Picropodophyllin (AXL1717) 是选择

Picropodophyllin (AXL1717) is a selective insulin-like growth factor-1 receptor (IGF-1R) inhibitor with an IC₅₀ of 1 nM.

IC50: 1 nM (IGF-1R)

Picropodophyllin (AXL1717) (0.5、2.5、10 μM) 有效抑制完整细胞中 IGF-1 刺激的 IGF-1R、Akt (Ser 473) 和 Erk1/2 磷酸化。Picropodophyllin (AXL1717) 还可抑制细胞生长，并诱导培养的 IGF-1R 阳性肿瘤细胞发生细胞凋亡^[1]。
Picropodophyllin (AXL1717) 通过进一步降低细胞活力和增强细胞凋亡，使 HMCL、原代人 MM 和小鼠 5T33MM 细胞对 ABT-737 和 ABT-199 协同敏感^[3]。
Picropodophyllin 和索拉非尼协同抑制肝癌细胞的增殖和运动^[4]。

Picropodophyllin (AXL1717) (20 mg/kg/12 小时，腹腔注射) 在异种移植了人 ES-1、BE 和 PC3 的 SCID 小鼠中引起肿瘤完全消退^[1]。
Picropodophyllin (AXL1717) 在 5T33MM 小鼠模型中显示出有效的抗肿瘤活性，可提高存活率^[2]。

414.41

C₂₂H₂₂O₈

固体

White to off-white

苦鬼臼毒素

• Phenylpropanoids
• Lignans

• 植物
• 小檗科
• 八角莲

Room temperature in continental US; may vary elsewhere.

• [1]. 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.  [Content Brief]

  [2]. 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.  [Content Brief]

  [3]. 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.  [Content Brief]

  [4]. 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.  [Content Brief]

  [5]. 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.  [Content Brief]

  [6]. 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.  [Content Brief]