A66 |
(2S)-1-N-[5-(2-tert-butyl-1,3-thiazol-4-yl)-4-methyl-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide |
(CAS 1166227-08-2) |
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Description: |
In vivo:A single dose of A66 at 100 mg/1kg induces a profound reduction in the phosphorylation of Akt/PKB and p70 S6 kinase, but not of ERK, in SK-OV-3 tumour tissue in vivo at both 1 hour and 6 hours after dosing. A66 dosed at 100 mg/1kg once daily (QD) for 21 days or 75 mg/1kg twice daily (BID) for 16 days induces a significant delay in growth of SK-OV-3 xenografted tumors with average TGI of 45.9% and 29.9%, respectively, which is even greater than that induced by the well-established pan-PI3K inhibitor BEZ-235. QD dosing of A66 in the HCT-116 xenograft model also induces a significant reduction in tumour volume with TGI of 77.2%, but causes a non-significant reduction in tumor volume in the U87MG xenograft model. [1] Administration of A66 at 10 mg in male CD1 mice induces significant impairments in the ITT (insulin tolerance test) and GTT (glucose tolerance test), and an increase in glucose production during a PTT (pyruvate tolerance test), almost to the same level as the pan-PI3K inhibitors. [3]
Features:Highly selective for the p110α isoform. |
Product No. |
KT00013 |
Product Name |
A66 |
Synonyms |
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Formal Name |
(2S)-1-N-[5-(2-tert-butyl-1,3-thiazol-4-yl)-4-methyl-1,3-thiazol-2-yl]pyrrolidine-1,2-dicarboxamide |
CAS Number |
1166227-08-2 |
Molecular Formula |
C17H23N5O2S2 |
Formula Weight |
393.53 |
Formulation |
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Purity |
98%min |
Stability |
1 year |
Storage |
-20℃ |
Shipping |
USD45 for Europe and USA. No shipping charge once amount reach USD500. |
Quality Control |
HNMR,CNMR,LCMS,HPLC,IR,etc. |
Price & Availability |
In Stock. Price Negotiated. |
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