1. Anti-infection
    Cell Cycle/DNA Damage
    Apoptosis
  2. Arenavirus
    DNA/RNA Synthesis
    Apoptosis
    Caspase
    Bcl-2 Family
  3. AVN-944

AVN-944  (Synonyms: VX-944)

Cat. No.: HY-13560 Purity: 99.56%
COA Handling Instructions

AVN-944 (VX-944) is an orally active, potent, selective, noncompetitive and specific inhibitor of IMPDH (inosine monophosphate dehydrogenase). AVN-944 is an essential rate-limiting enzyme in de novo guanine nucleotide synthesis. AVN-944 is also an inhibitor of arenavirus RNA synthesis, and blocks arenavirus infection. AVN-944 has broad anti-cancer activities, and can be used for multiple myeloma (MM) and acute myeloid leukemia (AML) research.

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

AVN-944 Chemical Structure

AVN-944 Chemical Structure

CAS No. : 297730-17-7

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 158 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 158 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 144 In-stock
Estimated Time of Arrival: December 31
10 mg USD 228 In-stock
Estimated Time of Arrival: December 31
50 mg USD 900 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

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Description

AVN-944 (VX-944) is an orally active, potent, selective, noncompetitive and specific inhibitor of IMPDH (inosine monophosphate dehydrogenase). AVN-944 is an essential rate-limiting enzyme in de novo guanine nucleotide synthesis. AVN-944 is also an inhibitor of arenavirus RNA synthesis, and blocks arenavirus infection. AVN-944 has broad anti-cancer activities, and can be used for multiple myeloma (MM) and acute myeloid leukemia (AML) research[1][2][3].

In Vitro

AVN-944 (0-1 μM, 48 h) inhibits growth of human multiple myeloma (MM) cell lines in a dose-dependent manner[1].
AVN-944 (800 nM, 0-72 h) induces apoptosis in MM cell lines via a caspase-independent, Bax/AIF/Endo G pathway[1].
AVN-944 (0-200 nM) enhances the cytotoxicity of Doxorubicin (HY-15142A) and Melphalan (HY-17575)[1].
AVN-944 inhibits the proliferation of the human MV-4-11 and murine Ba/F3-Flt3-ITD-dependent cell lines with IC50 values of 26 and 30 nM, respectively[2].
AVN-944 (0-32 μM, 48 h) shows good activity against arenavirus infection at low doses (7.5 μM) with less cytotoxicity[3].
AVN-944 (0-6.4 μM, 48 h) does not reduce the viability of peripheral blood mononuclear cells (PBMNCs)[1].

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

Cell Proliferation Assay[1]

Cell Line: RPMI8226, MM.1S, and U266 cells
Concentration: 0, 100, 200, 300, 400, 600, 1000 nM
Incubation Time: 48 h
Result: Significantly inhibited the growth of RPMI8226, MM.1S, and U266 cells in a dose-dependent fashion, with 50% inhibition (IC50) values at 48 h of 450, 450, and 600 nM, respectively. Inhibited growth of drug-resistant cell lines, including Doxorubicin (Dox)-resistant RPMI8226-Dox40, Melphalan (Mel) resistant RPMI8226-LR5, and Dex (Dexamethasone) resistant MM.1R cells, with IC50 values similar to the parental drug-sensitive cell lines.

Apoptosis Analysis[1]

Cell Line: MM.1S and RPMI8226 cells
Concentration: 800 nM
Incubation Time: 48 and 72 h
Result: Induced apoptosis in MM cell lines.

Western Blot Analysis[1]

Cell Line: MM.1S and RPMI8226 cells
Concentration: 800 nM
Incubation Time: 12, 24, 48 h
Result: Induced modest cleavage of caspase 3, 8 and 9 in MM.1S cells and RPMI8226 cells. Markedly upregulated Bax and Bak, without significant changes in Bcl-2, Mcl-1, XIAP, and Bad. Observed translocation of mitochondrial proapoptotic proteins, apoptosis-inducing factor (AIF) and endonuclease G (Endo G) to cytosolic fractions.

Cell Cytotoxicity Assay[1]

Cell Line: MM.1S cells, MM.1S cells cultured with BMSCs
Concentration: 0, 50, 200 nM
Incubation Time: 24 h
Result: Enhanced the cytotoxicity of of Doxorubicin and Melphalan in MM.1S cells. Additive effects were also observed in MM.1S cells cultured with BMSCs derived from MM patient.
In Vivo

AVN-944 (0-150 mg/kg, Orally, twice daily) significantly increases the median survival time of leukemia model mice[2].

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

Animal Model: Balb/c mice (leukemia model, using Ba/F3 cells transduced with an activating human Flt-3 mutation injected into mice)[2]
Dosage: 75 or 150 mg/kg
Administration: Orally, twice daily
Result: Provided a significant increase in median survival time. Three of the 12 mice treated with 150 mg/kg AVN-944 were still alive on Day 35 when the study was terminated.
Clinical Trial
Molecular Weight

477.51

Formula

C25H27N5O5

CAS No.
SMILES

O=C(O[[email protected]@H](CC#N)CC)N[[email protected]](C1=CC=CC(NC(NC2=CC=C(C3=CN=CO3)C(OC)=C2)=O)=C1)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (209.42 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0942 mL 10.4710 mL 20.9420 mL
5 mM 0.4188 mL 2.0942 mL 4.1884 mL
10 mM 0.2094 mL 1.0471 mL 2.0942 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.56%

References
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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.

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Product Name:
AVN-944
Cat. No.:
HY-13560
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