| Bioactivity | Bemcentinib (R428) GMP is an orally active and selective inhibitor of Axl with an IC50 of 14 nM[1][2]. |
| Target | IC50: 14 nM (Axl kinase). |
| Invitro | Bemcentinib (R428) (2 μM) 显著干扰Axlpos黑色素瘤细胞的迁移和侵袭机制，其水平与Axl敲低相当[1]。Bmcentinib (R428)协同CDDP增强肝脏微转移抑制作用[2]。Bmcentinib (R428) (50 nM-1 μM)可引起前脂肪细胞向成熟脂肪细胞分化的浓度依赖性抑制，这可以通过降低脂质摄取得到证明[3]。 0 --> Bemcentinib (GMP) 相关抗体: |
| In Vivo | Bemcentinib (R428) (125 mg/kg, p.o.) 显著阻断MDA-MB-231-luc-D3H2LN在两种独立小鼠乳腺癌扩散模型中的转移发展，抑制肿瘤血管生成和血管内皮生长因子(VEGF)诱导的角膜新生血管生成[2].Bemcentinib (R428) (75 mg/kg/day, 25 mg/kg twice daily, p.o.) 让老鼠保持高脂肪饮食导致体重增加和皮下和性腺脂肪量显著减少[3]。 |
| Name | Bemcentinib (GMP) |
| CAS | 1037624-75-1 |
| Formula | C30H34N8 |
| Molar Mass | 506.64 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Sensi M, et al. Human cutaneous melanomas lacking MITF and melanocyte differentiation antigens express a functional Axl receptor kinase. J Invest Dermatol. 2011 Dec;131(12):2448-57. [2]. Holland SJ, et al. R428, a selective small molecule inhibitor of Axl kinase, blocks tumor spread and prolongs survival in models of metastatic breast cancer. Cancer Res. 2010 Feb 15;70(4):1544-54. [3]. Lijnen HR, et al. Growth arrest-specific protein 6 receptor antagonism impairs adipocyte differentiation and adipose tissue development in mice. J Pharmacol Exp Ther. 2011 May;337(2):457-64. |