AG-120


Catalog No. size PriceQuantity
M6556-2 2mg solid $140
M6556-10 10mg solid $563

Description

Cas:1448346-63-1

Product Information:

AG-120 , a racemic mixture of AG-120, is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity. Upon administration, AG-120 specifically inhibits a mutated form of IDH1 in the cytoplasm, which inhibits the formation of the oncometabolite, 2-hydroxyglutarate (2HG). This may lead to both an induction of cellular differentiation and an inhibition of cellular proliferation in IDH1-expressing tumor cells.

 

Chemical Formula: C28H22ClF3N6O3

 

Exact Mass: 582.1394

 

Molecular Weight: 582.97

 

Elemental Analysis: C, 57.69; H, 3.80; Cl, 6.08; F, 9.78; N, 14.42; O, 8.23

 

Synonym:

 

AG-120 (racemic)

AG120

AG 120

AG-120

RG-120 (racemic)

RG-120

RG 120

Ivosidenib (racemic)

 

Chemical Name: (2S)-N-(1-(2-chlorophenyl)-2-((3,3-difluorocyclobutyl)amino)-2-oxoethyl)-1-(4-cyanopyridin-2-yl)-N-(5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide

 

InChi Key: 

WIJZXSAJMHAVGX-XADRRFQNSA-N

 

InChi Code: InChI=1S/C28H22ClF3N6O3/c29-21-4-2-1-3-20(21)25(26(40)36-18-11-28(31,32)12-18)37(19-10-17(30)14-34-15-19)27(41)22-5-6-24(39)38(22)23-9-16(13-33)7-8-35-23/h1-4,7-10,14-15,18,22,25H,5-6,11-12H2,(H,36,40)/t22-,25?/m0/s1

 

Smiles Code:

O=C([C@H](CC1)N(C2=NC=CC(C#N)=C2)C1=O)N(C(C3=CC=CC=C3Cl)C(NC4CC(F)(F)C4)=O)C5=CC(F)=CN=C5

 

 

Technical Data:

 

Appearance: White to off-white 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, not in water

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

 

 

References

 

  1. Birendra KC, DiNardo CD. Evidence for Clinical Differentiation and Differentiation Syndrome in Patients With Acute Myeloid Leukemia and IDH1 Mutations Treated With the Targeted Mutant IDH1 Inhibitor, AG-120. Clin Lymphoma Myeloma Leuk. 2016 Aug;16(8):460-5. doi: 10.1016/j.clml.2016.04.006. PubMed PMID: 27245312; PubMed Central PMCID: PMC4983480.

 

  1. Brody JR, Yabar CS, Zarei M, Bender J, Matrisian LM, Rahib L, Heartwell C, Mason K, Yeo CJ, Peiper SC, Jiang W, Varieur K, Madhavan S, Petricoin E 3rd, Fortuna D, Curtis M, Wang ZX, Pishvaian MJ, Winter JM. Identification of a novel metabolic-related mutation (IDH1) in metastatic pancreatic cancer. Cancer Biol Ther. 2016 Jul 28:0. [Epub ahead of print] PubMed PMID: 27466707.

 

  1. Caino MC, Altieri DC. Molecular Pathways: Mitochondrial Reprogramming in Tumor Progression and Therapy. Clin Cancer Res. 2016 Feb 1;22(3):540-5. doi: 10.1158/1078-0432.CCR-15-0460. Review. PubMed PMID: 26660517; PubMed Central PMCID: PMC4738153.

 

  1. Chen J, Yang J, Cao P. The Evolving Landscape in the Development of Isocitrate Dehydrogenase Mutant Inhibitors. Mini Rev Med Chem. 2016;16(16):1344-1358. PubMed PMID: 27292784.

 

  1. Cuyàs E, Fernández-Arroyo S, Corominas-Faja B, Rodríguez-Gallego E, Bosch-Barrera J, Martin-Castillo B, De Llorens R, Joven J, Menendez JA. Oncometabolic mutation IDH1 R132H confers a metformin-hypersensitive phenotype. Oncotarget. 2015 May 20;6(14):12279-96. PubMed PMID: 25980580; PubMed Central PMCID: PMC4494938.

 

Products are for research use only. Not for human use.

 

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