产品
编 号：F762369
分子式：C28H23ClF2N6O3
分子量：564.97
分子式：C28H23ClF2N6O3
分子量：564.97
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
结构图
CAS No: 1660107-77-6
产品详情
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.
体内研究：
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]323522
Vss [l/kg]2.62.01.8
AUC po d.n. [μM*h]0.40.61.4
Oral BAV [% F]4465100
Animal Model:Male Wistar Rats
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
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.
体外研究：
MAP855 (compound 30) has single-digit nM inhibition of pERK and proliferation in A375 cells (pERK EC50=5 nM).
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.
体内研究：
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]323522
Vss [l/kg]2.62.01.8
AUC po d.n. [μM*h]0.40.61.4
Oral BAV [% F]4465100
Animal Model:Male Wistar Rats
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
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.
体外研究：
MAP855 (compound 30) has single-digit nM inhibition of pERK and proliferation in A375 cells (pERK EC50=5 nM).
产品资料
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