A multi-AGC kinase inhibitor
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AT-13148

Item No. 21597

Technical Information
Formal Name
(αS)-α-(aminomethyl)-α-(4-chlorophenyl)-4-(1H-pyrazol-4-yl)-benzenemethanol
CAS Number
1056901-62-2
Molecular Formula
C17H16ClN3O
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml
λmax
257 nm
SMILES
ClC1=CC=C([C@@](CN)(O)C2=CC=C(C3=CNN=C3)C=C2)C=C1
InChi Code
InChI=1S/C17H16ClN3O/c18-16-7-5-15(6-8-16)17(22,11-19)14-3-1-12(2-4-14)13-9-20-21-10-13/h1-10,22H,11,19H2,(H,20,21)/t17-/m0/s1
InChi Key
IIRWNGPLJQXWFJ-KRWDZBQOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    AT-13148 is an orally bioavailable and ATP-competitive multi-AGC kinase inhibitor.1 It inhibits Akt1, 2, and 3 (IC50s = 38, 402, and 50 nM, respectively), in addition to other AGC kinase family members p70S6K, PKA, ROCK1, and ROCK2 (IC50s = 3-8 nM). AT-13148 inhibits growth of cancer cell lines with genetic mutations in PI3K-Akt-mTOR and RAS-RAF signaling pathways (GI50s = 1.54-3.77 μM). In vivo administration of AT-13148 (50 mg/kg, p.o.) inhibits the growth of MES-SA uterine sarcoma and BT474 breast cancer xenografts in mice by inhibiting Akt and p70S6K kinases. AT-13148 also stably inhibits ROCK-dependent phosphorylation of myosin light chain (MLC2) over a 24-hour period in 4599 mouse melanoma cells (EC50 = 0.1 μM).2 Oral administration at a dose of 40 mg/kg reduces motility of 4699 melanoma cells in murine xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yap, T.A., Walton, M.I., Grimshaw, K.M., et alAT13148 is a novel, oral multi-AGC kinase inhibitor with potent pharmacodynamic and antitumor activity. Clin. Cancer Res. 18(14), 3912-3923 (2012).

    2. Sadok, A., McCarthy, A., Caldwell, J., et alRho kinase inhibitors block melanoma cell migration and inhibit metastasis. Cancer Res. 75(11), 2272-2284 (2015).