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Numidargistat dihydrochloride

Catalog No. T61336

Numidargistat dihydrochloride (CB-1158) is a highly potent and orally active chemical compound that effectively inhibits arginase. It exhibits IC50 values of 86 nM and 296 nM for recombinant human arginase 1 and 2, respectively. Numidargistat dihydrochloride contributes to immuno-oncology, making it a valuable agent in the field [1].

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Numidargistat dihydrochloride Chemical Structure

Numidargistat dihydrochloride, CAS N/A

Pack Size	Availability	Price/USD
25 mg	10-14 weeks	Inquiry
50 mg	10-14 weeks	Inquiry
100 mg	10-14 weeks	Inquiry

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Numidargistat dihydrochloride (CB-1158) is a highly potent and orally active chemical compound that effectively inhibits arginase. It exhibits IC50 values of 86 nM and 296 nM for recombinant human arginase 1 and 2, respectively. Numidargistat dihydrochloride contributes to immuno-oncology, making it a valuable agent in the field [1].
In vitro	Numidargistat dihydrochloride is a potent, orally-bioavailable arginase inhibitor, demonstrating significant efficacy against both recombinant human arginase 1 and 2, with IC 50 values of 86 nM and 296 nM, respectively. It also effectively inhibits arginase activity in human granulocyte, erythrocyte, and hepatocyte lysates, with IC 50 values of 178 nM, 116 nM, and 158 nM, respectively, and in cancer patient plasma (IC 50, 122 nM). Moreover, Numidargistat dihydrochloride potently inhibits arginase in HepG2 and K562 cell lines, as well as in primary human hepatocytes, with IC 50 values of 32, 139, and 210 μM, respectively. It does not affect NOS activity and is not cytotoxic to murine cancer cell lines, highlighting its specificity and potential therapeutic value [1].
In vivo	Administered orally at a dosage of 100 mg/kg twice daily, Numidargistat dihydrochloride enhances the presence of tumor-infiltrating cytotoxic cells while reducing myeloid cell numbers in mice. Furthermore, when combined with PD-L1 blockade or LY 188011, it effectively suppresses tumor growth in mice implanted with CT26 cancer cells [1].

Molecular Weight	360.04
Formula	C11H24BCl2N3O5

Storage

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

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You can also refer to dose conversion for different animals. More

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

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What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Numidargistat dihydrochloride inhibitor inhibit

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