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GNE-490

Chemical Structure : GNE-490

CAS No.: 1033739-92-2

GNE-490 (GNE490)

Catalog No.: PC-63013Not For Human Use, Lab Use Only.

GNE-490 is a potent, selective, orally available class I PI3K inhibitor with IC50 of 3.5/25/5.2/15 nM for PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GNE-490 is a potent, selective, orally available class I PI3K inhibitor with IC50 of 3.5/25/5.2/15 nM for PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ。
GNE-490 shows >200-fold selectivity over mTOR (IC50=740 nM)。
GNE-490 has good PK profiles, and are efficacious in xenograft models.

Physicochemical Properties

M.Wt 386.474
Formula C18H22N6O2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-(2-Amino-4-methyl-5-pyrimidinyl)-α,α-dimethyl-4-(4-morpholinyl)thieno[3,2-d]pyrimidine-6-methanol

References

1. Sutherlin DP, et al. J Med Chem. 2010 Feb 11;53(3):1086-97.

2. Sampath D, et al. Neoplasia. 2013 Jul;15(7):694-711.

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