The IDO inhibitor 1-methyl-tryptophan exists in two stereoisomers with potentially different biological properties. The L isomer is the more potent inhibitor of IDO activity using the purified enzyme and in HeLa cell–based assays. However, the D isomer is significantly more effective in reversing the suppression of T cells created by IDO-expressing dendritic cells. Indoximod (D-1MT, NLG8189) inhibits the enzyme indoleamine 2,3-dioxygenase (IDO), which degrades the essential amino acid tryptophan, and may increase or maintain tryptophan levels important to T cell function. Oral administration of dl-1-methyl-tryptophan in combination with paclitaxel can elicit regression of autochthonous breast tumors.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | B16F10 and 4T1 tumor models mice |
| Formulation | - |
| Dosages | 400 mg/kg |
| Administration | oral gavage |
| Molecular Weight | 218.25 |
| Formula | C12H14N2O2 |
| CAS Number | 110117-83-4 |
| Solubility (25°C) | DMSO 1 mg/mL (Need ultrasonic and warming) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related IDO Products |
|---|
| IDO-IN-18
IDO-IN-18 is an IDO inhibitor. |
| IDO1-IN-21
IDO1-IN-21 is an IDO1 inhibitor (IC50 = 0.64 μM). |
| IDO1-IN-22
IDO1-IN-22 is a IDO1 inhibitor (biochemical hIDO1 IC50: 67.4 nM, HeLa hIDO1 IC50: 17.6 nM). |
| IDO1/TDO-IN-6
IDO1/TDO-IN-6 is a dual inhibitor of IDO1/TDO with IC50s of 2.25 and 2.89 μM, respectively. |
| IDO-IN-13
IDO-IN-13 is a potent indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with an EC50 of 17 nM, extracted from patent WO2019040102A1, example 43. |
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