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IPN60090

Catalog No. T11412   CAS 1853164-83-6
Synonyms: GLS1-IN-1

IPN60090 is a novel, potent, orally bioavailable, renal-type glutaminase (GLS1)-specific inhibitor with an IC50 value of 31 nM for GLS1. IPN60090 has potential anticancer and immunostimulant/immunomodulatory activity, selectively targets, binds, and inhibits human glutaminase, and can be used to study GLS1-mediated diseases.

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IPN60090 Chemical Structure
IPN60090, CAS 1853164-83-6
Pack Size Availability Price/USD Quantity
1 mg In stock $ 145.00
5 mg In stock $ 363.00
10 mg In stock $ 563.00
25 mg In stock $ 891.00
50 mg In stock $ 1,230.00
100 mg In stock $ 1,670.00
1 mL * 10 mM (in DMSO) In stock $ 426.00
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Purity: 100%
ee: 100%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description IPN60090 is a novel, potent, orally bioavailable, renal-type glutaminase (GLS1)-specific inhibitor with an IC50 value of 31 nM for GLS1. IPN60090 has potential anticancer and immunostimulant/immunomodulatory activity, selectively targets, binds, and inhibits human glutaminase, and can be used to study GLS1-mediated diseases.
Targets&IC50 GLS1:31 nM (IC50)
In vitro IPN60090 has an IC50 against GLS1 and an EC50 against A549 cell proliferation of <100 nM.[1]
In vivo IPN-60090 (100 mg/kg; oral administration; twice daily; 30 days;) causes tumor growth inhibition. IPN-60090 is robust in vivo target engagement in a dose-dependent manner. The glutamate/glutamine ratios and the free plasma concentrations of IPN-60090 at 4 hours post-dose on both day 4 and day 28 are all decreased.[2]
IPN60090 (3 mg/kg; i.v.; 10 mg/kg for p.o.) has excellent pharmacokinetic properties, with CL=4.1 mL/min/kg, t1/2=1 hour, Cmax=19 μM, F%=89%.[2]
Synonyms GLS1-IN-1
Molecular Weight 532.52
Formula C24H27F3N8O3
CAS No. 1853164-83-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 27.5 mg/mL (51.64 mM), Sonication is recommended.

TargetMolReferences and Literature

1. Maria Emilia Di Francesco, et al. Gls1 inhibitors for treating disease. WO2016004404A2. 2. Soth MJ, et al. Discovery of IPN60090, a Clinical Stage Selective Glutaminase-1 (GLS-1) Inhibitor with Excellent Pharmacokinetic and Physicochemical Properties. J Med Chem. 2020;63(21):12957-12977. 3. Wang D, et al. An updated patent review of glutaminase inhibitors (2019-2022). Expert Opin Ther Pat. 2023;33(1):17-28.

TargetMolCitations

1. Gong K, Huang Y, Zheng Y, et al.ZSWIM4 inhibition improves chemosensitivity in epithelial ovarian cancer cells by suppressing intracellular glycine biosynthesis.Journal of Translational Medicine.2024, 22(1): 1-21.

Related compound libraries

This product is contained In the following compound libraries:
Drug Repurposing Compound Library Anti-Cancer Active Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Inhibitor Library Bioactive Compound Library Immunology/Inflammation Compound Library Clinical Compound Library Anti-Cancer Compound Library Bioactive Compounds Library Max

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Keywords

IPN60090 1853164-83-6 Metabolism Others transporter IPN-60090 IPN 60090 GLS1-IN-1 inhibitor inhibit

 

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