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Cat. No.: HY-125014

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RET-IN-2

RET-IN-2 is a selective RET inhibitor with an IC₅₀ of 61.2 nM. RET-IN-2 inhibits the phosphorylation of RET and its downstream STAT3 and AKT proteins in BaF3/CCDC6-RET cells. RET-IN-2 inhibits the proliferation of RET fusion-positive cells. RET-IN-2 can be used for cancer-related research.

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

CAS No.: 2095172-11-3
Formula: C₁₃H₁₆N₆O₂
Molecular Weight:288.31

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

RET-IN-2 Chemical Structure

CAS No.: 2095172-11-3

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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
Chemical Information
Purity & Documentation
References
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Biological Activity

Description

IC₅₀ & Target

^[1]

STAT3

Akt

All STAT Isoforms :

All Akt Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	433 nM Compound: 23c	Antiproliferative activity against mouse BAF3 cells harboring CCDC6-RET fusion protein after 72 hrs by CCK8 assay Antiproliferative activity against mouse BAF3 cells harboring CCDC6-RET fusion protein after 72 hrs by CCK8 assay	[PMID: 28404375]

In Vitro

RET-IN-2 (compound 23c) inhibits RET kinase in biochemical assays with an IC₅₀ of 61.2 nM; it does not significantly inhibit VEGFR-2 (KDR)^[1].
RET-IN-2 inhibits BaF3/CCDC6-RET cell proliferation with an IC₅₀ of 433 nM^[1].
RET-IN-2 (0-1 μM) inhibits RET phosphorylation and downstream STAT3/AKT signaling in BaF3/CCDC6-RET cells^[1].

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

Related Protocols :

Chemical Information

CAS No. 2095172-11-3
Molecular Weight 288.31
Formula C₁₃H₁₆N₆O₂
SMILES

OC(C=1ON=C(C1)C2=NN(C3=NC=NC(N)=C23)C(C)C)C
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

Handling Instructions (2659 KB)

References

[1]. Wang C, et al. Synthesis and structure-activity relationship study of pyrazolo[3,4-d]pyrimidines as tyrosine kinase RET inhibitors. Bioorganic & medicinal chemistry letters. 2017 Jun 01;27(11):2544-2548. [Content Brief]

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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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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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RET-IN-2

All STAT Isoforms

All Akt Isoforms