WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 206804
Description: AMG-511 is a potent and selective pan class I PI3K inhibitor exhibiting IC50 values of 8, 11, 2, and 6 nM against the PI3K β, α, β, and ≤ isoforms respectively. AMG 511 inhibited PI3K pathway signaling in U87 MG glioblastoma cells as determined by dose-dependent reduction in AKT S473 phosphorylation (IC50 = 4 nM). AKT inhibition resulted in a concomitant reduction in PRAS40 phosphorylation (IC50 = 23 nM), a downstream effector of AKT. Reduced phosphorylation of mTORC1 substrates p70S6K (IC50 = 30 nM) and S6 (IC50 = 70 nM) but not 4EBP1 (T37/46), was also detected in U87 MG cells.
MedKoo Cat#: 206804
Chemical Formula: C22H28FN9O3S
Exact Mass: 517.202
Molecular Weight: 517.5844
Elemental Analysis: C, 51.05; H, 5.45; F, 3.67; N, 24.36; O, 9.27; S, 6.19
This product is not in stock, which may be available by custom synthesis.
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Synonym: AMG-511; AMG 511; AMG511.
IUPAC/Chemical Name: (R)-4-[2-[(5-fluoro-6-methoxypyridin-3-yl)amino]-5-[1-(4-methylsulfonylpiperazin-1-yl)ethyl]pyridin-3-yl]-6-methyl-1,3,5-triazin-2-amine
InChi Key: KUGIFHQBIIHRIZ-CYBMUJFWSA-N
InChi Code: 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
SMILES Code: NC1=NC(C2=CC([C@H](N3CCN(S(=O)(C)=O)CC3)C)=CN=C2NC4=CC(F)=C(OC)N=C4)=NC(C)=N1
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: 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.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 517.5844 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Lanman BA, Reed AB, Cee VJ, Hong FT, Pettus LH, Wurz RP, Andrews KL, Jiang J,
McCarter JD, Mullady EL, San Miguel T, Subramanian R, Wang L, Whittington DA, Wu
T, Zalameda L, Zhang N, Tasker AS, Hughes PE, Norman MH.
Phosphoinositide-3-kinase inhibitors: evaluation of substituted alcohols as
replacements for the piperazine sulfonamide portion of AMG 511. Bioorg Med Chem
Lett. 2014 Dec 15;24(24):5630-4. doi: 10.1016/j.bmcl.2014.10.085. PubMed PMID:
2: Subramanian R, Aidasani D, Bailey K, Branstetter D, Everds N, Jiang J, Norman
MH, Primack R, Skiles GL, Soto I, Stec MM, Wagner M, Wu T, Zhu X, Lebrec H.
P450-mediated O-demethylated metabolite is responsible for rat hepatobiliary
toxicity of pyridyltriazine-containing PI3K inhibitors. Toxicol Sci. 2014
Nov;142(1):298-310. doi: 10.1093/toxsci/kfu178. PubMed PMID: 25159132.
3: Norman MH, Andrews KL, Bo YY, Booker SK, Caenepeel S, Cee VJ, D'Angelo ND,
Freeman DJ, Herberich BJ, Hong FT, Jackson CL, Jiang J, Lanman BA, Liu L,
McCarter JD, Mullady EL, Nishimura N, Pettus LH, Reed AB, Miguel TS, Smith AL,
Stec MM, Tadesse S, Tasker A, Aidasani D, Zhu X, Subramanian R, Tamayo NA, Wang
L, Whittington DA, Wu B, Wu T, Wurz RP, Yang K, Zalameda L, Zhang N, Hughes PE.
Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series
of pyridyltriazines leading to the identification of a clinical candidate, AMG
511. J Med Chem. 2012 Sep 13;55(17):7796-816. doi: 10.1021/jm300846z. Erratum in:
J Med Chem. 2012 Oct 25;55(20):8975. PubMed PMID: 22897589.