2. Protein Tyrosine Kinase/RTK
  3. TAM Receptor
  4. Axl-IN-17

Axl-IN-17 (compound 13c) is an orally active, selective AXL inhibitor with an IC50 value of 3.2 nM. Axl-IN-17 reveals antitumor efficacy.

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Axl-IN-17 Chemical Structure

Axl-IN-17 Chemical Structure

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Axl-IN-17 Related Antibodies

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Description

Axl-IN-17 (compound 13c) is an orally active, selective AXL inhibitor with an IC50 value of 3.2 nM. Axl-IN-17 reveals antitumor efficacy[1].

IC50 & Target

Axl

3.23 nM (IC50)

Mer

 

Tyro3

 

In Vitro

Axl-IN-17 inhibits cancer-related kinases TYRO3, MER, MET, RON at 1 μM[1].
Axl-IN-17 exhibits antiproliferative activities in BaF3/TEL-AXL cell, with IC50 value <1 nM[1].
Axl-IN-17 (1 nM, 2 h) inhibits phosphorylation of AXL and its downstream signaling[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Axl-IN-17 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: BaF3/TEL-AXL
Concentration: 1 nM
Incubation Time: 72 h
Result: Inhibited proliferation activity in BaF3/TEL-AXL cells.

Western Blot Analysis[1]

Cell Line: BaF3/TEL-AXL
Concentration: 1 nM
Incubation Time: 2 h
Result: Inhibited phosphorylation of AXL and its downstream signaling
In Vivo

Axl-IN-17 (p.o.,3 mg/kg, once daily) reveals a T1/2 value of 10.09 h and an AUC value of 59815 ng•h/mL in pharmacokinetic study[1].
Axl-IN-17 (p.o.,25, 50 or 100 mg/kg, once daily for 7 days) exhibits antitumor efficacy in AXL-driven tumor xenograft mice[1].

Pharmacokinetic Analysis of AXL-IN-17 in Male Sprague-Dawley rats[1]

Route Dose (mg/kg) AUC0→∞ (ng·h/mL) T1/2 (h) Tmax (h) Cmax (ng/mL) MRT0→∞(h)
p.o. 3 mg/kg 59815 10.09 2 2906 16.5

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats /pharmacokinetic[1]
Dosage: 3 mg/kg (p.o.), once daily
Administration: Oral gavage
Result: Revealed a T1/2 value of 10.09 h and an AUC value of 59815 ng•h/mL.
Animal Model: BaF3/TEL-AXL xenograft mice[1]
Dosage: 25, 50 or 100 mg/kg, once daily for 7 days
Administration: Oral gavage
Result: Induced tumor regression.
Molecular Weight

563.60

Formula

C32H27F2N7O
SMILES

CC(C)N1C=C(C2=CC=C(F)C=C2)C(C3=C(NC4=CC(F)=C(C5=C(N)N=CC(C6=CN(C)N=C6)=C5)C=C4)N=CC=C31)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Axl-IN-17 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Axl-IN-17TAM ReceptorTyro3AxlMerreceptor tyrosine kinase AXLBaF3/TEL-AXLantitumorTYRO3MERMETRONInhibitorinhibitorinhibit

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