Purity/Purification
98%
CAS
2230263-60-0
Targets&IC50
IDH2 R172K:11.5 nM (IC50), IDH1 R132C:3.71 nM (IC50), IDH2 R140Q:36.9 nM (IC50), IDH1 R132H:6.27 nM (IC50), IDH2 wild-type:884 nM (IC50), IDH1 wild-type:105 nM (IC50)
Solubility
<1mg/ml refers to the product slightly soluble or insoluble
In vitro
Mutant IDH1-IN-6 (Example 2; 0-32 mg/kg; oral gavage; twice daily; for 3 days) treatment inhibitis of 2-hydroxyglutarate in a dose-dependent manner in IDHl mutant xenograft mice[1]. Animal Model: Athymic nude mice (20-22 g) injected with TB08 cells[1]. Dosage: 1 mg/kg, 2 mg/kg, 4 mg/kg, 8mg/kg, 16 mg/kg, 32 mg/kg. Administration: Oral gavage; twice daily; for 3 days. Result: Inhibitied of 2-hydroxyglutarate in IDHl mutant xenograft mice.
Preparation and Storage
Powder: -20 degree C for 3 years
In solvent: -80 degree C for 2 years
In solvent: -80 degree C for 2 years
Related Product Information for Mutant IDH1-IN-6 biochemical
Mutant IDH1-IN-6 is a potent, selective and orally active mutant isocitrate dehydrogenase (IDH) inhibitor with IC 50 s of 6.27 nM, 3.71 nM, 36.9 nM and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q and IDH2 R172K mutant enzymes, respectively. Mutant IDH1-IN-6 is less active at inhibiting the IDH wild-type enzymes.
References
1. Harald Engelhardt, et al. New macrocyclic compounds and derivatives as egfr inhibitors. WO2020260252A1.
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Product Notes
The Mutant IDH1-IN-6 (Catalog #AAA228226) is a Biochemical and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "Mutant IDH1-IN-6, Biochemical" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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