AVN944 free base · Synonyms: VX-944

AVN-944 is an orally active, potent, selective, noncompetitive and specific inhibitor of IMPDH.

For research use only. Not for human or veterinary use.

Target Arenavirus DNA/RNA Synthesis Apoptosis Caspase Bcl-2 Family

Research area Infection Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

AVN944 structure

CAS No.: 297730-17-7

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 420.00	BP-02481-100mg	In stock	Get quote
250 mg	USD 840.00	BP-02481-250mg	In stock	Get quote
500 mg	USD 1,340.00	BP-02481-500mg	In stock	Get quote
1 g	USD 2,150.00	BP-02481-1g	In stock	Get quote
2 g	USD 3,440.00	BP-02481-2g	In stock	Get quote
3 g	USD 4,128.00	BP-02481-3g	In stock	Get quote
5 g	USD 5,500.00	BP-02481-5g	In stock	Get quote

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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 .

Biological activity

In Vitro AVN-944 (0-1 μM, 48 h) inhibits growth of human multiple myeloma (MM) cell lines in a dose-dependent manner. AVN-944 (800 nM, 0-72 h) induces apoptosis in MM cell lines via a caspase-independent, Bax/AIF/Endo G pathway. AVN-944 (0-200 nM) enhances the cytotoxicity of Doxorubicin (HY-15142A) and Melphalan (HY-17575). 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. AVN-944 (0-32 μM, 48 h) shows good activity against arenavirus infection at low doses (7.5?μM) with less cytotoxicity. AVN-944 (0-6.4 μM, 48 h) does not reduce the viability of peripheral blood mononuclear cells (PBMNCs). In Vivo AVN-944 (0-150 mg/kg, Orally, twice daily) significantly increases the median survival time of leukemia model mice.

Identifiers

SMILES: CC[C@H](CC#N)OC(=O)N[C@@H](C)C1=CC=CC(NC(=O)NC2=CC=C(C3=CN=CO3)C(OC)=C2)=C1
InChIKey: GYCPCOJTCINIFZ-OXJNMPFZSA-N

Specifications

MW (average): 477.5124
Formula: C₂₅H₂₇N₅O₅
CAS No.: 297730-17-7
Physical state: Solid
Color: White to light yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 1 year;

Solubility

Soluble in DMSO

Documents

References

[1].Zimmermann AG, et al. Inosine-5'-monophosphate dehydrogenase: regulation of expression and role in cellular proliferation and T lymphocyte activation. Prog Nucleic Acid Res Mol Biol. 1998;61:181-209.

[2].Huang M, et al. Guanine nucleotide depletion inhibits pre-ribosomal RNA synthesis and causes nucleolar disruption. Leuk Res. 2008 Jan;32(1):131-41.

[3].Floryk D, et al. Antiproliferative effects of AVN944, a novel inosine 5-monophosphate dehydrogenase inhibitor, in prostate cancer cells. Int J Cancer. 2008 Nov 15;123(10):2294-302.

Same target

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Same research area

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