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，Kd 值为 0.23 nM，Ki 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，Kd>10 μM)。Mcl-1 inhibitor 6 是一种有效的抗肿瘤剂。
| Cas No. | 2598978-56-2 |
| 分子式 | C26H28ClNO6S |
| 分子量 | 518.02 |
| 溶解度 | DMSO : 100 mg/mL (193.04 mM; ultrasonic and warming and heat to 60°C) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Mcl-1 inhibitor 6 is an orally active, selectivemyeloid cell leukemia 1 (Mcl-1)protein inhibitor with aKdof 0.23 nM and aKiof 0.02 μM. Mcl-1 inhibitor 6 possesses superior selectivity over other Bcl-2 family members (Bcl-2, Bcl2A1, Bcl-xL, and Bcl-w, Kd>10 μM). Mcl-1 inhibitor 6 is a potent antitumor agent[1]. Mcl-1 inhibitor 6 has Kis of 10 μM and 1.57μM for Bcl-2 and Bfl-1, respectively[1].
Mcl-1 inhibitor 6 (1, 5 μM; for 48 h) significantly induces apoptosis in a concentration-dependent manner[1].
Mcl-1 inhibitor 6 (0.1, 5 μM; for 4 h) remarkably upregulates PARP cleavage in H929 cells in a concentration-dependent manner[1].
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)[1].
Apoptosis Analysis[1] | 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[1] | 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. |
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[1].
Mcl-1 inhibitor 6 (3 mg/kg with IV or 10 mg/kg with PO) has a T1/2of 2.3 hours, a CL of 15.18 mL/min•kg by IV[1].
| Animal Model: | Balb/c nude female mice (7 weeks) loaded with MV4-11 xenografts[1] | | 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)[1] | | Dosage: | 3 mg/kg (IV) or 10 mg/kg (PO) (Pharmacokinetic Analysis) | | Administration: | IV or PO | | Result: | Had a T1/2of 2.3 hours, a CL of 15.18 mL/min•kg by IV.
Had a T1/2of 2.1 hours, a CL of 36.8 mL/min•kg and a Cmaxof 2012.95 ng/mL. |
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