MAP855,1660107-77-6

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MAP855

CAS No. : 1660107-77-6

MCE 国际站：MAP855

产品活性：MAP855 是一种高效、具有选择性且口服有效的 ATP 竞争性 MEK1/2 激酶抑制剂 (MEK1 ERK2 cascade IC₅₀=3 nM, pERK EC₅₀=5 nM)。MAP855 对野生型和突变型 MEK1/2 具有同等的抑制作用。

研究领域：MAPK/ERK Pathway  |  Stem Cell/Wnt

作用靶点：MEK  |  ERK

In Vitro: MAP855 (compound 30) has single-digit nM inhibition of pERK and proliferation in A375 cells (pERK EC₅₀=5 nM).

In Vivo: MAP855 (3 mg/kg for i.v., 10 mg/kg for p.o.; single) has good oral bioavailability and medium clearance in rodents.
MAP855 (30 mg/kg; p.o., b.i.d, 14 days) achieves comparable efficacy to trametinib dosed at the mouse MTD without any body weight loss.
Pharmacokinetic Parameters of MAP855 in mouse, rat and dog.

	mouse	rat	dog
CL [mL/min*kg]	32	35	22
Vss [l/kg]	2.6	2.0	1.8
AUC po d.n. [μM*h]	0.4	0.6	1.4
Oral BAV [% F]	44	65	100

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