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Crelosidenib (gentisate)

  Cat. No.:  DC76856  
Chemical Structure
2759438-85-0
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Field of application
Crelosidenib (gentisate) is a potent, selective and orally active mutant isocitrate dehydrogenase (IDH) inhibitor with IC50 of 6.27 nM, 3.71 nM, 36.9 nM and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q and IDH2 R172K mutant enzymes, respectively. Crelosidenib (gentisate) is less active at inhibiting the IDH wild-type enzymes.
Cas No.: 2759438-85-0
Chemical Name: Crelosidenib (gentisate)
SMILES: OC(C1=C(C=CC(O)=C1)O)=O.O=C2OCC3=CN=C(N=C3N2CC)N[C@@H](C)C(C=C4)=CC=C4[C@@H](N5CCN(CC5)C(C=C)=O)CC6CC6.OC(C7=C(C=CC(O)=C7)O)=O
Formula: C42H48N6O11
M.Wt: 812.86
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Cat. No. Product name Field of application
DC44726 Enasidenib Mesylate Enasidenib (Idhifa, AG-221) mesylate is an orally available, selective and potent inhibitor of mutant isocitrate dehydrogenase 2 (IDH2).
DC28576 DS-1001b DS-1001b is a mutant IDH-1 (Isocitrate Dehydrogenase-1) inhibitor extracted from patent WO2016052697A1, Example 168, and has antitumor activity.
DC76857 Lanisidenib Lanisidenib is the inhibitor for isocitrate dehydrogenase that exhibits antineoplastic activity.
DC76856 Crelosidenib (gentisate) Crelosidenib (gentisate) is a potent, selective and orally active mutant isocitrate dehydrogenase (IDH) inhibitor with IC50 of 6.27 nM, 3.71 nM, 36.9 nM and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q and IDH2 R172K mutant enzymes, respectively. Crelosidenib (gentisate) is less active at inhibiting the IDH wild-type enzymes.
DC72374 (S,S)-GSK321 (S,S)-GSK321 is a (S,S)-enantiomer of GSK321.
DC70642 NCATS-SM5637 NCATS-SM5637 (NSC 791985) is a potent, selective mutant IDH1 inhibitor with IC50 of 81/72 nM for IDH1 mutant R132H/R132C, respctively.NCATS-SM5637 showed higher tumoral concentrations that corresponded to lower 2-HG concentrations in engineered mIDH1-U87-xenograft mouse model, compared with the approved drug AG-120 (ivosidenib).
DC49742 AGI-12026 AGI-12026 is brain-penetrant dual inhibitor of mutant IDH1 and 2. AGI-12026 shows partial inhibition of the IDH1-R132H homodimer as allosteric modulators. AGI-12026 has the potential for research of glioma.
DC48219 Safusidenib Safusidenib is a novel IDH1 inhibitor for the treatment of IDH1-mutated tumors.
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