GNE-490
GNE-490 Basic information
- Product Name:
- GNE-490
- Synonyms:
-
- GNE-490
- 2-(2-Amino-4-methyl-5-pyrimidinyl)-alpha,alpha-dimethyl-4-(4-morpholinyl)thieno[3,2-d]pyrimidine-6-methanol
- GNE490;GNE 490
- CS-2657
- Thieno[3,2-d]pyrimidine-6-methanol, 2-(2-amino-4-methyl-5-pyrimidinyl)-α,α-dimethyl-4-(4-morpholinyl)-
- 2-(2-(2-amino-4-methylpyrimidin-5-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)propan-2-ol
- PI3Kβ,GNE 490,PI3Kδ,Mammalian target of Rapamycin,mTOR,GNE-490,MCF7.1,PI3K,PI3Kα,Phosphoinositide 3-kinase,PI3Kγ,breast cancer,Inhibitor,GNE490,inhibit
- 2-[2-(2-amino-4-methylpyrimidin-5-yl)-4-(morpholin-4-yl)thieno[3,2-d]pyrimidin-6-yl]propan-2-ol
- CAS:
- 1033739-92-2
- MF:
- C18H22N6O2S
- MW:
- 386.47
- Mol File:
- 1033739-92-2.mol
GNE-490 Chemical Properties
- storage temp.
- 4°C, protect from light
- solubility
- DMSO : ≥ 100 mg/mL (258.75 mM)
- form
- Solid
- color
- White to off-white
GNE-490 Usage And Synthesis
Description
GNE-490 is a highly selective pan-PI3K inhibitor, demonstrating selectivity over mTOR.
Uses
GNE-490, a (thienopyrimidin-2-yl)aminopyrimidine, is a potent pan-PI3K inhibitor with IC50s of 3.5 nM, 25 nM, 5.2 nM, 15 nM for ?PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ, respectively. GNE-490 has >200 fold selectivity for mTOR (IC50=750 nM). GNE-490 shows potent suppression efficacy profile against MCF7.1 breast cancer xenograft model[1].
IC 50
PI3Kα: 3.5 nM (IC50); PI3Kβ: 25 nM (IC50); PI3Kδ: 5.2 nM (IC50); PI3Kγ: 15 nM (IC50); mTOR: 750 nM (IC50)
References
[1] Daniel P Sutherlin, et al. Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer. J Med Chem. 2010 Feb 11;53(3):1086-97. DOI:10.1021/jm901284w
GNE-490Supplier
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