AMG-511

Based on 6 reference(s) in Google Scholar 8 10 6

Axon 3827

CAS [1253573-53-3]

MF C22H28FN9O3S
MW 517.58

  • Purity: 99%
  • Optical purity: 99% e.e.
  • Soluble in DMSO
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AMG-511

Description

AMG-511 is an orally bioavailable, highly potent and selective pan-class I phosphatidylinositol-3 kinase (PI3K) inhibitor with in vitro Ki values of 4nM/6nM/2nM/1nM for p110α/β/δ/γ isoforms, respectively, and is highly selective over mTOR (IC50 > 10000 nM), hVPS34 (IC50 > 9000 nM), DNAPK (IC50 = 12000 nM), and a broad panel of other protein kinases. It effectively inhibited pAKT in tumor tissue in a dose- and time-dependent manner (up to 16 hours). In animal studies it efficaciously inhibited tumor growth in PTEN-null, KRAS mutant, and HER2 amplified xenograft models. It is currently in clinical trials for cancer treatment.

KEYWORDS: AMG-511 | PI3K inhibitor | AMG511 | AMG 511 | CT-AMG511 | CAS [1253573-53-3] | Phosphatidylinositol | PI3K | Inhibitor | Enzymes

Orally bioavailable, highly potent and selective pan-class I phosphatidylinositol-3 kinase (PI3K) inhibitor

Chemical name

(R)-4-(2-(5-fluoro-6-methoxypyridin-3-ylamino)-5-(1-(4-(methylsulfonyl)piperazin-1-yl)ethyl)pyridin-3-yl)-6-methyl-1,3,5-triazin-2-amine

Source information

Sold in collaboration with Chemietek

Parent CAS No.

[1253573-53-3]

The purity of Axon Ligands™ is confirmed by HPLC-MS, 1H-NMR and/or microanalysis. Analytical data are available upon request.

Caution: Axon Ligands™ are not fully tested. They are for research purposes only! Not for human consumption!

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