MTHFD2-IN-5
MTHFD2-IN-5 (Compound 16e) is a selective MTHFD2 inhibitor with an IC50 of 66 nM. MTHFD2-IN-5 selectively inhibits MTHFD2. MTHFD2-IN-5 exhibits anticancer activity against acute myeloid leukemia. MTHFD2-IN-5 acts synergistically with Alimta to inhibit the proliferation of acute myeloid leukemia cells.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 3068001-31-7
- Formule: C17H18ClN7O7
- Masse moléculaire:467.82
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
- Pureté et documentation
- Références
-
Help & FAQs
Activité biologique
|
MTHFD2 66 nM (IC50) |
MTHFD1 1790 nM (IC50) |
MTHFD2-IN-5 potently inhibits purified MTHFD2 protein, with an IC50 value of 66 nM[1].
MTHFD2-IN-5 inhibits purified MTHFD1 protein with an IC50 of 1790 nM, and is 27.1-fold more selective for MTHFD2 than for MTHFD1[1].
MTHFD2-IN-5 (72 h) potently inhibits the proliferation of MOLM-14 acute myeloid leukemia cells, with a GI50 of 720 nM[1].
MTHFD2-IN-5 (250-500 nM; 72 h) acts synergistically with Alimta to inhibit the proliferation of MOLM-14 acute myeloid leukemia cells, with a combination index of 0.80[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | T1/2 | CL | Vss | AUC0-inf |
|---|---|---|---|---|---|---|
| Mice[1] | 2 mg/kg | i.v. | 6.5 h | 12.3 mL/min/kg | 0.6 L/kg | 2702 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:NOD/SCID (female, 9-10 weeks old)[1]
-
Dosage:15 mg/kg
-
Administration:i.v.; once daily
-
Result:Achieved 75.7% tumor growth inhibition (TGI) on day 7.
Achieved 57.4% tumor growth inhibition (TGI) on day 14.
Reduced mean tumor volume to 598 mm3 on day 14, compared to 1307 mm3 in the vehicle-treated group.
Showed no significant change in mouse body weight throughout the study period.
Chemical Information
-
CAS No. 3068001-31-7
-
Masse moléculaire 467.82
-
Formule C17H18ClN7O7
-
SMILES
OC(CC[C@@H](C(O)=O)NC(C1=CC(Cl)=C(C=C1)NC(NC2=C(NC(N)=NC2=O)N)=O)=O)=O
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MTHFD2-IN-5 Related Classifications
HY-170361 Related Classifications
Powered by Bioz
- MTHFD2-IN-5
- 3068001-31-7
- Methylenetetrahydrofolate Dehydrogenase (MTHFD)
- dehydrogenase activities
- acute myeloid leukemia
- MTHFD2
- pharmacokinetic properties
- MOLM-14 acute myeloid leukemia cells
- cocrystal structure
- MTHFD1
- cyclohydrolase activities
- xenograft models
- flt3 internal tandem duplication mutations
- Inhibitor
- inhibitor
- inhibit