AXL-IN-13

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AXL-IN-13 是一种有效的、具有口服活性的 AXL 抑制剂 (IC50: 1.6 nM，Kd : 0.26 nM)。AXL-IN-13 逆转 TGF-β1 诱导的上皮间质转化 (EMT)，并抑制癌细胞迁移和侵袭。

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.

Western Blot Analysis Cell Line:MDA-MB-231 cells Concentration:0, 0.11, 0.33, 1, 3 μM.Incubation Time:3 daysResult:Restored the protein levels of E-cadherin and N-cadherin to control levels.Cell Migration Assay 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.

Animal Model:Xenograft model derived from highly metastatic 4T1 cells.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 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).

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Angiogenesis

FLT

FLT | PDGFR | TGF-beta/Smad | TAM Receptor

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2376928-82-2

632.72

C34H41FN6O5

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (158.05 mM; 超声助溶 )

O(C=1C2=C(C=C(OCCCN3CCOCC3)C(OC)=C2)N=CC1)C4=C(F)C=C(NC=5C(C(NC6CCCCC6)=O)=CN(C)N5)C=C4

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(-20℃)

With Ice Pack

≥ 2 years