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
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Storage:
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]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
IC50: 0.3 nM (pKIT); 0.9 nM (Exon 11 KIT)[1]
In Vitro
BLU-808 (c-Kit-IN-13) (10 nM) effectively inhibits the activation of human CD34+ mast cells, reducing CD63 expression (IC50 = 2.7 nM) and histamine release (IC50 = 8.6 nM)[2].
BLU-808 potently inhibits SCF (HY-P70781)-stimulated pKIT in M-07e cells (IC50 = 0.37 nM) and SCF-stimulated proliferation in UT-7 cells (IC50 = 1.3 nM)[2].
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].
BLU-808 shows selectivity over the key off-target proteins PDGFRA, PDGFRB, and FLT3 in cellular assays[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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
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CAS No. 3041025-10-6
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Molecular Weight 529.57
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Formula C27H28FN9O2
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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
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Synonyms
c-Kit-IN-13
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BLU-808 Related Classifications
HY-180652 Related Classifications
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