-
AVN-944
- names:
(R)-1-cyanobutan-2-yl ((S)-1-(3-(3-(3-methoxy-4-(oxazol-5-yl)phenyl)ureido)phenyl)ethyl)carbamate
- CAS号:
297730-17-7
MDL Number: - MF(分子式): C25H27N5O5 MW(分子量): 477.51
- EINECS: Reaxys Number:
- Pubchem ID: Brand:BIOFOUNT
货品编码 | 规格 | 纯度 | 价格 (¥) | 现价(¥) | 特价(¥) | 库存描述 | 数量 | 总计 (¥) |
---|
中文别名 | AVN-944 |
英文别名 | AVN 944; AVN-944; AVN944; VX944; VX 944; VX-944. |
CAS号 | 297730-17-7 |
SMILES | 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 |
Inchi | InChI=1S/C25H27N5O5/c1-4-20(10-11-26)35-25(32)28-16(2)17-6-5-7-18(12-17)29-24(31)30-19-8-9-21(22(13-19)33-3)23-14-27-15-34-23/h5-9,12-16,20H,4,10H2,1-3H3,(H,28,32)(H2,29,30,31)/t16-,20+/m0/s1 |
InchiKey | GYCPCOJTCINIFZ-OXJNMPFZSA-N |
分子式 Formula | C25H27N5O5 |
分子量 Molecular Weight | 477.51 |
闪点 FP | |
熔点 Melting point | |
沸点 Boiling point | |
Polarizability极化度 | |
密度 Density | |
蒸汽压 Vapor Pressure | |
溶解度Solubility | |
性状 | Solid powder |
储藏条件 Storage conditions | Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years). |
产品说明 | AVN-944(CAS:297730-17-7):仅限应用于工业或者科学研究过程中非医疗目的,不应用于人类或动物的临床诊断以及治过程疗,该产品非药用,非食用。 |
Introduction | AVN-944 (VX-944) is an orally available, synthetic small molecule with potential antineoplastic activity. AVN944 inhibits inosine monosphosphate dehydrogenase (IMPDH), an enzyme involved in the de novo synthesis of guanosine triphosphate (GTP), a purine molecule required for DNA and RNA synthesis. Inhibition of IMPDH deprives cancer cells of GTP, resulting in disruption of DNA and RNA synthesis, inhibition of cell proliferation, and the induction of apoptosis. AVN944 appears to have a selective effect on cancer cells in that deprivation of GTP in normal cells results in a temporary slowing of cell growth only. IMPDH is overexpressed in some cancer cells, particularly in hematological malignancies. |
Application1 | |
Application2 | |
Application3 |
[1]Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2009 Mar;31(2):107-46. PubMed PMID: 19455266. |
[2]Huang M, Itahana K, Zhang Y, Mitchell BS. Depletion of guanine nucleotides leads to the Mdm2-dependent proteasomal degradation of nucleostemin. Cancer Res. 2009 Apr 1;69(7):3004-12. doi: 10.1158/0008-5472.CAN-08-3413. Epub 2009 Mar 24. PubMed PMID: 19318567. |
[3] Hamilton JM, Harding MW, Genna T, Bol DK. A phase I dose-ranging study of the pharmacokinetics, pharmacodynamics, safety, and tolerability of AVN944, an IMPDH inhibitor, in healthy male volunteers. J Clin Pharmacol. 2009 Jan;49(1):30-8. doi: 10.1177/0091270008325149. Epub 2008 Oct 29. PubMed PMID: 18971325. |
[4] Floryk D, Thompson TC. 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. doi: 10.1002/ijc.23788. PubMed PMID: 18712736; PubMed Central PMCID: PMC2887704. |
[5] Chen L, Pankiewicz KW. Recent development of IMP dehydrogenase inhibitors for the treatment of cancer. Curr Opin Drug Discov Devel. 2007 Jul;10(4):403-12. Review. PubMed PMID: 17659481. |
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