Mcl-1 inhibitor 6

产品编号 T40230Cas号 2598978-56-2

Mcl-1 inhibitor 6 is a potent, orally active chemical compound that selectively inhibits the myeloid cell leukemia 1 (Mcl-1) protein, with a high affinity (K d = 0.23 nM) and binding activity (K i = 0.02 μM). This compound exhibits exceptional selectivity over other members of the Bcl-2 family, including Bcl-2, Bcl2A1, Bcl-xL, and Bcl-w (K d >10 μM). Notably, Mcl-1 inhibitor 6 demonstrates strong antitumor activity.

Mcl-1 inhibitor 6

产品编号 T40230Cas号 2598978-56-2

规格	价格	库存	数量
2 mg	¥ 1,290	5日内发货
5 mg	¥ 2,430	5日内发货

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生物活性

产品描述	Mcl-1 inhibitor 6 is a potent, orally active chemical compound that selectively inhibits the myeloid cell leukemia 1 (Mcl-1) protein, with a high affinity (K d = 0.23 nM) and binding activity (K i = 0.02 μM). This compound exhibits exceptional selectivity over other members of the Bcl-2 family, including Bcl-2, Bcl2A1, Bcl-xL, and Bcl-w (K d >10 μM). Notably, Mcl-1 inhibitor 6 demonstrates strong antitumor activity.
靶点活性	BCL2A1:>10 μM (Kd), BCL-W:>10 μM (Kd), BCL-XL:>10 μM (Kd), BCL2:>10 μM (Kd), BCL2:10 μM (Ki), Bfl-1:1.57 μM (Ki), MCL1:0.02 μM (Ki), MCL1:0.23 nM (Kd)
体外活性	Mcl-1 inhibitor 6 has K i s 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; IC 50 =0.36-3.02 μM). Mcl-1 inhibitor 6 shows ideal selectivity against CML cell line K562 (IC 50 >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.
体内活性	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 T 1/2 of 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 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.