This product is for research use only, not for human use. We do not sell to patients.
| Size | Price | Stock |
|---|---|---|
| 100mg | $1150 | To Be Confirmed |
| 250mg | $1750 | To Be Confirmed |
| 500mg | $2625 | To Be Confirmed |
: Cat #: V7270 CAS #: 2095732-06-0 (free base) Purity ≥ 98%
Description: Numidargistat 2HCl (CB-1158 B, INCB-01158; INCB001158) is a novel, potent and orally bioavailable immunomodulating agent acting as an arginase inhibitor with IC50s of 86 nM and 296 nM for recombinant human arginase 1 and recombinant human arginase 2, respectively.
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| Molecular Weight (MW) | 360.04 |
|---|---|
| Molecular Formula | C11H24BCl2N3O5 |
| CAS No. | 2095732-06-0 (free base) |
| Synonyms | Numidargistat dihydrochloride; CB-1158 dihydrochloride; INCB01158 dihydrochloride |
| Protocol | In Vitro | Numidargistat dihydrochloride is a potent and orally-bioavailable inhibitor of arginase, with IC50s 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 IC50s of 178 nM, 116 nM and 158 nM, respectively, and blocks Arg1 in cancer patient plasma (IC50, 122 nM). Numidargistat dihydrochloride also exhibits potent inhibitory activity against arginase in human HepG2, K562 cell lines and primary human hepatocytes with IC50s 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. |
|---|---|---|
| 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. |
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.7775 mL | 13.8873 mL | 27.7747 mL | 55.5494 mL |
| 5mM | 0.5555 mL | 2.7775 mL | 5.5549 mL | 11.1099 mL |
| 10mM | 0.2777 mL | 1.3887 mL | 2.7775 mL | 5.5549 mL |
| 20mM | 0.1389 mL | 0.6944 mL | 1.3887 mL | 2.7775 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.