MK-2206 DIHYDROCHLORIDE SALT (2XHCL SALT)

Background Information:

MK-2206 Monohydrochloride (1xHCl salt) is a highly potent, selective
and orally bioactive allosteric Akt inhibitor with IC50 at 8 nM, 5 nM,
and 65 nM for Akt1, Akt2 and Akt3, respectively, currently in clinical
evaluation for cancer treatment. (Chemietek offers two salt forms:
Monohydrochloride (1xHCl salt) (a white to off-white color), the
clinical formulation format being used in clinical studies, and
dihydrochloride (2xHCl salt, yellow powder) (Our Prod No. CT-MK2HCL, Cas
No 1032350-13-2).

Reference:

1. Hirai, H.,Sootome, H.,Nakatsuru, Y., et al. MK-2206, an allosteric
Akt inhibitor, enhances antitumor efficacy by standard chemotherapeutic
agents or molecular targeted drugs in vitro and in vivo. Molecular
Cancer Therapeutics 9(7), 1956-1967 (2010).
2. Kurosu, T.,Nagao, T.,Wu, N., et al. Inhibition of the PI3K/Akt/GSK3
pathway downstream of BCR/ABL, Jak2-V617F, or FLT3-ITD downregulates DNA
damage-induced Chk1 activation as well as G2/M arrest and prominently
enhances induction of apoptosis. PLoS One 8(11), (2013).

APIM050199: MK-2206 DIHYDROCHLORIDE SALT (2XHCL SALT)

CAS No.: 1032350-13-2.
Molecular Formula: C₂₅H₂₁N₅O•2HCl.
Molecular Weight: 482.4 (or refer to Certificate of Analysis, batch-specific).
Purity: >99.5% (HPLC at 214 and 254 nm).
QC: HPLC, ¹HNMR, and Quantitative Elemental Analysis Report.
Solubility: Refer to Certificate of Analysis.
Storage: Refer to Certificate of Analysis.