Mcl-1 inhibitor 6|cas:2598978-56-2|西域试剂

Mcl-1 inhibitor 6,98.40%

产品编号：Bellancom-132307| CAS NO：2598978-56-2| 分子式：C₂₆H₂₈ClNO₆S| 分子量：518.02

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货号	价格	库存与货期
Bellancom-132307	￥2700.00	杭州北京（现货）
Bellancom-132307	￥4050.00	杭州北京（现货）
Bellancom-132307	￥8550.00	杭州北京（现货）
Bellancom-132307	￥13500.00	杭州北京（现货）

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Mcl-1 inhibitor 6

产品介绍

Mcl-1 inhibitor 6 是一种口服有效的，选择性的骨髓细胞白血病 1 (Mcl-1) 蛋白抑制剂，K_d 值为 0.23 nM，K_i 值为 0.02 μM。Mcl-1 inhibitor 6 对 Mcl-1 的选择性高于其他 Bcl-2 家族成员 (Bcl-2、Bcl2A1、Bcl-xL 和 Bcl-w，K_d>10 μM)。Mcl-1 inhibitor 6 是一种有效的抗肿瘤剂。

生物活性

Mcl-1 inhibitor 6 is an orally active, selective myeloid cell leukemia 1 (Mcl-1) protein inhibitor with a K_d of 0.23 nM and a K_i of 0.02 μM. Mcl-1 inhibitor 6 possesses superior selectivity over other Bcl-2 family members (Bcl-2, Bcl2A1, Bcl-xL, and Bcl-w, K_d>10 μM). Mcl-1 inhibitor 6 is a potent antitumor agent.

体外研究

Mcl-1 inhibitor 6 has K_is of 10 μM and 1.57μM for Bcl-2 and Bfl-1, respectively.
Mcl-1 inhibitor 6 (1, 5 μM; for 48 h) significantly induces apoptosis in a concentration-dependent manner.
Mcl-1 inhibitor 6 (0.1, 5 μM; for 4 h) remarkably upregulates PARP cleavage in H929 cells in a concentration-dependent manner.
Mcl-1 inhibitor 6 (for 72 h) shows antiproliferative activities against the tumor cell lines (H929, MV4-11, SK-BR-3, NCI-H23; IC₅₀=0.36-3.02 μM). Mcl-1 inhibitor 6 shows ideal selectivity against CML cell line K562 (IC₅₀>30 μM).

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

Apoptosis Analysis

Cell Line:	H929 cells
Concentration:	1, 5 μM
Incubation Time:	For 48 hours
Result:	Significantly induced apoptosis in a concentration-dependent manner.

Western Blot Analysis

Cell Line:	H929 cells
Concentration:	0.1, 0.5, 1, 5 μM
Incubation Time:	For 4 hours
Result:	Remarkably upregulated PARP cleavage in H929 cells in a concentration-dependent manner.

体内研究
(In Vivo)

Mcl-1 inhibitor 6 (compound 40; 60 mg/kg with PO or 20 mg/kg with IP; every two days for 14 days) shows desired in vivo tumor growth inhibition activity.
Mcl-1 inhibitor 6 (3 mg/kg with IV or 10 mg/kg with PO) has a T_1/2 of 2.3 hours, a CL of 15.18 mL/min•kg by IV.

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

Animal Model:	Balb/c nude female mice (7 weeks) loaded with MV4-11 xenografts
Dosage:	60 mg/kg (PO) or 20 mg/kg (IP)
Administration:	IP or PO; every two days for 14 days
Result:	Showed desired in vivo tumor growth inhibition activity (T/C = 37.30% and 5.52% by po and ip administration, respectively).

Animal Model:	SD rats (200-250 g)
Dosage:	3 mg/kg (IV) or 10 mg/kg (PO) (Pharmacokinetic Analysis)
Administration:	IV or PO
Result:	Had a T_1/2 of 2.3 hours, a CL of 15.18 mL/min•kg by IV. Had a T_1/2 of 2.1 hours, a CL of 36.8 mL/min•kg and a C_max of 2012.95 ng/mL.

体内研究

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

Animal Model:	Balb/c nude female mice (7 weeks) loaded with MV4-11 xenografts
Dosage:	60 mg/kg (PO) or 20 mg/kg (IP)
Administration:	IP or PO; every two days for 14 days
Result:	Showed desired in vivo tumor growth inhibition activity (T/C = 37.30% and 5.52% by po and ip administration, respectively).

Animal Model:	SD rats (200-250 g)
Dosage:	3 mg/kg (IV) or 10 mg/kg (PO) (Pharmacokinetic Analysis)
Administration:	IV or PO
Result:	Had a T_1/2 of 2.3 hours, a CL of 15.18 mL/min•kg by IV. Had a T_1/2 of 2.1 hours, a CL of 36.8 mL/min•kg and a C_max of 2012.95 ng/mL.

体内研究

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

Animal Model:	Balb/c nude female mice (7 weeks) loaded with MV4-11 xenografts
Dosage:	60 mg/kg (PO) or 20 mg/kg (IP)
Administration:	IP or PO; every two days for 14 days
Result:	Showed desired in vivo tumor growth inhibition activity (T/C = 37.30% and 5.52% by po and ip administration, respectively).

Animal Model:	SD rats (200-250 g)
Dosage:	3 mg/kg (IV) or 10 mg/kg (PO) (Pharmacokinetic Analysis)
Administration:	IV or PO
Result:	Had a T_1/2 of 2.3 hours, a CL of 15.18 mL/min•kg by IV. Had a T_1/2 of 2.1 hours, a CL of 36.8 mL/min•kg and a C_max of 2012.95 ng/mL.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (193.04 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	1.9304 mL	9.6521 mL	19.3043 mL
5 mM	0.3861 mL	1.9304 mL	3.8609 mL
10 mM	0.1930 mL	0.9652 mL	1.9304 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