Apitolisib (GDC-0980, RG7422)是一种有效的，I型PI3K抑制剂，作用于PI3Kα/β/δ/γ，IC₅₀分别为5 nM/27 nM/7 nM/14 nM，也抑制mTOR，K_i为17 nM，高选择性作用于其他PIKK家族激酶。

98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

GDC-0980；RG7422

White to Light Yellow Solid

DMSO : 14.29 mg/mL (28.66 mM; Need ultrasonic)

p110α；p110δ；p110γ；mTOR ；p110β

Apitolisib (GDC-0980) is remarkably selective for several other members of the closely related PIKK family kinases: C2alpha IC₅₀=1300 nM; C2beta IC₅₀=7 94 nM; VPS34 IC50=2000 nM; PI4Kalpha >10 μM; PI4Kbeta >10 μM; DNA-PK Kiapp=623 nM, respectively. A recent study shows that Apitolisib (GDC-0980) reduces cancer cell viability by inhibiting cell-cycle procession and inducing apoptosis with most potency in prostate (IC50 < 200 nM 50%), <500 nm 100%), breast (ic₅₀ <200 nm 37%, <500 78%) and nsclc lines (ic₅₀ <200 nm 29%, <500 88%) and less potency in pancreatic (ic50 <200 13%, 67%) melanoma cell lines (ic₅₀ <200 nM 0%, <500 nM 33%).

In both PC-3 and MCF-7 neo/HER2 xenograft models, GDC-0980 at a dose of 1 mg/kg, exhibits significant antitumor activity by causing tumor growth delay. Furthermore, GDC-0980 results in tumor stasis or regressions at the maximum tolerated dose of 7.5 mg/kg. In mice, intravenous GDC-0980 administration at 1 mg/kg leads to low clearance (Clp: 9.2 mL/min/kg, Vss: 1.7 L/kg). While, oral administration at 5 mg/kg in 80% PEG400 and at 50 mg/kg as a crystalline suspension in 0.5% methylcellulose/0.2% Tween-80 also results in favorable pharmacokinetic parameters.