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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- 화학식: C30H36FN7O4
- 분자량:577.65
-
보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- 순도&문서
- References
-
Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
PDGFRa 9 nM (IC50) |
KIT |
In Vitro
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 PDGFRAD842V 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 PDGFRAD842V in intact GIST cells at low nanomolar concentrations to potently block oncogenic downstream signal transduction[1].
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.
-
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.
Chemical Information
-
분자량 577.65
-
화학식 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
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
KIT/PDGFRA-IN-3 Related Classifications
HY-189238 Related Classifications
Powered by Bioz