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Cat. No.: HY-144706

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Axl-IN-3

Axl-IN-3 is a potent, selective and orally active AXL kinase inhibitor with an IC₅₀ of 41.5 nM. Axl-IN-3 has lower inhibition of other kinases.

For research use only. We do not sell to patients.

CAS No.: 2783991-34-2
Formula: C₂₄H₂₅ClN₆O₂
Molecular Weight:464.95

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (268 KB)

Axl-IN-3 Chemical Structure

CAS No.: 2783991-34-2

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

Axl-IN-3 is a potent, selective and orally active AXL kinase inhibitor with an IC₅₀ of 41.5 nM. Axl-IN-3 has lower inhibition of other kinases^[1].

IC₅₀ & Target

Axl

All TAM Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
SK-OV-3	GI₅₀	1.02 μM Compound: 54	Antiproliferative activity against human SK-OV-3 cells as reduction in cell growth measured after 72 hrs by Celltiter-Glo luminescent assay Antiproliferative activity against human SK-OV-3 cells as reduction in cell growth measured after 72 hrs by Celltiter-Glo luminescent assay	[PMID: 34600239]

In Vitro

Axl-IN-3 (Compound 54) shows anti-proliferative activity in SKOV3 cells with a GI₅₀ of 1.02 μM^[1].
Axl-IN-3 (Compound 54; 1-10 μM; pretreated 1 h) inhibits AXL signaling in SKOV3 cells. Axl-IN-3 shows a dose dependent reduction of phosphorylated AXL (pAXL) levels compared to untreated cells. Additionally, the reduction of pAXL levels also lead to the concomitant reduction in downstream pERK1/2 levels^[1].

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

In Vivo

Pharmacokinetic studies of Axl-IN-3 (Compound 54) at 5 mg/kg reveal rapid oral absorption with a T_max of 0.25 hr, C_max of 460 ng/mL, T_1/2 of 2.46 hr, and area under the curve (AUC) values of 1620 (ng*hr/mL)^[1].

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

Chemical Information

CAS No. 2783991-34-2
Molecular Weight 464.95
Formula C₂₄H₂₅ClN₆O₂
SMILES

COC1=CC=C(C=C1)N2C=C(C=N2)C3=NNC4=C3C=C(C(Cl)=C4)N[C@@H]5CCN(C5)C6COC6
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (268 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)

References

[1]. Pearly Shuyi Ng, et al. Fragment-based lead discovery of indazole-based compounds as AXL kinase inhibitors. Bioorg Med Chem. 2021 Nov 1;49:116437. [Content Brief]

Calculators

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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.

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100 mg

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