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Mcl-1 inhibitor 3

CAS No. : 2376774-73-9

MCE 站：Mcl-1 inhibitor 3

产品活性：Mcl-1 inhibitor 3，化合物 1，是一种高效且可口服活化的大环 Mcl-1 抑制剂 (在 OPM-2 细胞活力测定中，K_i = 0.061 nM；IC₅₀=19 nM)。 Mcl-1 inhibitor 3 具有良好的药代动力学特性和出色的体内功效，且无毒性。

研究领域：Apoptosis

作用靶点：Bcl-2 Family

In Vitro: Mcl-1 inhibitor 3 shows an IC₅₀ value of 19 nM in an OPM-2 cell viability assay, and a K_i value of 0.061 nM in Mcl-1 HTRF/TR-FRET assay.

In Vivo: Mcl-1 inhibitor 3 (oral administration; 3, 10, or 30 mg/kg; 6 hours) causes a significant loss of luminescence (?40%) over vehicle at 30 mg/kg,This effect was observed with unbound drug levels in plasma, the [plasma]_u/OPM-2 IC₅₀ values are 0.24, 0.93 and 3.65 μM in 3, 10, 30 mg/kg doses,respectively.
Mcl-1 inhibitor 3 (oral administration; 10, 30, or 60 mg/kg; 6 hours) activates Bak by 8-fold at 30 mg/kg and by 14-fold at 60 mg/kg in this OPM-2 Luc assay,this test is based on the detection of activated Bak in nude mice subcutaneously injected with via electrochemiluminescence..
Mcl-1 inhibitor 3 (oral administration; 10, 30, or 60 mg/kg; 30 days) led to a robust dose-dependent tumor growth inhibition at 30 mg/kg (44% TGI) and 34% tumor regression when the animals were dosed at 60 mg/kg.Lastly, no body weight loss is observed in any of the mice in this study efficacy models.

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