Numidargistat (CB1158, INCB01158)
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 100mg | $2650 | To Be Confirmed |
| 200mg | $3975 | To Be Confirmed |
| 500mg | $6705 | To Be Confirmed |
: Cat #: V17647 CAS #: 2095732-06-0 Purity ≥ 98%
Description: Numidargistat (CB-1158 B, INCB-01158) is a novel, potent and orally bioavailable immunomodulating agent acting as an arginase inhibitor with anticancer effects.
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- Physicochemical and Storage Information
- Protocol
- Related Biological Data
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| Molecular Weight (MW) | 287.12 |
|---|---|
| Molecular Formula | C11H22BN3O5 |
| CAS No. | 2095732-06-0 |
| SMILES Code | O=C([C@]1(N)CN(C([C@H](C)N)=O)C[C@@H]1CCCB(O)O)O |
| Synonyms | CB-1158; CB1158; CB 1158; INCB01158; INCB 01158; INCB-01158; INCB 001158; INCB-001158; INCB001158; Numidargistat; |
| Protocol | In Vitro | Numidargistat 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 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 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 show no effect on NOS. In addition, Numidargistat is not directly cytotoxic to murine cancer cell lines. |
|---|---|---|
| In Vivo | Numidargistat (100 mg/kg, p.o., twice per day) increases the number of tumor-infiltrating cytotoxic cells and decreases myeloid cells in mice. Numidargistat in combination with PD-L1 blockade or gemcitabine inhibits tumor growth in mice bearing CT26 cancer cells. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 3.4829 mL | 17.4143 mL | 34.8286 mL | 69.6573 mL |
| 5mM | 0.6966 mL | 3.4829 mL | 6.9657 mL | 13.9315 mL |
| 10mM | 0.3483 mL | 1.7414 mL | 3.4829 mL | 6.9657 mL |
| 20mM | 0.1741 mL | 0.8707 mL | 1.7414 mL | 3.4829 mL |
The molarity calculator equation
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The dilution calculator equation
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Step One: Enter information below
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Step Two: Enter the in vivo formulation
%DMSO
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%
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%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
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Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
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,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:
- (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.