AXL-IN-13_product_DataBase

Bioactivity	AXL-IN-13 is a potent and orally active AXL inhibitor (IC50: 1.6 nM, Kd: 0.26 nM). AXL-IN-13 reverses TGF-β1-induced epithelial-mesenchymal transition (EMT), and inhibits cancer cell migration and invasion[1].
Invitro	AXL-IN-13 (化合物 6li) 抑制 Ba/F3-TEL-AXL 细胞增殖，IC50 为 4.7 nM (通过 ELISA 测定)[1].AXL-IN-13 还显示对 CSF1R、FLT1/3/4、KLT、PDGFRB、TIE2 的结合亲和力[1]。AXL-IN-13 (0-500 nM，6 小时) 抑制 MDA-MB-231 和 4T1 细胞中 AXL 的磷酸化[1]。AXL-IN-13 (0-3 μM，3 天) 阻断 MDA-MB-231 细胞中 TGF-β1 (10 ng/mL) 诱导的 EMT[1]。AXL-IN-13 (0-3 μM，24 小时) 抑制 TGF-β1 (10 ng/mL) 诱导的 MDA-MB-231 细胞迁移和侵袭[1]。 Western Blot Analysis[1] Cell Line:
In Vivo	AXL-IN-13 (化合物 6li) (50 或 100 mg/kg，口服，14 天) 抑制 4T1 肿瘤生长和转移[1]。AXL-IN-13 (25 mg/kg, 口服) 显示出较好的 PK 曲线，AUC 为 8410.21 ng/mL/h，T1/2 值为 4.22 h，口服生物利用度 (F) 为 14.4%[1]。 Animal Model:
Name	AXL-IN-13
CAS	2376928-82-2
Formula	C34H41FN6O5
Molar Mass	632.72
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]. Chan S, et al. Discovery of 3-Aminopyrazole Derivatives as New Potent and Orally Bioavailable AXL Inhibitors. J Med Chem. 2022 Nov 24;65(22):15374-15390.

PeptideDB