2. Metabolic Enzyme/Protease
  3. Methylenetetrahydrofolate Dehydrogenase (MTHFD)
  4. 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.

MTHFD2-IN-5

MTHFD2-IN-5 Chemical Structure

CAS No. : 3068001-31-7

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MTHFD2-IN-5 Related Antibodies

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Description

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[1].

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.

MTHFD2-IN-5 Related Antibodies
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

Compound 16e (MTHFD2-IN-5) (15 mg/kg; intravenous injection; once daily) exhibits potent in vivo anti-tumor activity in MOLM-14 xenograft mice without inducing significant body weight changes[1].

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.
Molecular Weight

467.82

Formula

C17H18ClN7O7
CAS No.
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.
Purity & Documentation
References
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MTHFD2-IN-5 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MTHFD2-IN-53068001-31-7Methylenetetrahydrofolate Dehydrogenase (MTHFD)dehydrogenase activitiesacute myeloid leukemiaMTHFD2pharmacokinetic propertiesMOLM-14 acute myeloid leukemia cellscocrystal structureMTHFD1cyclohydrolase activitiesxenograft modelsflt3 internal tandem duplication mutationsInhibitorinhibitorinhibit

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