|GDC-0980 (RG7422) Class I PI3K inhibitor for PI3Kα/β/δ/γ|
Sample solution is provided at 25 µL, 10mM.
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|Description||Apitolisib (GDC-0980, RG7422) is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 values of 5 nM/27 nM/7 nM/14 nM, respectively.|
|IC50||5 nM||7 nM||14 nM||17 nM(Ki app)||27 nM|
|Cas No.||1032754-93-0||SDF||Download SDF|
|Solubility||>21.35mg/mL in DMSO||Storage||Store at -20°C|
|Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
GDC-0980 (RG7422) is a selective, novel, potent and orally bioavailable inhibitor of class 1 PI3K/mTOR kinase with the Ki value of 17nmol/L for mTOR kinase .
GDC-0980 (RG7422) has shown the effective inhibition with the IC50 values of ＜200nmol/L in prostate, breast and NSCLC lines, respectinely. In addition, GDC-0980 (RG7422) has been reported to reduce cell viability in KPL4 cells by cell-cycle inhibition and induction of apoptosis with the IC50 value of 109nM and the EC50 value of 78nM. Furthermore, GDC-0980 (RG7422) has been revealed to significantly inhibit tumor responses in xenograft models in oral dose of the compound. Besides, GDC-0980 (RG7422) has been noted to enhance the antitumor activity in combination with antitumor agents ( docetaxel) in vivo .
 Wallin JJ1, Edgar KA, Guan J, Berry M, Prior WW, Lee L, Lesnick JD, Lewis C, Nonomiya J, Pang J, Salphati L, Olivero AG, Sutherlin DP, O'Brien C, Spoerke JM, Patel S, Lensun L, Kassees R, Ross L, Lackner MR, Sampath D, Belvin M, Friedman LS. GDC-0980 is a novel class I PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway. Mol Cancer Ther. 2011 Dec;10(12):2426-36. doi: 10.1158/1535-7163.MCT-11-0446. Epub 2011 Oct 13.