MSC2504877 M2912|cas:1460286-21-8|西域试剂

MSC2504877 M2912,98.50%

产品编号：Bellancom-123851| CAS NO：1460286-21-8| 分子式：C₁₇H₁₈N₂O₂| 分子量：282.34

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货号	价格	库存与货期
Bellancom-123851	￥1700.00	杭州北京（现货）
Bellancom-123851	￥2700.00	杭州北京（现货）
Bellancom-123851	￥5265.00	杭州北京（现货）
Bellancom-123851	￥8424.00	杭州北京（现货）
Bellancom-123851	￥13480.00	杭州北京（现货）

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MSC2504877 M2912

产品介绍

MSC2504877 (M2912) 是一种有效的，具有口服活性的 tankyrase 抑制剂，对 TNKS、TNKS2、PARP1 的 IC₅₀ 值分别为 0.0007、0.0008、0.54 µM。MSC2504877 增加 AXIN2 和 TNKS 蛋白的表达水平并降低 β-catenin 蛋白水平。MSC2504877 具有抗肿瘤活性。

生物活性

MSC2504877 (M2912) is a potent and orally active tankyrase inhibitor with IC₅₀s of 0.0007, 0.0008, 0.54 µM for TNKS, TNKS2, PARP1, respectively. MSC2504877 increases the expression of AXIN2 and TNKS protein levels and decreases β-catenin levels. MSC2504877 shows anti-tumor activity.

体外研究

MSC2504877 (1, 3, 10 µM；24 小时) 增加 APC 突变体 COLO320DM 结直肠肿瘤细胞中 AXIN2 和 TNKS 蛋白水平的表达并降低 β-catenin 蛋白水平。
MSC2504877 (0-100 µM；5 天) 抑制 APC^−/− 细胞和 COLO320DM 细胞的存活。
MSC2504877 (1 µM；24 小时) 与 albociclib (HY-50767) (0.03 µM) 联合使用可诱导细胞周期停滞在 G1 期。

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

Western Blot Analysis

Cell Line:	APC mutant COLO320DM colorectal tumour cells
Concentration:	1, 3, 10 µM
Incubation Time:	24 h
Result:	Increased AXIN2 protein levels and decreased β-catenin levels.

体内研究
(In Vivo)

MSC2504877 (30 mg/kg；口服；一次) 抑制小鼠体内的 TNKS 和 Wnt 信号传导。
MSC2504877 (50 mg/kg+palbociclib (HY-50767) 150mg/kg；口服；一次) 抑制体内 Apc 缺陷细胞的过度增殖。

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

Animal Model:	CB17 SCID mice (APC mutant COLO320DM tumour cell xenografts)
Dosage:	30 mg/kg
Administration:	P.o.; once
Result:	Elicited an increase in both TNKS and AXIN2 levels in tumours, peaking at 6–10 hours after drug administration and falling 18 hours after.

Animal Model:	Villin-CreERT2; Apcfl/fl mice
Dosage:	50 mg/kg + palbociclib (150 mg/kg)
Administration:	P.o.; once
Result:	Suppressed the expression of the archetypal Wnt target gene and stem cell marker Lgr5 and combination drug treatment caused a profound increase in nuclear p21.

体内研究

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

Animal Model:	CB17 SCID mice (APC mutant COLO320DM tumour cell xenografts)
Dosage:	30 mg/kg
Administration:	P.o.; once
Result:	Elicited an increase in both TNKS and AXIN2 levels in tumours, peaking at 6–10 hours after drug administration and falling 18 hours after.

Animal Model:	Villin-CreERT2; Apcfl/fl mice
Dosage:	50 mg/kg + palbociclib (150 mg/kg)
Administration:	P.o.; once
Result:	Suppressed the expression of the archetypal Wnt target gene and stem cell marker Lgr5 and combination drug treatment caused a profound increase in nuclear p21.

体内研究

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

Animal Model:	CB17 SCID mice (APC mutant COLO320DM tumour cell xenografts)
Dosage:	30 mg/kg
Administration:	P.o.; once
Result:	Elicited an increase in both TNKS and AXIN2 levels in tumours, peaking at 6–10 hours after drug administration and falling 18 hours after.

Animal Model:	Villin-CreERT2; Apcfl/fl mice
Dosage:	50 mg/kg + palbociclib (150 mg/kg)
Administration:	P.o.; once
Result:	Suppressed the expression of the archetypal Wnt target gene and stem cell marker Lgr5 and combination drug treatment caused a profound increase in nuclear p21.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (442.73 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.5418 mL	17.7091 mL	35.4183 mL
5 mM	0.7084 mL	3.5418 mL	7.0837 mL
10 mM	0.3542 mL	1.7709 mL	3.5418 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