2. Metabolic Enzyme/Protease
  3. Glutaminase
  4. IPN60090

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

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IPN60090 Chemical Structure

IPN60090 Chemical Structure

CAS No. : 1853164-83-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 375 In-stock
Solution
10 mM * 1 mL in DMSO USD 375 In-stock
Solid
1 mg USD 128 In-stock
5 mg USD 320 In-stock
10 mg USD 500 In-stock
25 mg USD 810 In-stock
50 mg USD 1200 In-stock
100 mg USD 1600 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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IPN60090 Related Antibodies

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Description

IPN-60090 is an orally active and highly selective inhibitor of glutaminase 1 (GLS1; IC50=31 nM), with no activity observed against GLS-2. IPN-60090 exhibits excellent physicochemical and pharmacokinetic properties in vivo. IPN-60090 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 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 inhibits the proliferation of A549 cells with an IC50 of 26 nM[2].

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

IPN60090 Related Antibodies
In Vivo

IPN60090 (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 (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 (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 in combination with TAK228 strongly causes an 85% tumor growth inhibition, IPN-60090 alone causes a 28% tumor growth inhibition in vivo[2].

MedChemExpress (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

532.52

Formula

C24H27F3N8O3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NC1=NN=C(CC[C@@H](F)CN2N=NC(C(NC)=O)=C2)C=C1)CC3=NC(C)=CC(OC4CC(F)(F)C4)=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 31.43 mg/mL (59.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8779 mL 9.3893 mL 18.7786 mL
5 mM 0.3756 mL 1.8779 mL 3.7557 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 3.14 mg/mL (5.90 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.14 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (31.4 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.47%

COA (244 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8779 mL 9.3893 mL 18.7786 mL 46.9466 mL
5 mM 0.3756 mL 1.8779 mL 3.7557 mL 9.3893 mL
10 mM 0.1878 mL 0.9389 mL 1.8779 mL 4.6947 mL
15 mM 0.1252 mL 0.6260 mL 1.2519 mL 3.1298 mL
20 mM 0.0939 mL 0.4695 mL 0.9389 mL 2.3473 mL
25 mM 0.0751 mL 0.3756 mL 0.7511 mL 1.8779 mL
30 mM 0.0626 mL 0.3130 mL 0.6260 mL 1.5649 mL
40 mM 0.0469 mL 0.2347 mL 0.4695 mL 1.1737 mL
50 mM 0.0376 mL 0.1878 mL 0.3756 mL 0.9389 mL
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IPN60090 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

IPN600901853164-83-6IPN 60090IPN-60090Glutaminasekidney-typeglutaminaseGLS1cancerimmunologicalneurologicaldisordersInhibitorinhibitorinhibit

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