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MK 2206

Catalog No.: 51505
Cas No.: 1032350-13-2
Purity : 98% 
51505 - MK 2206 | CAS 1032350-13-2

Catalog number : 51505

CAS number : 1032350-13-2

分子式 : C25H23Cl2N5O 

分子量 : 480.39 

Iupac 化学名称 : 8-(4-(1-aminocyclobutyl)phenyl)-9-phenyl-8,9-dihydro-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3(2H)-one dihydrochloride 

Smile : O=C1NN=C2C3=CC(C4=CC=CC=C4)C(C5=CC=C(C6(N)CCC6)C=C5)N=C3C=CN21

InChiKey : ATHMWHVQBQZTAB-UHFFFAOYSA-N

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同义词MK-2206; MK2206; MK 2206; MK-2206 dihydrochloride; MK-2206 dihydrochloride; MK2206 dihydrochloride; MK 2206 dihydrochloride; MK2206 hydrochloride. 
英文同义词MK-2206; MK2206; MK 2206; MK-2206 dihydrochloride; MK-2206 dihydrochloride; MK2206 dihydrochloride; MK 2206 dihydrochloride; MK2206 hydrochloride. 
分子式C25H23Cl2N5O 
分子量480.39 
外观Yellow solid powder 
纯度98% 
可溶性Soluble in DMSO 
存储3 years -20ºCpowder 
SmileO=C1NN=C2C3=CC(C4=CC=CC=C4)C(C5=CC=C(C6(N)CCC6)C=C5)N=C3C=CN21
InChiKeyATHMWHVQBQZTAB-UHFFFAOYSA-N
InChiInChI=1S/C25H23N5O/c26-25(12-4-13-25)18-9-7-17(8-10-18)22-19(16-5-2-1-3-6-16)15-20-21(27-22)11-14-30-23(20)28-29-24(30)31/h1-3,5-11,14-15,19,22H,4,12-13,26H2,(H,29,31)
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MK-2206 (Merck, Whitehouse Station, NJ) is an investigational oral allosteric AKT inhibitor (Appendix Fig A1, online only) with nanomolar potency against purified recombinant human AKT1 (half maximal inhibitory concentration [IC50], 5 nmol/L) and AKT2 enzymes (IC50, 12 nmol/L) but lower potency against human AKT3 (IC50, 65 nmol/L). MK-2206 inhibits phosphorylation at both Thr308 and Ser473 residues of AKT and demonstrates greater than 100-fold selectivity for AKT against 256 other kinases.MK-2206 has in vitro and in vivo antitumor activity as a single agent and enhances the preclinical activity of conventional cytotoxics and other molecular targeted therapies. These promising data led to a phase I dose-escalation study of MK-2206 in patients with advanced solid tumors.

 

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