Apitolisib

Apitolisib (GDC-0980; GNE 390; RG 7422) is a selective, potent, orally bioavailable Class I PI3 kinase and mTOR kinase (TORC1/2) inhibitor with IC50s of 5 nM/27 nM/7 nM/14 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ, and with a Ki of 17 nM for mTOR.

Product Specifications

CAS Number

[1032754-93-0]

Product Name Alternative

GDC-0980; GNE 390; RG 7422

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; mTOR; PI3K

Type

Reference compound

Related Pathways

Apoptosis; PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/gdc-0980.html

Concentration

10mM

Purity

99.29

Solubility

DMSO : 14.29 mg/mL (ultrasonic)

Smiles

C[C@@H](C(N1CCN(CC1)CC2=C(C3=NC(C4=CN=C(N=C4)N)=NC(N5CCOCC5)=C3S2)C)=O)O

Molecular Formula

C23H30N8O3S

Molecular Weight

498.60

Precautions

H302, H315, H319, H335

References & Citations

[1]Sutherlin DP, et al. Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K) /mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer. J Med Chem, 2011, 54 (21), 7579-7587.|[2]Wallin JJ, et al. 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, 10 (12), 2426-2436.