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Picropodophyllin-d6
MCE 国际站:Picropodophyllin-d6
品牌:MedChemExpress (MCE)
货号:HY-15494S1
中文名称:苦鬼臼毒素-d6
Synonyms:苦鬼臼毒素-d6
AXL1717-d6
Picropodophyllotoxin-d6
PPP-d6
存储条件:请将产品存放在分析证书上推荐的条件下。
运输条件:美国大陆的室温;其他地方可能有所不同。
产品活性:Picropodophyllin-d6 (AXL1717-d6) 是 Picropodophyllin 氘代物。Picropodophyllin (AXL1717) 是选择性的胰岛素样生长因子-1受体 (IGF-1R)抑制剂,IC50 为1 nM。
体外:氢、碳和其他元素的稳定重同位素已被整合到药物分子中,主要用作药物开发过程中定量的示踪剂。氘化因其可能影响药物的药代动力学和代谢特征而受到关注[1]。MCE 尚未独立证实这些方法的准确性。它们仅供参考。
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参考文献:
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019
53(2):211-216.
[2]. Girnita A, et al. Cyclolignans as inhibitors of the insulin-like growth factor-1 receptor and malignant cell growth. Cancer Res. 2004 Jan 1
64(1):236-42.
[3]. Menu E, et al. Inhibiting the IGF-1 receptor tyrosine kinase with the cyclolignan PPP: an in vitro and in vivo study in the 5T33MM mouse model. Blood. 2006 Jan 15
107(2):655-60. Epub 2005 Jul 26.
[4]. Bieghs L, et al. The IGF-1 receptor inhibitor picropodophyllin potentiates the anti-myeloma activity of a BH3-mimetic. Oncotarget. 2014 Nov 30
5(22):11193-208.
[5]. Tomizawa M, et al. Picropodophyllin and sorafenib synergistically suppress the proliferation and motility of hepatocellular carcinoma cells. Oncol Lett. 2014 Nov
8(5):2023-2026. Epub 2014 Aug 27.
[6]. Stromberg T, et al. IGF-1 receptor tyrosine kinase inhibition by the cyclolignan PPP induces G2/M-phase accumulation and apoptosis in multiple myeloma cells. Blood. 2006 Jan 15
107(2):669-78. Epub 2005 Sep 15.
[7]. Kong YL, et al. Insulin deficiency induces rat renal mesangial cell dysfunction via activation of IGF-1/IGF-1R pathway. Acta Pharmacol Sin. 2016 Feb
37(2):217-27.