An orally bioavailable and ATP-competitive multi-AGC kinase inhibitor; inhibits Akt1

AT-13148 – 5 mg

Brand:
Cayman
CAS:
1056901-62-2
Storage:
-20
UN-No:
Non-Hazardous - /

AT-13148 is an orally bioavailable and ATP-competitive multi-AGC kinase inhibitor.{38275} It inhibits Akt1, 2, and 3 (IC50s = 38, 402, and 50 nM, respectively), in addition to other AGC kinase family members p70S6K, PKA, ROCK-I, and ROCK-II (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).{38276} Oral administration at a dose of 40 mg/kg reduces motility of 4699 melanoma cells in murine xenograft model.  

 

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Description

An orally bioavailable and ATP-competitive multi-AGC kinase inhibitor; inhibits Akt1, 2, and 3 (IC50s = 38, 402, and 50 nM, respectively); inhibits p70S6K, PKA, and ROCK-I and ROCK-II (IC50s = 3-8 nM); antiproliferative against cancer cell lines with genetic mutations in PI3K-Akt-mTOR or RAS-RAF pathways (GI50s = 1.54-3.77 μM); inhibits growth of MES-SA uterine sarcoma and BT474 breast cancer xenografts in mice (50 mg/kg, p.o.); inhibits ROCK-dependent phosphorylation of MLC2 over a 24-hour period in 4599 mouse melanoma cells (EC50 = 0.1 μM); reduces motility of 4699 melanoma cells in murine xenograft model

Formal name: (αS)-α-(aminomethyl)-α-(4-chlorophenyl)-4-(1H-pyrazol-4-yl)-benzenemethanol

Synonyms: 

Molecular weight: 313.8

CAS: 1056901-62-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|PKA||Product Type|Biochemicals|Kinase Inhibitors|PKB/Akt||Product Type|Biochemicals|Kinase Inhibitors|ROCK||Product Type|Biochemicals|Kinase Inhibitors|S6K||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling|cAMP Signaling||Research Area|Cancer|Cell Signaling|ERK/MAPK Signaling||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling||Research Area|Cancer|Cell Signaling|ROCK Signaling||Research Area|Cell Biology|Cell Signaling|cAMP Signaling||Research Area|Cell Biology|Cell Signaling|PI3K/Akt/mTOR Signaling

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