BLU-808
Based on 1 Customer Validation
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).
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- Purity : 98.63%
- CAS No.: 3041025-10-6
- 화학식: C27H28FN9O2
- 분자량:529.57
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
제품 설명
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
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CAS No. 3041025-10-6
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Appearance Solid
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분자량 529.57
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화학식 C27H28FN9O2
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Color White to off-white
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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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 100 mg/mL (188.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
순도&문서
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Data Sheet (298 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8883 mL | 9.4416 mL | 18.8832 mL | 47.2081 mL |
| 5 mM | 0.3777 mL | 1.8883 mL | 3.7766 mL | 9.4416 mL | |
| 10 mM | 0.1888 mL | 0.9442 mL | 1.8883 mL | 4.7208 mL | |
| 15 mM | 0.1259 mL | 0.6294 mL | 1.2589 mL | 3.1472 mL | |
| 20 mM | 0.0944 mL | 0.4721 mL | 0.9442 mL | 2.3604 mL | |
| 25 mM | 0.0755 mL | 0.3777 mL | 0.7553 mL | 1.8883 mL | |
| 30 mM | 0.0629 mL | 0.3147 mL | 0.6294 mL | 1.5736 mL | |
| 40 mM | 0.0472 mL | 0.2360 mL | 0.4721 mL | 1.1802 mL | |
| 50 mM | 0.0378 mL | 0.1888 mL | 0.3777 mL | 0.9442 mL | |
| 60 mM | 0.0315 mL | 0.1574 mL | 0.3147 mL | 0.7868 mL | |
| 80 mM | 0.0236 mL | 0.1180 mL | 0.2360 mL | 0.5901 mL | |
| 100 mM | 0.0189 mL | 0.0944 mL | 0.1888 mL | 0.4721 mL |