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.
For research use only. We do not sell to patients.
- CAS No.: 3068001-31-7
- Formula: C17H18ClN7O7
- Molecular Weight:467.82
-
Storage:
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]
-
Biological Activity
-
Chemical Information
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
MTHFD2 66 nM (IC50) |
MTHFD1 1790 nM (IC50) |
In Vitro
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. Further protocols information, click here.
Parmacokinetics
| 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 |
In Vivo
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
-
Molecular Weight 467.82
-
Formula 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
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
-
Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MTHFD2-IN-5 Related Classifications
HY-170361 Related Classifications
Powered by Bioz
Keywords
- 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