q588^) model
Dosage:	50 mg/kg/d
Administration:	Intraperitoneal injection, drug treatments were started at day 28 after transplantation
Result:	Significantly delayed progression of disease in both models.

体内研究

BAP1-IN-1 (Compound 8) (50 mg/kg/d; i.p.; 4 weeks) delays the progression of ASXL1-mutant leukemia and improves survival in mice.

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

Animal Model:	NSGS mice, K562 (ASXL1-WT/Y591^) xenograft model and patient-derived tumor cells (ASXL1-WT/Q588^) model
Dosage:	50 mg/kg/d
Administration:	Intraperitoneal injection, drug treatments were started at day 28 after transplantation
Result:	Significantly delayed progression of disease in both models.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (171.04 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.4208 mL	17.1040 mL	34.2079 mL
5 mM	0.6842 mL	3.4208 mL	6.8416 mL
10 mM	0.3421 mL	1.7104 mL	3.4208 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 (protect from light)。-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

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

参考文献