IPN60090
Based on 1 Customer Validation
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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 98.96%
- CAS No.: 1853164-83-6
- Formule: C24H27F3N8O3
- Masse moléculaire:532.52
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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GK921Glutaminase Inhibitor -
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IPN60090 (Standard)Reference Standard -
HY-19359
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TG-2-IN-1TGM-2 Inhibitor -
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UPGL00004GAC Inhibitor
Activité biologique
Description
IC50 & Target
IC50: 31 nM (GLS1)[2]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
26 nM
Compound: 27
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Antiproliferative activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by celltiter-fluor assay
Antiproliferative activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by celltiter-fluor assay
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[PMID: 33118821] |
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.
In Vivo
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.
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Animal Model:Female CD-1 mice[2]
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Dosage:3 mg/kg for i.v.; 10 mg/kg for p.o. (Pharmacokinetic Analysis)
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Administration:Intravenous injection and oral administration
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Result:CL (4.1 mL/min/kg), t1/2 (1 hour) for i.v.; Cmax (19 μM), F% (89%) for p.o..
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Animal Model:Ru337 non-small cell lung cancer patient-derived xenograft (PDX) subcutaneous mouse model as monotherapy or in combination[2]
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Dosage:100 mg/kg
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Administration:Oral administration; 100 mg/kg; twice daily; 30 days; monotherapy or in combination with TAK228
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Result:Exhibited an improvement in the combination regimen group over either single agent.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1853164-83-6
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Appearance Solid
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Masse moléculaire 532.52
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Formule C24H27F3N8O3
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Color Light yellow to yellow
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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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (271 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Maria Emilia Di Francesco, et al. Gls1 inhibitors for treating disease. WO2016004404A2.
[2]. Michael J Soth, et al. Discovery of IPN60090, a Clinical Stage Selective Glutaminase-1 (GLS-1) Inhibitor with Excellent Pharmacokinetic and Physicochemical Properties. J Med Chem. 2020 Nov 12;63(21):12957-12977. [Content Brief]
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 |
IPN60090 Related Classifications
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