An allosteric inhibitor of Akt1/2
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BAY-1125976

Item No. 28913

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[4-(1-aminocyclobutyl)phenyl]-3-phenyl-imidazo[1,2-b]pyridazine-6-carboxamide
CAS Number
1402608-02-9
Molecular Formula
C23H21N5O
Formula Weight
383.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5mg/mLDMF:PBS (pH 7.2) (1:3): 0.25mg/mLDMSO: 3mg/mL
λmax
241, 379 nm
SMILES
NC(C(C=C1)=NN2C1=NC(C3=CC=C(C4(N)CCC4)C=C3)=C2C5=CC=CC=C5)=O
InChi Code
InChI=1S/C23H21N5O/c24-22(29)18-11-12-19-26-20(21(28(19)27-18)16-5-2-1-3-6-16)15-7-9-17(10-8-15)23(25)13-4-14-23/h1-3,5-12H,4,13-14,25H2,(H2,24,29)
InChi Key
JBGYKRAZYDNCNV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    10 mg

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    Product Description

    BAY-1125976 is an allosteric inhibitor of Akt1 and -2 (IC50s = 5.2 and 18 nM, respectively, in a time-resolved FRET assay).1 It is selective for Akt1 and -2 over Akt3 (IC50 = 427 nM in the same assay) but does inhibit the activity of the receptor tyrosine kinases FLT1, -3, -4, and Mer by greater than 50% in a panel of 227 kinases at 1 µM. BAY-1125976 inhibits the proliferation of 23 cancer cell lines (IC50s = 0.02-10 µM) and reduces tumor growth in KPL-4, MCF-7, and patient-derived xenograft (PDX) mouse models when administered at a dose of 50 mg/kg per day.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Politz, O., Siegel, F., Bärfacker, L., et al. BAY 1125976, a selective allosteric AKT1/2 inhibitor, exhibits high efficacy on AKT signaling-dependent tumor growth in mouse models. Int. J. Cancer 140(2), 449-459 (2017).