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.
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- CAS No.: 3068001-31-7
- 화학식: C17H18ClN7O7
- 분자량:467.82
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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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.
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Animal Model:NOD/SCID (female, 9-10 weeks old)[1]
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Dosage:15 mg/kg
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Administration:i.v.; once daily
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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
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CAS No. 3068001-31-7
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분자량 467.82
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화학식 C17H18ClN7O7
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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
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MTHFD2-IN-5 Related Classifications
HY-170361 Related Classifications
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- 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