AT13148 caused substantial blockade of AKT, p70S6K, PKA, ROCK, and SGK substrate phosphorylation and induced apoptosis in a concentration and time-dependent manner in cancer cells with clinically relevant genetic defects in vitro and in vivo. Antitumor efficacy in HER2-positive, PIK3CA-mutant BT474 breast, PTEN-deficient PC3 human prostate cancer, and PTEN-deficient MES-SA uterine tumor xenografts was shown.Induction of AKT phosphorylation at serine 473 by AT13148, as reported for other ATP-competitive inhibitors of AKT, is not a therapeutically relevant reactivation step.AT13148 has a predominant effect on apoptosis genes, whereas the selective AKT inhibitor CCT128930 modulates cell-cycle genes.
Molecular Weight | 313.78 |
Formula | C17H16ClN3O |
CAS Number | 1056901-62-2 |
Solubility (25°C) | DMSO |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
Related Akt Products |
---|
LY2780301
LY2780301 is an oral dual-target inhibitor of AKT/RSK that binds to and inhibits the activity of Akt, thereby inhibiting the PI3K/Akt signaling pathway, which in turn inhibits cell proliferation and induces apoptosis in tumor cells, and possesses antitumor activity. |
Akt/SKG Substrate Peptide
Akt/SKG Substrate Peptide is a synthetic peptide suitable as a substrate for Akt/PKB, which is not phosphorylated by p70S6K or MAPK1. |
Adropin (34-76) (human, mouse, rat)
Adropin (34-76) (human, mouse, rat) regulates fuel selection preferences in skeletal muscle. |
Apoptin-derived peptide
Apoptin-derived peptide is an antitumor polypeptide with cytotoxicity. |
TAT-TCL1-Akt-in
TAT-TCL1-Akt-in is an Akt inhibitor. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.