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IDH-305

Catalog No. T15550 CAS 1628805-46-8

IDH-305 is an orally available, mutation-selective, and brain-penetrant IDH1 inhibitor targeting the IDH1 (R132) mutation. IDH-305 is 200-fold more selective for mutant IDH1 isoforms than wild type with IC50s of 27 nM,28 nM and 6.14 nM for IDH1R132H, IDH1R132C and IDH1WT, respectively.

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IDH-305, CAS 1628805-46-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 52.00
5 mg	In stock	$ 128.00
10 mg	In stock	$ 178.00
25 mg	In stock	$ 369.00
50 mg	In stock	$ 558.00
1 mL * 10 mM (in DMSO)	In stock	$ 139.00

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Purity: 99.13%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	IDH-305 is an orally available, mutation-selective, and brain-penetrant IDH1 inhibitor targeting the IDH1 (R132) mutation. IDH-305 is 200-fold more selective for mutant IDH1 isoforms than wild type with IC50s of 27 nM,28 nM and 6.14 nM for IDH1R132H, IDH1R132C and IDH1WT, respectively.
Targets&IC50	IDH1 (R132C):28 nM, IDH1 (R132H):27 nM, IDH1 (WT):6.14 μM
In vitro	IDH-305 suppresses HCT116-IDH1R132H /- cells (IC50 of 24 nM)[1].
In vivo	P.o. administration of 30-300 mg/kg IDH-305 twice daily for 21 days suppresses 2-HG production and 2-HG-dependent tumor growth of an IDH1 mutant PDX melanoma model [1].

Molecular Weight	490.45
Formula	C23H22F4N6O2
CAS No.	1628805-46-8

Storage

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

Solubility Information

DMSO: 100 mg/mL (203.90 mM)

References and Literature

1. Cho YS, et al. Discovery and Evaluation of Clinical Candidate IDH305, a Brain Penetrant Mutant IDH1 Inhibitor. ACS Med Chem Lett. 2017 Sep 18;8(10):1116-1121. 2. Courtney D DiNardo, et al. A Phase I Study of IDH305 in Patients with Advanced Malignancies Including Relapsed/Refractory AML and MDS That Harbor IDH1R132 Mutations. Blood, 128(22), 1073.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Orally Active Compound Library Clinical Compound Library Glutamine Metabolism Compound Library ReFRAME Related Library Metabolism Compound Library

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Keywords

IDH-305 1628805-46-8 Metabolism Dehydrogenase IDH 305 Isocitrate Dehydrogenase (IDH) IDH305 Inhibitor inhibit inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.