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Chemical Structure| 297730-17-7 Chemical Structure| 297730-17-7

Structure of AVN-944
CAS No.: 297730-17-7

Chemical Structure| 297730-17-7

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AVN-944 is a selective, noncompetitive inhibitor of the enzyme directed against human IMPDH with Ki of 6-10 nM for IMPDH1/IMPDH2.

Synonyms: VX-944

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Product Details of AVN-944

CAS No. :297730-17-7
Formula : C25H27N5O5
M.W : 477.51
SMILES Code : O=C(O[C@H](CC)CC#N)N[C@H](C1=CC=CC(NC(NC2=CC=C(C3=CN=CO3)C(OC)=C2)=O)=C1)C
Synonyms :
VX-944
MDL No. :MFCD22200574
InChI Key :GYCPCOJTCINIFZ-OXJNMPFZSA-N
Pubchem ID :9918559

Safety of AVN-944

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of AVN-944

DNA
pyroptosis

Isoform Comparison

Biological Activity

Description
AVN-944 (also known as VX-944) is an orally active, potent, selective, noncompetitive, and specific inhibitor of IMPDH (inosine monophosphate dehydrogenase). IMPDH is an essential rate-limiting enzyme in de novo guanine nucleotide synthesis. Additionally, AVN-944 acts as an inhibitor of arenavirus RNA synthesis, blocking arenavirus infection. It exhibits broad anti-cancer activities and is applicable to research on multiple myeloma (MM) and acute myeloid leukemia (AML) [1][2][3].

In Vitro:

Cell Line
Concentration Treated Time Description References
K562 cells 1 µM 8 to 24 h To study the effect of MG132 on AVN-944-induced nucleostemin degradation, results showed that MG132 almost completely prevented the loss of nucleostemin protein. Cancer Res. 2009 Apr 1;69(7):3004-12
U2OS cells 1 µM 8 to 24 h To study the effect of AVN-944 on nucleostemin protein, results showed that the degradation of nucleostemin protein could be reversed by withdrawal of AVN-944 and addition of guanosine. Cancer Res. 2009 Apr 1;69(7):3004-12
NB4 cells 1 µM 4 to 24 h To study the effect of AVN-944 on nucleolar protein nucleostemin, results showed that nucleostemin protein was reduced at 4 hours and nearly absent at 8 hours, while nucleophosmin and nucleolin protein levels remained unchanged. Cancer Res. 2009 Apr 1;69(7):3004-12
PC-3 cells 5 μM 3 days AVN944 inhibited proliferation of PC-3 cells and induced S-phase cell cycle block. Int J Cancer. 2008 Nov 15;123(10):2294-302
DU145 cells 5 μM 3 days AVN944 inhibited proliferation of DU145 cells and induced S-phase cell cycle block. Int J Cancer. 2008 Nov 15;123(10):2294-302
CWR22Rv1 cells 5 μM 3 days AVN944 inhibited proliferation of CWR22Rv1 cells and induced S-phase cell cycle block. Int J Cancer. 2008 Nov 15;123(10):2294-302
LNCaP cells 5 μM 3 days AVN944 inhibited proliferation of LNCaP cells and induced G1 phase cell cycle arrest. Int J Cancer. 2008 Nov 15;123(10):2294-302
Vero76 cells 7.5 μM 48 h To evaluate the inhibitory effect of AVN-944 on Tacaribe virus infection, results showed that 7.5 μM AVN-944 significantly reduced virus titers (>90%) with minimal cytotoxicity. Antiviral Res. 2018 Sep;157:140-150
BSR-T7/5 cells 1.6 μM 48 h To evaluate the inhibitory effect of AVN-944 on viral RNA synthesis, results showed that 1.6 μM AVN-944 significantly reduced reporter activity to background levels with no pronounced cytotoxicity. Antiviral Res. 2018 Sep;157:140-150
16HBE cells 0.18 μM 72 h Inhibited NC H1N1 virus replication with EC50 of 0.18 μM J Virol. 2020 Mar 17;94(7):e02149-19
MDCK cells 0.21 μM 48 h Inhibited BIRFLU virus replication with EC50 of 0.21 μM J Virol. 2020 Mar 17;94(7):e02149-19
Human A549 cells 0.07 μM (GFP), 0.13 μM (Scarlet) 24 h To evaluate the inhibitory activity of AVN-944 against recombinant vaccinia virus (rVACV). Results showed that AVN-944 significantly inhibited rVACV with low EC50 values. Microbiol Spectr. 2023 Aug 17;11(4):e0474522

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.09mL

0.42mL

0.21mL

10.47mL

2.09mL

1.05mL

20.94mL

4.19mL

2.09mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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