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AVN-944 (Synonyms: VX-944) 纯度: 99.56%
AVN-944(VX-944)是选择性非竞争性IMPDH抑制剂,对IMPDH1和IMPDH2的Ki值为6-10nMIMPDH。
AVN-944 Chemical Structure
CAS No. : 297730-17-7
规格 | 价格 | 是否有货 | 数量 |
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10 mM * 1 mL in DMSO | ¥1786 | In-stock | |
2 mg | ¥1133 | In-stock | |
5 mg | ¥1700 | In-stock | |
10 mg | ¥2450 | In-stock | |
50 mg | ¥7500 | In-stock | |
100 mg | 询价 | ||
200 mg | 询价 |
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AVN-944 相关产品
•相关化合物库:
- Covalent Screening Library Plus
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- Clinical Compound Library Plus
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- Anti-Cancer Compound Library
- Clinical Compound Library
- Drug Repurposing Compound Library
- Covalent Screening Library
- Targeted Diversity Library
生物活性 |
AVN-944(VX-944) is a selective, noncompetitive inhibitor of the enzyme directed against human IMPDH with Ki of 6-10 nM for IMPDH1/IMPDH2. IC50 value: 6-10 nM (Ki) [1] Target: IMPDH in vitro: AVN-944 strikingly inhibit RNA synthesis within 2 h of exposure. Depletion of guanine nucleotides by MPA and AVN-944 also causes an early and near-complete reduction in levels of the 45S precursor rRNA synthesis and the concomitant translocation of nucleolar proteins including nucleolin, nucleophosmin, and nucleostemin from the nucleolus to the nucleoplasm [2]. AVN944 induced caspase-dependentand caspase-independent cell death in LNCaP, CWR22Rv1, and DU145 cells. AVN944 induced expression of p53-target proteins Bok, Bax and Noxa in androgen-responsive cell lines and suppressed expression of survivin in prostate cancer cells regardless of their androgen sensitivity. AVN944 also induced differentiation of androgen-independent prostate cancer cells as indicated by morphological changes and increased expression of genes coding for prostasomal proteins, keratins and other proteins, including tumor suppressor genes MIG-6 and NDRG1. AVN944-differentiated androgen-independent DU145 and PC-3 cells are sensitized to TRAIL-induced apoptosis as demonstrated by induction of caspases and PARP cleavage [3]. |
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Clinical Trial |
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分子量 |
477.51 |
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Formula |
C25H27N5O5 |
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CAS 号 |
297730-17-7 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : 100 mg/mL (209.42 mM; Need ultrasonic) 配制储备液
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
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参考文献 |
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