Art. -Nr.: HY-151904

AXL-IN-13

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AXL-IN-13 is a potent and orally active AXL inhibitor (IC₅₀: 1.6 nM, K_d: 0.26 nM). AXL-IN-13 reverses TGF-β1-induced epithelial-mesenchymal transition (EMT), and inhibits cancer cell migration and invasion.

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Reinheit: 98.03%
CAS. Nr.: 2376928-82-2
Formel: C₃₄H₄₁FN₆O₅
Molecular Weight:632.72

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

AXL-IN-13 Chemical Structure

CAS. Nr.: 2376928-82-2

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

Axl	PDGFRβ 2.3 nM (Kd)

Alle TAM Receptor Isoform-spezifische Produkte anzeigen :

Alle PDGFR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	4.7 nM Compound: 6li	Antiproliferative activity against mouse BaF3 cells transfected with TEL-AXL assessed as inhibition of cell growth incubated for 72 hrs Antiproliferative activity against mouse BaF3 cells transfected with TEL-AXL assessed as inhibition of cell growth incubated for 72 hrs	[PMID: 36358010]

In Vitro

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

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

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 (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/mL•h, a T_1/2 value of 4.22 h, and an oral bioavailability (F) of 14.4%^[1].

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

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 T_1/2 (h) C_max (ng/mL) AUC_last 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

Chemical Information

CAS. Nr. 2376928-82-2
Appearance Solid
Molecular Weight 632.72
Formel C₃₄H₄₁FN₆O₅
Color Off-white to light yellow
SMILES

COC1=C(C=C(C2=C1)N=CC=C2OC3=C(C=C(C=C3)NC4=NN(C=C4C(NC5CCCCC5)=O)C)F)OCCCN6CCOCC6
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (158.05 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.5805 mL

7.9024 mL

15.8048 mL

5 mM

0.3161 mL

1.5805 mL

3.1610 mL

10 mM

0.1580 mL

0.7902 mL

1.5805 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.5 mg/mL (3.95 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (3.95 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: 2.5 mg/mL (3.95 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.5805 mL	7.9024 mL	15.8048 mL	39.5120 mL
	5 mM	0.3161 mL	1.5805 mL	3.1610 mL	7.9024 mL
	10 mM	0.1580 mL	0.7902 mL	1.5805 mL	3.9512 mL
	15 mM	0.1054 mL	0.5268 mL	1.0537 mL	2.6341 mL
	20 mM	0.0790 mL	0.3951 mL	0.7902 mL	1.9756 mL
	25 mM	0.0632 mL	0.3161 mL	0.6322 mL	1.5805 mL
	30 mM	0.0527 mL	0.2634 mL	0.5268 mL	1.3171 mL
	40 mM	0.0395 mL	0.1976 mL	0.3951 mL	0.9878 mL
	50 mM	0.0316 mL	0.1580 mL	0.3161 mL	0.7902 mL
	60 mM	0.0263 mL	0.1317 mL	0.2634 mL	0.6585 mL
	80 mM	0.0198 mL	0.0988 mL	0.1976 mL	0.4939 mL
	100 mM	0.0158 mL	0.0790 mL	0.1580 mL	0.3951 mL

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AXL-IN-13

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Orally Active Compound Library

Angiogenesis-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle TAM Receptor Isoform-spezifische Produkte anzeigen

Alle PDGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

parameters	T_1/2 (h)	C_max (ng/mL)	AUC_last	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

AXL-IN-13

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Orally Active Compound Library

Angiogenesis-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle TAM Receptor Isoform-spezifische Produkte anzeigen

Alle PDGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AXL-IN-13 Related Classifications

HY-151904 Related Classifications