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Cat. No.: HY-189238

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KIT/PDGFRA-IN-3

KIT/PDGFRA-IN-3 is a KIT and PDGFRA mutant kinase inhibitor, with an IC₅₀ of 9 nM against human PDGFRA. KIT/PDGFRA-IN-3 inhibits the kinase activity of KIT, exhibiting superior selectivity for mutant KIT over wild-type KIT. KIT/PDGFRA-IN-3 suppresses the kinase activity of PDGFRA and blocks downstream signaling pathways. KIT/PDGFRA-IN-3 can be used in studies of gastrointestinal stromal tumors.

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

Formula: C₃₀H₃₆FN₇O₄
Molecular Weight:577.65

Storage:

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

KIT/PDGFRA-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
Help & FAQs
Classifications
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Biological Activity

Description

IC₅₀ & Target

^[1]

PDGFRa

9 nM (IC₅₀)

KIT

All PDGFR Isoforms :

In Vitro

Anti-cancerOthers

Anti-cancer

KIT/PDGFRA-IN-3 (compound 44) (0.5 h) achieves potent, mutant-selective kinase inhibition against KIT-D816H with minimal activity against wild-type KIT, supporting its role as a selective inhibitor of oncogenic KIT/PDGFRA variants^[1].
KIT/PDGFRA-IN-3 exhibits exceptionally high cellular potency and excellent target selectivity against PDGFRA^D842V dependent GIST cells, with very low activity in non-KIT/PDGFRA-driven control cells^[1].
KIT/PDGFRA-IN-3 (10-300 nM; 24 h) engages PDGFRA^D842V in intact GIST cells at low nanomolar concentrations to potently block oncogenic downstream signal transduction^[1].

Others

KIT/PDGFRA-IN-3 (10 μM; 20 h) exhibits a highly reduced off-target phenotypic profile in non-oncogene-driven U2OS cells, indicating a low propensity for global cellular pathway perturbation and improved selectivity^[1].

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

Western Blot Analysis^[1]

Cell Line:

T1-a-D842V PDGFRA mutant GIST cells
Concentration:

10 nM; 30 nM; 100 nM; 300 nM
Incubation Time:

24 h
Result:

Achieved strong suppression of phospho-PDGFRA at 10-30 nM.
Effectively reduced phosphorylation of the downstream AKT, MAPK, and S6 signaling proteins.

Related Protocols :

Chemical Information

Molecular Weight 577.65
Formula C₃₀H₃₆FN₇O₄
SMILES

C[C@](C1=CC=C(F)C=C1)(C2=CN=C(N3CCN(C4=C5C=C(OCCOC)C(OCCOC)=CC5=NC=N4)CC3)N=C2)N
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]. Schulz T, et al. Structure-based scaffold hopping reveals strategies to overcome oncogenic KIT and PDGFRA mutation-driven drug-resistance in GIST. Nature communications. 2026 Aug 06;17(1):7932.

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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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Minimum order quantity

100 mg

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

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KIT/PDGFRA-IN-3

All PDGFR Isoforms

Biological Activity

Description

IC50 & Target

In Vitro

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

KIT/PDGFRA-IN-3 Related Classifications

HY-189238 Related Classifications

Bioz

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