MAP855 | whatman (沃特曼)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

MAP855

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。

MAP855 Chemical Structure

CAS No. : 1660107-77-6

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生物活性

MAP855 is a highly potent, selective, ATP-competitive and orally active MEK1/2 kinase inhibitor (MEK1 ERK2 cascade IC₅₀=3 nM, pERK EC₅₀=5 nM). MAP855 shows equipotent inhibition of wild-type and mutant MEK1/2^[1].

IC₅₀ & Target

ERK

5 nM (EC₅₀)

MEK1

3 nM (IC₅₀)

体外研究
(In Vitro)

MAP855 (compound 30) has single-digit nM inhibition of pERK and proliferation in A375 cells (pERK EC₅₀=5 nM)^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line:	A375 cells^[1]
Concentration:	0-10 nM
Incubation Time:	72 hours
Result:	Showed single-digit nM inhibition of pERK and proliferation in A375 cells (pERK EC₅₀=5 nM).

体内研究
(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^[1].
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^[1].
Pharmacokinetic Parameters of MAP855 in mouse, rat and dog^[1].

	mouse	rat	dog
CL [mL/min*kg]	32	35	22
V_ss [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

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Wistar Rats^[1]
Dosage:	3 mg/kg for i.v., 10 mg/kg for p.o.
Administration:	i.v. and p.o., single
Result:	Showed good oral bioavailability and medium clearance.

Animal Model:	A375 Tumor Bearing Mice^[1]
Dosage:	30 mg/kg
Administration:	p.o., b.i.d, 14 days
Result:	Achieved comparable efficacy to trametinib dosed at the mouse MTD without any body weight loss.

分子量

564.97

Formula

C₂₈H₂₃ClF₂N₆O₃

CAS 号

1660107-77-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. Poddutoori R, et al. Discovery of MAP855, an Efficacious and Selective MEK1/2 Inhibitor with an ATP-Competitive Mode of Action. J Med Chem. 2022;65(5):4350-4366.

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