An allosteric Akt inhibitor
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MK-2206 (hydrochloride)

Item No. 11593

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
8-[4-(1-aminocyclobutyl)phenyl]-9-phenyl-1,2,4-triazolo[3,4-f][1,6]naphthyridin-3(2H)-one, dihydrochloride
CAS Number
1032350-13-2
Molecular Formula
C25H21N5O • 2HCl
Formula Weight
480.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 0.2 mg/mlDMF:PBS (pH 7.2)(1:3): 0.2 mg/mlDMSO: 2 mg/ml
λmax
210, 257, 357 nm
SMILES
NC1(CCC1)C(C=C2)=CC=C2C(C(C3=CC=CC=C3)=C4)=NC5=C4C(N6C=C5)=NNC6=O.Cl.Cl
InChi Code
InChI=1S/C25H21N5O.2ClH/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;;/h1-3,5-11,14-15H,4,12-13,26H2,(H,29,31);2*1H
InChi Key
HWUHTJIKQZZBRA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    MK-2206 is an orally active, allosteric Akt inhibitor that is equally potent toward purified human recombinant Akt1 and Akt2 (IC50s = 5 and 12 nM, respectively) and approximately 5-fold less potent against human Akt3 (IC50 = 65 nM).1 In combination with other anticancer agents including topoisomerase inhibitors, antimetabolites, antimicrotubule agents, DNA cross-linkers or growth factor inhibitors, MK-2206 has been shown to synergistically inhibit cell proliferation of human cancer cell lines.1 At 5 μM, MK-2206 significantly enhances apoptosis in hematopoietic cells treated with chemotherapeutics.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    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. Mol. Cancer Ther. 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).