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Cat. No.: HY-189799

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Kit-IN-3

Kit-IN-3 is a KIT inhibitor with an IC₅₀ of 2.4 nM. Kit-IN-3 targets the wild-type receptor tyrosine kinase, blocks SCF-mediated autophosphorylation, and reduces cellular activity in serum. Kit-IN-3 inhibits the off-target class III receptor tyrosine kinase PDGFRα with an IC₅₀ of 97 nM, is selective for PDGFRα and PDGFRβ, and has no activity against CSF1R and FLT3.

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

Formula: C₂₁H₁₇F₂N₅O₂
Molecular Weight:409.39

Storage:

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

Kit-IN-3 Chemical Structure

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Use of MCE Products

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

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

Description

IC₅₀ & Target

^[1]

KIT

2.4 nM (IC₅₀)

PDGFRα

97 nM (IC₅₀)

PDGFRβ

All PDGFR Isoforms :

In Vitro

Anti-cancerOthers

Anti-cancer

Kit-IN-3 (Compound 69) (50 min) inhibits SCF-mediated KIT autophosphorylation in M07e cells with pKIT IC₅₀ = 7.5 nM under serum-free conditions and 200 nM in 100% serum^[1].

Others

Kit-IN-3 (1 h) is a potent biochemical KIT inhibitor (IC₅₀ = 2.4 nM) with high selectivity over PDGFRβ, CSF1R, and FLT3 in HTRF assays^[1].
Kit-IN-3 (0.5 μM; different time points) has low intrinsic clearance in rat and human hepatocytes (rat CL_int = 3.76; human CL_int <2.70 μL/min/10⁶ cells)^[1].

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

Chemical Information

Molecular Weight 409.39
Formula C₂₁H₁₇F₂N₅O₂
SMILES

O=C(NC1=CC=C(OC)C=C1)CC2=C(F)C=C(C3=CC4=NC(N)=NN4C=C3)C=C2F
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]. Moon H, et al. Leveraging Structure-Based Design to Overcome Class III RTK Off-Target Activity in the Development of Selective Wild-Type KIT Inhibitors. J Med Chem. 2026;69:21335-21362.

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

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Kit-IN-3

All PDGFR Isoforms

Biological Activity

Description

IC50 & Target

In Vitro

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

Kit-IN-3 Related Classifications

HY-189799 Related Classifications

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