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Chemical Structure : GDC-0980
CAS No.: 1032754-93-0
Catalog No.: PC-43426Not For Human Use, Lab Use Only.
GDC-0980 (Apitolisib, GNE 390, RG 7422) is a potent, selective, orally available class I PI3K/mTOR inhibitor with IC50 of 5 nM/27 nM/7 nM/14 nM for PI3Kα/β/δ/γ, inhibits mTOR inhibitor with Ki of 17 nM.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $128 | In stock | |
| 25 mg | $218 | In stock | |
| 50 mg | $358 | In stock | |
| 100 mg | $558 | In stock | |
| 200 mg | Get quote | ||
| 1 g | Get quote |
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GDC-0980 (Apitolisib, GNE 390, RG 7422) is a potent, selective, orally available class I PI3K/mTOR inhibitor with IC50 of 5 nM/27 nM/7 nM/14 nM for PI3Kα/β/δ/γ, inhibits mTOR inhibitor with Ki of 17 nM.
GDC-0980 displays remarkably selectivity for several other members of the closely related PIKK family kinases, including C2alpha, C2beta, VPS34 I, PI4Kalpha, PI4Kbeta and DNA-PK.
GDC-0980 potently inhibits signal transduction downstream of both PI3K and mTOR, reduces viability in multiple cancer cell lines by cell-cycle inhibition and induction of apoptosis (prostate IC50<200 nM, NSCLC lines <200 nM).
GDC-0980 potently inhibits tumor growth in xenograft models with activated PI3K, loss of LKB1 or PTEN.
| M.Wt | 498.6011 | |
| Formula | C23H30N8O3S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
1-Propanone, 1-[4-[[2-(2-amino-5-pyrimidinyl)-7-methyl-4-(4-morpholinyl)thieno[3,2-d]pyrimidin-6-yl]methyl]-1-piperazinyl]-2-hydroxy-, (2S)- |
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1. Wallin JJ, et al. Mol Cancer Ther. 2011 Dec;10(12):2426-36.
2. Sutherlin DP, et al. J Med Chem. 2011 Nov 10;54(21):7579-87.
3. Spoerke JM, et al. Clin Cancer Res. 2012 Dec 15;18(24):6771-83.et al.
4. Makhov PB, et al. Mol Cancer Ther. 2012 Jul;11(7):1510-7.
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