1. Metabolic Enzyme/Protease
  2. Glutaminase
  3. IPN60090 dihydrochloride

IPN60090 dihydrochloride 

Cat. No.: HY-103671A
Handling Instructions

IPN-60090 dihydrochloride is an orally active and highly selective inhibitor of glutaminase 1 (GLS1; IC50=31 nM), with no activity observed against GLS-2. IPN-60090 dihydrochloride exhibits excellent physicochemical and pharmacokinetic properties in vivo. IPN-60090 dihydrochloride can be used for solid tumors research, such as lung and ovarian cancers.

For research use only. We do not sell to patients.

IPN60090 dihydrochloride Chemical Structure

IPN60090 dihydrochloride Chemical Structure

CAS No. : 2102101-72-2

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Description

IPN-60090 dihydrochloride is an orally active and highly selective inhibitor of glutaminase 1 (GLS1; IC50=31 nM), with no activity observed against GLS-2. IPN-60090 dihydrochloride exhibits excellent physicochemical and pharmacokinetic properties in vivo. IPN-60090 dihydrochloride can be used for solid tumors research, such as lung and ovarian cancers[1][2].

IC50 & Target

IC50: 31 nM (GLS1)[2]

In Vitro

There are two known isoforms of glutaminase: GLS-1 (also called kidney-type or KGA), and GLS-2 (also called liver-type or LGA). GLS-1 is ubiquitous and GLS-2 expression appears limited primarily to the liver.
In a dual-coupled enzyme assay, IPN60090 dihydrochloride inhibits purified recombinant human GLS-1 (GAC isoform) with an IC50 of 31 nM, and has no activity against GLS-2, with an IC50 of >50000 nM[2].
IPN60090 dihydrochloride inhibits the proliferation of A549 cells with an IC50 of 26 nM[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

IPN60090 dihydrochloride (3 mg/kg for 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].
IPN-60090 dihydrochloride (oral administration; 100 mg/kg; twice daily; 30 days) shows similar efficacy and target engagement to CB-839 (HY-12248) dosed orally at 250 mg/kg twice daily. And the 100 mg/kg BID dose of IPN-60090 is a tolerated dose for the following model study[2].
IPN-60090 dihydrochloride (oral administration; 100 mg/kg; twice daily; 30 days; monotherapy or in combination with TAK228 (HY-13328)) causes tumor growth inhibition. IPN-60090 alone demonstrates 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]. Furthermore, IPN-60090 dihydrochloride in combination with TAK228 strongly causes an 85% tumor growth inhibition, IPN-60090 alone causes a 28% tumor growth inhibition in vivo[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female CD-1 mice[2]
Dosage: 3 mg/kg for i.v.; 10 mg/kg for p.o. (Pharmacokinetic Analysis)
Administration: Intravenous injection and oral administration
Result: CL (4.1 mL/min/kg), t1/2 (1 hour) for i.v.; Cmax (19 μM), F% (89%) for p.o..
Animal Model: Ru337 non-small cell lung cancer patient-derived xenograft (PDX) subcutaneous mouse model as monotherapy or in combination [2]
Dosage: 100 mg/kg
Administration: Oral administration; 100 mg/kg; twice daily; 30 days; monotherapy or in combination with TAK228
Result: Exhibited an improvement in the combination regimen group over either single agent.
Clinical Trial
Molecular Weight

605.44

Formula

C₂₄H₂₉Cl₂F₃N₈O₃

CAS No.

2102101-72-2

SMILES

O=C(NC)C1=CN(C[[email protected]](F)CCC2=NN=C(NC(CC3=NC(C)=CC(OC4CC(F)(F)C4)=C3)=O)C=C2)N=N1.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

IPN60090IPN 60090IPN-60090Glutaminasekidney-typeglutaminaseGLS1cancerimmunologicalneurologicaldisordersInhibitorinhibitorinhibit

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IPN60090 dihydrochloride
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HY-103671A
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