A pan-Akt inhibitor
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Afuresertib (hydrochloride)

Item No. 17988

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl]-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide, monohydrochloride
CAS Number
1047645-82-8
Synonyms
  • GSK2110183B
Molecular Formula
C18H17Cl2FN4OS • HCl
Formula Weight
463.8
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 50 mg/mLDMSO: 30 mg/mLEthanol: 50 mg/mLEthanol:PBS(pH 7.2) (1:1): 0.5 mg/mL
λmax
230, 262 nm
SMILES
FC1=CC=CC(C[C@@H](CN)NC(C2=CC(C3=C(Cl)C=NN3C)=C(Cl)S2)=O)=C1.Cl
InChi Code
InChI=1S/C18H17Cl2FN4OS.ClH/c1-25-16(14(19)9-23-25)13-7-15(27-17(13)20)18(26)24-12(8-22)6-10-3-2-4-11(21)5-10;/h2-5,7,9,12H,6,8,22H2,1H3,(H,24,26);1H/t12-;/m0./s1
InChi Key
YFQJOPFTGMHYNV-YDALLXLXSA-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

    Afuresertib is a pan-Akt inhibitor (IC50s = 0.08, 2, and 2.6 nM for Akt1, -2, and -3, respectively).1 It is selective for Akt over a panel of 13 kinases (IC50s = >100 nM) but does inhibit PKA, PKG1α, and PKG1β (IC50s = 1.3, 0.9, and 4 nM, respectively). Afuresertib (10, 30, and 100 mg/kg) inhibits tumor growth in an SKOV3 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Dumble, M., Crouthamel, M.C., Zhang, S.Y., et al. Discovery of novel AKT inhibitors with enhanced anti-tumor effects in combination with the MEK inhibitor. PLoS One 9(6), e100880 (2014).