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AXL-IN-13

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

CAS号

2376928-82-2

分子式

C34H41FN6O5

主要靶点

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

仅限科研使用

Cat No : CM07021

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Synonyms

验证数据展示

  • CAS No.: 2376928-82-2

    AXL-IN-13
    CAS#: 2376928-82-2

产品信息

AXL-IN-13 is a potent and orally active AXL inhibitor with an IC50 value of 1.6 nM and a Kd value of 0.26 nM.AXL-IN-13 exhibits anticancer activity, reverses TGF-β1-induced epithelial-mesenchymal transition (EMT) and inhibits cancer cell migration and invasion.

CAS号 2376928-82-2
分子式 C34H41FN6O5
主要靶点 TGF-beta/Smad|FLT|TAM Receptor|PDGFR
主要通路 干细胞|蛋白酪氨酸激酶|血管生成
分子量 632.72
纯度 99.38%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件
别名

靶点活性

AXL:1.6 nM|PDGFRβ:2.3 nM (Kd)

体内活性

AXL-IN-13 (Compound 6li) (50 or 100 mg/kg; p.o.; 14 days; Xenograft model derived from highly metastatic 4T1 cells) inhibits 4T1 tumor growth and metastasis.[1] AXL-IN-13 (25 mg/kg; oral; Xenograft model derived from highly metastatic 4T1 cells) shows a good PK curve, with an AUC of 8410.21 ng/mL/h, a T1/2 value of 4.22 h, and an oral bioavailability (F) of 14.4%.[1]

体外活性

AXL-IN-13 (Compound 6li) inhibits Ba/F3-TEL-AXL cell proliferation with an IC50 of 4.7 nM (as determined by ELISA).[1] AXL-IN-13 (0-500 nM; 6 hours) inhibits AXL phosphorylation in MDA-MB-231 and 4T1 cells.[1] AXL-IN-13 also shows binding affinity for CSF1R, FLT1/3/4, KLT, PDGFRB, TIE2.[1] AXL-IN-13 (0-3 μM; 3 days) blocks TGF-β1 (10 ng/mL)-induced EMT in MDA-MB-231 cells.[1] AXL-IN-13 (0-3 μM; 24 hours) inhibits TGF-β1 (10 ng/mL)-induced migration and invasion of MDA-MB-231 cells.[1]

参考文献

1.Chan S, et al. Discovery of 3-Aminopyrazole Derivatives as New Potent and Orally Bioavailable AXL Inhibitors. J Med Chem. 2022;65(22):15374-15390.

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