Network Version
Product Name: | A-443654 | |
---|---|---|
CAS No.: | 552325-16-3 | |
Cat. No.: | HY-10425 | |
MWt: | 397.47 | |
Formula: | C24H23N5O | |
Purity : | >98% | |
Solubility: | DMSO : ≥ 100 mg/mL (251.59 mM) | |
Mechanisms: | Target: Cancer | |
Biological Activity: | ||
A-443654 is a pan-Akt inhibitor and has equal potency against Akt1, Akt2, or Akt3 within cells (Ki=160 pM)[1]. IC50 & Target: Ki: 160 pM (Akt1) In Vitro: A-443654 exhibits a Ki of 160 pM, a 30,000-fold improvement in potency versus the initial lead molecule. A-443654 is 40-fold selective for Akt over PKA. A-443654 inhibits Akt1, Akt2, or Akt3 equally within cells. A-443654 reduces the P-GSK3 in a dose-responsive manner in all three cell lines. A-443654 inhibits the proliferation of tumor cells with EC50 of 0.1 μM[1]. A-443654-induced morphological changes occur very rapidly (within 2 to 4 h) in both 10A and 10CA1a cells, with 10CA1a cells more sensitive to A-443654 than the 10A cells. A-443654 alone at 2 μM causes the 10CA1a cells, but not the 10A cells, to detach from the plate after 12 h, whereas 1 μM of A-443654 causes 10CA1a cells to detach from the plate after 12 h. FACScan Analysis of rapamycin and A-443654 effects on DNA content in 10A and 10CA1a cells. In contrast, A-443654 at 2 and 5 μM decreases Bcl-2 levels by 30 to 40% in the 10CA1a cells at 8h. The combination of rapamycin with 2 or 5 μM A-443654, however, markedly decreases Bcl-2 protein levels by appr 40 to 50% in the 10A cells and by appr 70% in the 10CA1a cells, respectively[2]. A-443654 demonstrates the greatest selective effect on the mutant cells compared to the WT cells with greater than 3.5 fold relative growth inhibition of the mutant cells[3]. In Vivo: A-443654 (7.5 mg/kg/d, s.c.) inhibits tumor growth in the 3T3-Akt1 flank tumor model. A-443654 (50 mg/kg, s.c.) induces apoptosis in 3T3-Akt1 flank tumors. A-443654 (30 mg/kg, s.c.) leads to increased levels of phosphorylated Akt1 in MiaPaCa-2 tumors[1]. |
1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA
Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Web:www.medchemexpress.com
Keywords: buy A-443654 | A-443654 Supplier | purchase A-443654 | A-443654 cost | A-443654 manufacturer | order A-443654 | A-443654 distributor | A-443654 structure buy 552325-16-3 | 552325-16-3 Supplier | purchase 552325-16-3 | 552325-16-3 cost | 552325-16-3 manufacturer | order 552325-16-3 | 552325-16-3 distributor | 552325-16-3 structure