Go Back GDC-0941 bismesylate
Product Detail
| Cat # | PKI-GDC0941-005 |
| Size | 5 mg |
| Price |
$152.00 |
GDC-0941 is a potent ATP competitive and selective small molecule inhibitor of class I PI3K. The compound is equipotent against p110? and 110? (IC50 = 3 nM), displaying modest levels of selectivity against p110� (10-fold) and p110? (25- fold) whereas half maximal inhibitory concentration for class II PI3Ks (C2�, Vps34, DNA-PK, and mTOR) is in the micro molar range. Over a panel of 228 tested kinases GDC-0941 displayed an outstanding selectivity for the PI3K family kinases. However, partial inhibition was detected for FLT3 and TrkA kinases. Testing of GDC-0941 against various human tumor cell lines indicated that the compound potently inhibits cell proliferation associated with an inhibition of Akt phosphorylation. Since GDC-0941 has shown favorable in vivo anticancer efficacies and low toxicities the compound is currently undergoing clinical testing for treatment of various advanced malignancies.