产品
编 号：F754006
分子式：C26H28ClNO6S
分子量：518.02
分子式：C26H28ClNO6S
分子量：518.02
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
结构图
CAS No: 2598978-56-2
产品详情
生物活性：
Mcl-1 inhibitor 6 is an orally active, selective myeloid cell leukemia 1 (Mcl-1) protein inhibitor with a Kd of 0.23 nM and a Ki 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, Kd>10 μM). Mcl-1 inhibitor 6 is a potent antitumor agent.
体内研究：
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 T1/2 of 2.3 hours, a CL of 15.18 mL/min?kg by IV. 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 T1/2 of 2.3 hours, a CL of 15.18 mL/min?kg by IV. Had a T1/2 of 2.1 hours, a CL of 36.8 mL/min?kg and a Cmax of 2012.95 ng/mL.
体外研究：
Mcl-1 inhibitor 6 has Kis 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).
Mcl-1 inhibitor 6 is an orally active, selective myeloid cell leukemia 1 (Mcl-1) protein inhibitor with a Kd of 0.23 nM and a Ki 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, Kd>10 μM). Mcl-1 inhibitor 6 is a potent antitumor agent.
体内研究：
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 T1/2 of 2.3 hours, a CL of 15.18 mL/min?kg by IV. 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 T1/2 of 2.3 hours, a CL of 15.18 mL/min?kg by IV. Had a T1/2 of 2.1 hours, a CL of 36.8 mL/min?kg and a Cmax of 2012.95 ng/mL.
体外研究：
Mcl-1 inhibitor 6 has Kis 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).
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备