| Company Name: |
Shanghai YuanYe Biotechnology Co., Ltd.
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| Tel: |
021-61312847; 18021002903 |
| Email: |
3008007409@qq.com |
| Products Intro: |
Product Name:2376928-82-2
CAS:2376928-82-2
Package:10mg Remarks:V38509
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| Company Name: |
Shanghai Yifei Biotechnology Co. , Ltd.
|
| Tel: |
021-65675885 18964387627 |
| Email: |
customer_service@efebio.com |
| Products Intro: |
Product Name:AXL-IN-13
CAS:2376928-82-2
Purity:99% Package:1mg;5mg;10mg
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1H-Pyrazole-4-carboxamide, N-cyclohexyl-3-[[3-fluoro-4-[[6-methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinolinyl]oxy]phenyl]amino]-1-methyl- manufacturers
- AXL-IN-13
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- $79.00
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2026-05-11
- CAS:2376928-82-2
- Purity: 99.95%
- Supply Ability: 10g
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| | 1H-Pyrazole-4-carboxamide, N-cyclohexyl-3-[[3-fluoro-4-[[6-methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinolinyl]oxy]phenyl]amino]-1-methyl- Basic information |
| | 1H-Pyrazole-4-carboxamide, N-cyclohexyl-3-[[3-fluoro-4-[[6-methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinolinyl]oxy]phenyl]amino]-1-methyl- Chemical Properties |
| Boiling point | 795.4±60.0 °C(Predicted) | | density | 1.33±0.1 g/cm3(Predicted) | | pka | 14.15±0.20(Predicted) | | form | Solid | | color | Off-white to light yellow |
| | 1H-Pyrazole-4-carboxamide, N-cyclohexyl-3-[[3-fluoro-4-[[6-methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinolinyl]oxy]phenyl]amino]-1-methyl- Usage And Synthesis |
| Uses | 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]. | | in vivo | AXL-IN-13 (compound 6li) (50 or 100 mg/kg, p.o, 14 days) inhibits 4T1 tumor growth and metastasis[1].
AXL-IN-13 (25 mg/kg, p.o.) displays reasonable PK profiles with an AUC of 8410.21 ng/mLh, a T1/2 value of 4.22 h, and an oral bioavailability (F) of 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.
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| 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 |
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| | IC 50 | Axl; PDGFRβ: 2.3 nM (Kd) | | References | [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. DOI:10.1021/acs.jmedchem.2c01346 |
| | 1H-Pyrazole-4-carboxamide, N-cyclohexyl-3-[[3-fluoro-4-[[6-methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinolinyl]oxy]phenyl]amino]-1-methyl- Preparation Products And Raw materials |
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