Numidargistat dihydrochloride
PRODUCTS SPECIFICATIONS
DESCRIPTION
Overview
| MDL | - |
|---|---|
| Molecular Weight | 360.04 |
| Molecular Formula | C11H24BCl2N3O5 |
| SMILES | O=C([C@@H](N)C)N1C[C@H](CCCB(O)O)[C@](N)(C(O)=O)C1.Cl.Cl |
2 Publications Citing Use of MCE
Summary
IC50 & Target
IC50: 86 nM (Arginase 1), 296 nM (Arginase 2) [1]
In Vitro
Numidargistat dihydrochloride is a potent and orally-bioavailable inhibitor of arginase, with IC 50 s of 86 and 296 nM for recombinant human arginase 1 and 2, respectively. Numidargistat dihydrochloride inhibits native rginase 1 (Arg1) in human granulocyte, erythrocyte, and hepatocyte lysate with IC 50 s of 178 nM, 116 nM and 158 nM, respectively, and blocks Arg1 in cancer patient plasma (IC 50 , 122 nM). Numidargistat dihydrochloride also exhibits potent inhibitory activity against arginase in human HepG2, K562 cell lines and primary human hepatocytes with IC 50 s of 32, 139, 210 μM, respectively. Numidargistat dihydrochloride shows no effect on NOS. In addition, Numidargistat dihydrochloride is not directly cytotoxic to murine cancer cell lines [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Numidargistat dihydrochloride (100 mg/kg, p.o., twice per day) increases the number of tumor-infiltrating cytotoxic cells and decreases myeloid cells in mice. Numidargistat dihydrochloride in combination with PD-L1 blockade or LY 188011 inhibits tumor growth in mice bearing CT26 cancer cells [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
-20°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
Solvent & Solubility
DMSO : 55 mg/mL ( 152.76 mM ; Need ultrasonic)
H 2 O : 37.78 mg/mL ( 104.93 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.7775 mL | 13.8873 mL | 27.7747 mL |
| 5 mM | 0.5555 mL | 2.7775 mL | 5.5549 mL |
| 10 mM | 0.2777 mL | 1.3887 mL | 2.7775 mL |
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1.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (277.75 mM); Clear solution; Need ultrasonic
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2.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: 3.25 mg/mL (9.03 mM); Suspended solution; Need ultrasonic
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3.
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4.
Add each solvent one by one: 5% DMSO >> 95% (20% SBE-β-CD in saline)
Solubility: ≥ 1.38 mg/mL (3.83 mM); Clear solution