AMG-511
- Optical Purity: 99% e.e.
- Soluble in DMSO
- MF: C22H28FN9O3S
- MW: 517.58
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.
More Information
| Parent CAS No. | 1253573-53-3 |
|---|---|
| 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 |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | N1C=C([C@@H](C)N2CCN(S(=O)(=O)C)CC2)C=C(C2N=C(N)N=C(C)N=2)C=1NC1C=NC(OC)=C(F)C=1 |&1:3,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C22H28FN9O3S/c1-13(31-5-7-32(8-6-31)36(4,33)34)15-9-17(20-27-14(2)28-22(24)30-20)19(25-11-15)29-16-10-18(23)21(35-3)26-12-16/h9-13H,5-8H2,1-4H3,(H,25,29)(H2,24,27,28,30)/t13-/m1/s1 |
| InChiKey | KUGIFHQBIIHRIZ-CYBMUJFWSA-N |
| CID | 56947516 |
| Short Description | PI3K inhibitor |
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