IDH-889
- Product Name
- IDH-889
- CAS No.
- 1429179-07-6
- Chemical Name
- IDH-889
- Synonyms
- IDH889;IDH-889;IDH889 (IDH 889;IDH889, 10 mM in DMSO;IDH889;IDH-889;IDH 889;Inhibitor,inhibit,Isocitrate Dehydrogenase (IDH),IDH889,IDH 889,IDH-889;2-Oxazolidinone, 3-[2-[[(1S)-1-[5-(4-fluoro-3-methylphenyl)-2-pyrimidinyl]ethyl]amino]-4-pyrimidinyl]-4-(1-methylethyl)-, (4S)-
- CBNumber
- CB33354248
- Molecular Formula
- C23H25FN6O2
- Formula Weight
- 436.48
- MOL File
- 1429179-07-6.mol
IDH-889 Property
- Boiling point:
- 589.5±60.0 °C(Predicted)
- Density
- 1.284±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- form
- Solid
- pka
- 4.15±0.10(Predicted)
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- CS-0044740
- Product name
- IDH889
- Packaging
- 5mg
- Price
- $300
- Updated
- 2021/12/16
- Product number
- CS-0044740
- Product name
- IDH889
- Packaging
- 10mg
- Price
- $500
- Updated
- 2021/12/16
- Product number
- CS-0044740
- Product name
- IDH889
- Packaging
- 25mg
- Price
- $850
- Updated
- 2021/12/16
- Product number
- CS-0044740
- Product name
- IDH889
- Packaging
- 50mg
- Price
- $1200
- Updated
- 2021/12/16
- Product number
- CS-0044740
- Product name
- IDH889
- Packaging
- 100mg
- Price
- $1800
- Updated
- 2021/12/16
IDH-889 Chemical Properties,Usage,Production
Description
IDH889 is a potent and selective inhibitors of IDH1. IDH899 shows IDH (R132H) IC50 = 20 nM; Cell 2-HG IC50 = 14 nM. IDH889 demonstrates significantly improved plasma exposure in mice vs IDH662 (AUC 3.6 μM·h, Cmax 1.7 μM at 10 mg/kg; AUC 55.5 μM·h, Cmax 14.2 μM at 100 mg/kg). IDH889 also has excellent permeability and no efflux in the Caco-2 and human MDR1-MDCK cell lines, supporting the hypothesis that potent inhibition of mutant IDH1 function by binding at the allosteric binding site is compatible with brain penetration.
Uses
IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC50s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1R132H, IDH1R132C and IDH1wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC50 of 0.014 μM[1].
References
[1] Levell JR, et al. Optimization of 3-Pyrimidin-4-yl-oxazolidin-2-ones as Allosteric and Mutant Specific Inhibitors of IDH1. ACS Med Chem Lett. 2016 Dec 16;8(2):151-156. DOI:10.1021/acsmedchemlett.6b00334
IDH-889 Preparation Products And Raw materials
Raw materials
Preparation Products
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