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 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.

Solid

Mcl-1 0.23 nM (Kd) Mcl-1 0.02 μM (Ki)

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

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

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Peng-Ju Zhu, et al. Discovery of 3,5-Dimethyl-4-Sulfonyl-1 H-Pyrrole-Based Myeloid Cell Leukemia 1 Inhibitors with High Affinity, Selectivity, and Oral Bioavailability. J Med Chem. 2021 Aug 12;64(15):11330-11353.

In Vitro: DMSO : 100 mg/mL (193.04 mM; ultrasonic and warming and heat to 60°C)配制储备液