BLU-808
BLU-808 (c-Kit-IN-13) is an orally active and selective c-kit kinase inhibitor. BLU-808 inhibits autophosphorylation of wild-type c-kit with an IC50 of 0.3 nM. BLU-808 inhibits Exon 11 KIT with an IC50 of 0.9 nM. BLU-808 targets WT KIT to prevent stem cell factor-induced KIT autophosphorylation and activation of downstream intracellular signaling cascades. BLU-808 is used in research related to mast cell-mediated diseases (such as chronic urticaria, asthma, and gastrointestinal stromal tumors).
For research use only. We do not sell to patients.
- CAS No.: 3041025-10-6
- Formula: C27H28FN9O2
- Molecular Weight:529.57
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
IC50: 0.3 nM (pKIT); 0.9 nM (Exon 11 KIT)[1]
In Vitro
BLU-808 (Compound I) inhibits autophosphorylation of wild-type c-kit in M-07e cells with an IC50 of 0.3 nM, and inhibits autophosphorylation of Exon 11 KIT in HMC1.1 cells with an IC50 of 0.9 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
BLU-808 (p.o.; single dose) improves lung function in the rodent
Ovalbumins (HY-W250978)-induced asthma model[2].
BLU-808 inhibits SCF-induced histamine release in mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 3041025-10-6
-
Molecular Weight 529.57
-
Formula C27H28FN9O2
-
SMILES
CC1=NN(C=C1C2=CC3=C(C=NN3C=C2)C(NC4=C(C=C(C(C5=NN(N=N5)C6CC6)=C4)F)C)=O)CC(C)(O)C
-
Synonyms
c-Kit-IN-13
-
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
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)