2376928-82-2
2376928-82-2 structure
- Name: AXL-IN-13
- Chemical Name: AXL-IN-13
- CAS Number: 2376928-82-2
- Molecular Formula: C34H41FN6O5
- Molecular Weight: 632.72
- Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK FLT3
- Create Date: 2023-01-15 12:31:13
- Modify Date: 2024-04-09 10:10:32
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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].
| Name | AXL-IN-13 |
|---|
| Description | 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]. |
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| Related Catalog | |
| Target |
PDGFRβ:2.3 nM (Kd) |
| In Vitro | 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: MDA-MB-231 cells Concentration: 0, 0.11, 0.33, 1, 3 μM. Incubation Time: 3 days Result: Restored the protein levels of E-cadherin and N-cadherin to control levels. Cell Migration Assay [1] Cell Line: MDA-MB-231 cell Concentration: 0, 0.11, 0.33, 1, 3 μM. Incubation Time: 24 h Result: Inhibited cell migration at 1 and 3 μM. Inhibited the invasion of MDA-MB-231 cells by 22.6, 34.8, 56.5, and 70.4% at the concentrations of 0.11, 0.33, 1.0, and 3.0 μM, respectively. |
| 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: Xenograft model derived from highly metastatic 4T1 cells.[1] Dosage: 50 or 100 mg/kg Administration: Oral administration (p.o.) Result: Suppressed 4T1 tumor growth with a tumor growth inhibition (TGI) of 78.0 and 95.9% at 50 and 100 mg/kg, respectively. Inhibited the phosphorylation of AXL. Showed that liver is one of the most common sites of breast cancer metastasis. Animal Model: Rats[1] Dosage: 5 mg/kg (i.v.), 25 mg/kg (p.o.) Administration: Intravenous injection (i.v.), oral administration (p.o.) Result: Pharmacokinetic parameters of AXL-IN-13 (Compound 6li). parameters T1/2 (h) Cmax (ng/mL) AUClast F (%) 5 mg/kg (i.v.) 3.31 12280.44 11684.24 25 mg/kg (p.o.) 4.22 887.75 8410.21 14.4 |
| References |
| Molecular Formula | C34H41FN6O5 |
|---|---|
| Molecular Weight | 632.72 |