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Apitolisib

$77$539

Products Details

Product 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.

Web ID

– HY-13246

Storage Temperature

– -20°C, 3 years; 4°C, 2 years (Powder)

Shipping

– Room Temperature

Applications

– Cancer-Kinase/protease

Molecular Formula

– C23H30N8O3S

References

– [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.

CAS Number

– 1032754-93-0

Molecular Weight

– 498.60

Compound Purity

– 99.65

SMILES

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

Clinical Information

– Phase 2

Research Area

– Cancer

Solubility

– DMSO : 14.29 mg/mL (ultrasonic)

Target

– Apoptosis;mTOR;PI3K

Isoform

– mTOR;mTORC1;mTORC2;PI3Kα;PI3Kβ;PI3Kγ;PI3Kδ

Pathway

– Apoptosis;PI3K/Akt/mTOR

Product type

– Reference compound

Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.

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