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Apitolisib

CAT: 0804-HY-13246-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-13246-01Size:5 mg
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Description
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.
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 2
Isoform
MTOR; mTORC1; mTORC2; PI3Kα; PI3Kβ; PI3Kγ; PI3Kδ