MK 2206
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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Chemical Information
| Name | MK 2206 |
|---|---|
| Iupac Chemical Name | 8-(4-(1-aminocyclobutyl)phenyl)-9-phenyl-8,9-dihydro-[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3(2H)-one dihydrochloride |
| Synonyms | MK-2206; MK2206; MK 2206; MK-2206 dihydrochloride; MK-2206 dihydrochloride; MK2206 dihydrochloride; MK 2206 dihydrochloride; MK2206 hydrochloride. |
| Molecular Formula | C25H23Cl2N5O |
| Molecular Weight | 480.39 |
| 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 |
| InChi | InChI=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) |
| CAS Number | 1032350-13-2 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Yellow solid powder |
|---|---|
| Purity | 98% |
| Storage | 3 years -20ºCpowder |
| Solubility | Soluble in DMSO |
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Chemical Structure
