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Numidargistat

Catalog No. T10692L CAS 2095732-06-0

Synonyms: INCB01158, CB-1158

CB-1158 is a potent and orally bioavailable inhibitor of arginase (IC50s: 86 and 296 nM for recombinant human arginase 1 and 2).

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Numidargistat, CAS 2095732-06-0

Pack Size	Availability	Price/USD
25 mg	6-8 weeks	$ 736.00
50 mg	6-8 weeks	$ 957.00
100 mg	6-8 weeks	$ 1,440.00

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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	CB-1158 is a potent and orally bioavailable inhibitor of arginase (IC50s: 86 and 296 nM for recombinant human arginase 1 and 2).
Targets&IC50	Arginases II:296 nM, Arginases I:86 nM
In vitro	CB-1158 is not directly cytotoxic to murine cancer cell lines [1]. CB-1158 inhibits native arginase 1 (Arg1) in human granulocyte, erythrocyte, and hepatocyte lysate (IC50s: 178 nM, 116 nM, and 158 nM) and blocks Arg1 in cancer patient plasma (IC50, 122 nM). CB-1158 shows no effect on NOS and it also shows potent inhibitory activity against arginase in human HepG2, K562 cell lines, and primary human hepatocytes (IC50s: 32, 139, 210 μM).
In vivo	CB-1158 in combination with PD-L1 blockade or gemcitabine inhibits tumor growth in mice bearing CT26 cancer cells. CB-1158 (100 mg/kg, p.o., twice per day) increases the number of tumor-infiltrating cytotoxic cells and decreases myeloid cells in mice.

Synonyms	INCB01158, CB-1158
Molecular Weight	287.12
Formula	C11H22BN3O5
CAS No.	2095732-06-0

Storage

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

References and Literature

1. Steggerda SM, et al. Inhibition of arginase by CB-1158 blocks myeloid cell-mediated immune suppression in the tumor microenvironment. J Immunother Cancer. 2017 Dec 19;5(1):101.

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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.

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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 2095732-06-0 Others CB 1158 CB1158 INCB01158 INCB 01158 INCB-01158 CB-1158 inhibitor inhibit

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