An inhibitor of mutant IDH1
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Olutasidenib

Item No. 30370

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-[[(1S)-1-(6-chloro-1,2-dihydro-2-oxo-3-quinolinyl)ethyl]amino]-1,6-dihydro-1-methyl-6-oxo-2-pyridinecarbonitrile
CAS Number
1887014-12-1
Synonyms
  • FT-2102
Molecular Formula
C18H15ClN4O2
Formula Weight
354.8
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
λmax
236, 335 nm
SMILES
O=C1C([C@H](C)NC2=CC=C(C#N)N(C)C2=O)=CC3=CC(Cl)=CC=C3N1
InChi Code
InChI=1S/C18H15ClN4O2/c1-10(21-16-6-4-13(9-20)23(2)18(16)25)14-8-11-7-12(19)3-5-15(11)22-17(14)24/h3-8,10,21H,1-2H3,(H,22,24)/t10-/m0/s1
InChi Key
NEQYWYXGTJDAKR-JTQLQIEISA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $69

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    5 mg

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    10 mg

    $399

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    Cayman Chemical
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    Product Description

    Olutasidenib is an inhibitor of mutant isocitrate dehydrogenase 1 (IDH1; IC50s = 0.021 and 0.114 µM for IDH1R132H and IDH1R132C, respectively).1 It is selective for mutant IDH1 over wild-type IDH1 and mutant IDH2 (IC50s = 22.4, 27.3, and >100 μM for wild-type IDH1, IDH2R172K, and IDH2R140Q, respectively). Olutasidenib inhibits production of ɑ-hydroxyglutaric acid (2-HG; Item Nos. 25894 | 16374) in U87 cells expressing mutant IDH1R132H, IDH1R132C, IDH1R132L, IDH1R132G, and IDH1R132S with IC50 values of 0.009, 0.039, 0.042, 0.006, and 0.009 µM, respectively. It reduces intratumor 2-HG levels in HCT116-IDH1R132H and HCT116-IDH1R132C mouse xenograft models when administered at doses of 12.5, 25, and 50 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Caravella, J.A., Lin, J., Diebold, R.B., et al. Structure-based design and identification of FT-2102 (olutasidenib), a potent mutant-selective IDH1 inhibitor. J. Med. Chem. 63(4), 1612-1623 (2020).