A GLS1 inhibitor
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IPN60090

Item No. 35855

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[(3,3-difluorocyclobutyl)oxy]-N-[6-[(3R)-3-fluoro-4-[4-[(methylamino)carbonyl]-1H-1,2,3-triazol-1-yl]butyl]-3-pyridazinyl]-6-methyl-2-pyridineacetamide
CAS Number
1853164-83-6
Synonyms
  • IACS-6274
Molecular Formula
C24H27F3N8O3
Formula Weight
532.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: SolubleMethanol: Soluble
SMILES
FC1(F)CC(OC2=CC(C)=NC(CC(NC3=CC=C(CC[C@H](CN4N=NC(C(NC)=O)=C4)F)N=N3)=O)=C2)C1
InChi Code
InChI=1S/C24H27F3N8O3/c1-14-7-18(38-19-10-24(26,27)11-19)8-17(29-14)9-22(36)30-21-6-5-16(31-33-21)4-3-15(25)12-35-13-20(32-34-35)23(37)28-2/h5-8,13,15,19H,3-4,9-12H2,1-2H3,(H,28,37)(H,30,33,36)/t15-/m1/s1
InChi Key
GEHZIZWHNLQFAS-OAHLLOKOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    Product Description

    IPN60090 is an inhibitor of glutaminase 1 (GLS1; IC50 = 0.031 µM for the glutaminase C isoform).1 It is selective for GLS1 over GLS2 (IC50 = >50 µM), as well as panels of 80 ion channels and receptors and 97 kinases at 10 µM. IPN60090 also binds to zinc finger SWIM domain-containing protein 4 (ZSWIM4; Kd = 2.98 µM).2 It decreases the viability of A549 non-small cell lung cancer (NSCLC) cells (IC50 = 26 nM) and decreases glycine levels in OVCAR-8 and SKOV3 ovarian cancer cells.1,2 IPN60090 (30 mg/kg, p.o.), in combination with the DNA-crosslinking agent carboplatin (Item No. 13112), decreases tumor weight and volume in a SKOV3 mouse xenograft model.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Soth, M.J., Le, K., Di Francesco, M.E., et al. Discovery of IPN60090, a clinical stage selective glutaminase-1 (GLS-1) inhibitor with excellent pharmacokinetic and physicochemical properties. J. Med. Chem. 63(21), 12957-12977 (2020).

    2. Gong, K., Huang, Y., Zheng, Y., et al. ZSWIM4 inhibition improves chemosensitivity in epithelial ovarian cancer cells by suppressing intracellular glycine biosynthesis. J. Transl. Med. 22(1), 192 (2021).