2. Metabolic Enzyme/Protease
  3. Dihydrofolate reductase (DHFR)
  4. 5-Monobutyl methotrexate

5-Monobutyl methotrexate  (Synonyms: NSC 305986; γ-MBMTX)

Cat. No.: HY-137357
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5-Monobutyl methotrexate (NSC 305986; γ-MBMTX) is a dihydrofolate reductase (DHFR) inhibitor and esterase substrate. 5-Monobutyl methotrexate is hydrolyzed by esterases to produce methotrexate. In rhesus monkeys, 5-Monobutyl methotrexate clears more slowly from cerebrospinal fluid than from serum, and its serum protein binding rate exceeds 99%. At the same dose rate, 5-Monobutyl methotrexate achieves cerebrospinal fluid concentrations comparable to those of Methotrexate (HY-14519), and exhibits activity against Methotrexate-resistant cells (with transport defects) that is comparable to that against sensitive parental cells. 5-Monobutyl methotrexate can be used in studies related to Methotrexate-resistant tumors.

For research use only. We do not sell to patients.

5-Monobutyl methotrexate

5-Monobutyl methotrexate Chemical Structure

CAS No. : 66147-31-7

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5-Monobutyl methotrexate Related Antibodies

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Description

5-Monobutyl methotrexate (NSC 305986; γ-MBMTX) is a dihydrofolate reductase (DHFR) inhibitor and esterase substrate. 5-Monobutyl methotrexate is hydrolyzed by esterases to produce methotrexate. In rhesus monkeys, 5-Monobutyl methotrexate clears more slowly from cerebrospinal fluid than from serum, and its serum protein binding rate exceeds 99%. At the same dose rate, 5-Monobutyl methotrexate achieves cerebrospinal fluid concentrations comparable to those of Methotrexate (HY-14519), and exhibits activity against Methotrexate-resistant cells (with transport defects) that is comparable to that against sensitive parental cells. 5-Monobutyl methotrexate can be used in studies related to Methotrexate-resistant tumors[1].

In Vitro

The binding rate of 5-Monobutyl methotrexate (74-290 μM; MeOH extract) to rhesus monkey serum albumin exceeds 99% at total concentrations of 74, 130, and 290 μM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

5-Monobutyl methotrexate Related Antibodies
In Vivo

5-Monobutyl methotrexate (γ-MBMTX) (27 mg, 10 g/m2; intravenous injection; single administration) remains relatively stable in rhesus monkeys, with only Methotrexate (HY-14519) as the major metabolite. The serum protein binding rate of 5-Monobutyl methotrexate is >99%. At an equivalent dose rate, it achieves a CSF concentration comparable to that of Methotrexate, and its efflux rate from CSF is slower than that from serum, with the CSF/serum ratio increasing over time[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Macaca mulatta (adult, 10-15 kg, male and female)[1]
Dosage: 27 mg (bolus); 10 g/m2 (1.25-hour infusion); 10 g/m2 (4-hour infusion)
Administration: i.v. (bolus over 1-2 minutes); i.v. (infusion over 1.25 hours); i.v. (infusion over 4 hours)
Result: Accounted for 67%-94% of total serum radioactivity for up to 60 min, with [3H]MTX comprising 4%-13% and only traces of other products after intravenous bolus.
Reached approximately equal proportions with MTX in serum at 2 h after intravenous bolus.
Was the major species in urine over 60 minutes and up to 4 hours, declining from 95% to 54% of total urinary radioactivity, while MTX increased to 31% and other products increased to 15% after intravenous bolus.
Reached free serum level of 1×10-4 M at end of 1.25-h infusion, declining to 7×10-6 M over 5 h.
Peaked at 1.5×10-5 M in CSF after 1.25-h infusion, with CSF/serum ratios increasing from 0.15 at 2 h post-infusion to 1.0 at 5 h post-infusion.
Showed free serum MTX ranging from 1×10-5 M to 4.8×10-6 M over 5 h, with CSF MTX ranging from 4.7×10-6 M to 7.5×10-6 M, and CSF/serum MTX ratios consistently above 0.5 after 1.25-hour infusion.
Remained detectable in serum at 24 hours, with MTX present in CSF at 24 hours (≈4×10-6 M) after 1.25-hour infusion.
Had free serum levels roughly 50% lower than after 1.25-hour infusion at corresponding time points after 4-hour infusion.
Showed CSF levels following a similar lower pattern to serum after 4-hour infusion, with CSF/serum ratios increasing from 0.18 at end of infusion to 1.2 at 3 hours post-infusion.
Was below 1×10-6 M in free serum at 24 hours, while remaining above 4×10-6 M in CSF after 4-hour infusion.
Showed free serum MTX peaking at 5.4×10-4 M at 2 hours post-infusion, with MTX undetectable in CSF (<1×10-6 M) at all time points after 4-hour infusion.
Molecular Weight

510.55

Formula

C24H30N8O5
CAS No.
SMILES

NC1=NC(N)=NC(N=C2)=C1N=C2CN(C(C=C3)=CC=C3C(N[C@H](C(O)=O)CCC(OCCCC)=O)=O)C
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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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5-Monobutyl methotrexate 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:

5-Monobutyl methotrexate66147-31-7NSC 305986 γ-MBMTXNSC305986NSC-305986Dihydrofolate reductase (DHFR)esterasesmethotrexate-resistant cellsserum proteinsmtx-resistant tumorscerebrospinal fluiddihydrofolate reductaseserumRhesus monkeysmethotrexate-sensitive parent cellsInhibitorinhibitorinhibit

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