An inhibitor of Akt and PDPK1 (Ki = 2.7 and 5.2 μM

PHT-427 – 5 mg

Brand:
Cayman
CAS:
1191951-57-1
Storage:
-20
UN-No:
Non-Hazardous - /

PHT-427 is an inhibitor of the serine/threonine kinases Akt and phosphoinositide-dependent protein kinase-1 (PDPK1) with Ki values of 2.7 and 5.2 μM, respectively, that selectively binds to the pleckstrin homology binding domain of both kinases.{38927} PHT-427 (10 µM) inhibits PDPK1 and Akt autophosphorylation in BxPC-3 prostate cancer cells. In vivo, PHT-427 (125-250 mg/kg) reduces tumor growth in BxPC-3, Panc-1, MiaPaCa-2, PC3, SK-OV-3, A549, and MCF-7 xenograft mouse models, with up to 80% reduction in growth for those containing PIK3CA mutations. PHT-427 (200 mg/kg) also enhances the antitumor effect of paclitaxel (Item No. 10461) in an MCF-7 breast cancer xenograft mouse model.  

 

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SKU: 24188 - 5 mg Category:

Description

An inhibitor of Akt and PDPK1 (Ki = 2.7 and 5.2 μM, respectively); binds to the pleckstrin homology binding domain; inhibits PDPK1 and Akt autophosphorylation in BxPC-3 prostate cancer cells (10 µM); reduces tumor growth in BxPC-3, Panc-1, MiaPaCa-2, PC3, SK-OV-3, A549, and MCF-7 xenograft mouse models (125-250 mg/kg); enhances the antitumor effect of paclitaxel in an MCF-7 breast cancer xenograft mouse model,

Formal name: 4-dodecyl-N-1,3,4-thiadiazol-2-yl-benzenesulfonamide

Synonyms:  Akt Inhibitor XIV

Molecular weight: 409.6

CAS: 1191951-57-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Serine/Threonine Kinases||Product Type|Biochemicals|Kinase Inhibitors|PKB/Akt||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling

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