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PHT-427
Cat No.
CEI-1478
Description
PHT-427 is an inhibitor of Akt and PDPK1 with Ki values of 2.7 μM and 5.2 μM, respectively.
Product Overview
PHT-427 is an inhibitor of Akt and PDPK1 (Ki =2.7 μM and 5.2 μM, respectively). Akt is a serine/threonine-specific protein kinase that plays a vital role in multiple cellular processes including glucose metabolism, apoptosis, cell proliferation, transcription and cell migration etc. In BxPC-3 cells, PHT-427 showed inhibition upon Akt function with IC50 value of 8.6±0.8 μM and for its downstream substrates. PHT-427 reduced the Akt phosphorylation on Ser473 residue and did not decrease total Akt protein level. PHT-427 also inhibited p70S6K and GSK3β in a dose-dependent manner. In SCID (severe combined immunodeficiency) mice of BxPC-3 pancreatic cancer xenografts, administration of PHT-427 exerted prominent antitumor activity that halted tumor growth. PHT-427 in combination with erlotinib exhibited greater than additive antitumor activity in NSC lung cancer and with paclitaxel in breast cancer.
CAS No.
1191951-57-1
Molecular Weight
409.61
Purity
0.98
Storage
Store at -20°C
Targets
Akt; PDPK1
IC50
2.7 μM(Ki); 5.2 μM(Ki)
Molecular Formula
C20H31N3O2S2
Chemical Name
4-dodecyl-N-(1,3,4-thiadiazol-2-yl)benzenesulfonamide
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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