Catalog Number
ACM1032754816
Description
GNE-477 is a dual inhibitor of PI3K (IC50 = 4 nM for PI3Kα) and mTOR (apparent Ki = 21 nM).
Synonyms
GNE-477; GNE477; GNE 477
IUPAC Name
5-(7-methyl-6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine
Molecular Formula
C21H28N8O3S2
Canonical SMILES
NC1=NC=C(C2=NC(N3CCOCC3)=C4C(C(C)=C(CN5CCN(S(=O)(C)=O)CC5)S4)=N2)C=N1
InChI
InChI=1S/C21H28N8O3S2/c1-14-16(13-27-3-5-29(6-4-27)34(2,30)31)33-18-17(14)25-19(15-11-23-21(22)24-12-15)26-20(18)28-7-9-32-10-8-28/h11-12H,3-10,13H2,1-2H3,(H2,22,23,24)
InChI Key
AKKCGLXULFRAET-UHFFFAOYSA-N
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Storage
Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
Biological Target
GNE-477 is a potent and efficacious dual PI3K (IC50=4 nM)/mTOR(Ki=21 nM) inhibitor.
Drug Formulation
This drug may be formulated in DMSO
Elemental Analysis
C, 49.98; H, 5.59; N, 22.21; O, 9.51; S, 12.71
HS Tariff Code
2934.99.9001
In Vitro Activity
GNE-477 exerted an obvious inhibitory effect on U87 and U251 cells, and the effect on the viability of the two cell lines was dose-dependent (Figures 1B,C).
Reference: Front Pharmacol. 2021 Jul 26;12:659511. https://pubmed.ncbi.nlm.nih.gov/34381355/
In Vivo Activity
Tumor growth curve results, Figure 4A, demonstrated that intraperitoneal (i.p.) injection of GNE-477, at 10 or 50 mg/kg (daily, for 3 weeks), potently inhibited RCC1 xenograft tumor growth in nude mice.
Reference: Aging (Albany NY). 2020 May 18;12(10):9489-9499. https://pubmed.ncbi.nlm.nih.gov/32421688/
Shipping
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Stock Solution Storage
0-4 °C for short term (days to weeks), or -20 °C for long term (months).
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