SB-590885 [405554-55-4]
Cat# HY-10966-10mg
Size : 10mg
Brand : MedChemExpress
SB-590885 is a potent B-Raf inhibitor with Ki of 0.16 nM, and has 11-fold greater selectivity for B-Raf over c-Raf, without inhibition to other human kinases.
For research use only. We do not sell to patients.
SB-590885 Chemical Structure
CAS No. : 405554-55-4
This product is a controlled substance and not for sale in your territory.
Based on 5 publication(s) in Google Scholar
View All Raf Isoform Specific Products:
Description |
SB-590885 is a potent B-Raf inhibitor with Ki of 0.16 nM, and has 11-fold greater selectivity for B-Raf over c-Raf, without inhibition to other human kinases. |
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IC50 & Target[1] |
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In Vitro |
SB-590885 displays significant selectivity for B-Raf over c-Raf with Ki of 0.16 nM over 1.72 nM. SB-590885 is a more potent inhibitor than the previously described Raf/VEGFR kinase inhibitor BAY 439006 (Ki=38 nM for mutant B-Raf, 6 nM for c-Raf). SB-590885 displays potent selectivity over 46 other kinases. Unlike the multi-kinase inhibitor BAY43-9006, SB-590885 stabilizes the oncogenic B-Raf kinase domain in an active configuration. In Colo205, HT29, A375P, SKMEL28, and MALME-3M cells expressing oncogenic B-RafV600E, SB-590885 treatment potently inhibits ERK phosphorylation with EC50 of 28 nM, 58 nM, 290 nM, 58 nM, and 190 nM, respectively, and consistently, inhibits the proliferation with EC50 of 0.1 μM, 0.87 μM, 0.37 μM, 0.12 μM, and 0.15 μM, respectively. SB-590885 decreases anchorage-independent growth of melanoma cell lines in a BRAF mutant-selective manner[1]. SB-590885 displays high affinity for B-Raf with Kd of 0.3 nM[2]. Most of the melanoma cell lines that harbor the BRAF V600E mutation and lack CDK4 mutations (451Lu, WM35, and WM983) are highly sensitive to SB-590885 with IC50 of <1 μM. Increased levels of cyclin D1 resulting from genomic amplification mediate SB-590885 resistance in B-Raf V600E-mutated melanomas[3]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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In Vivo |
Administration of SB-590885 potently decreases tumorigenesis in murine xenografts established from mutant B-Raf-expressing A375P melanoma cells, and modestly inhibits tumor growth[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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Molecular Weight |
453.54 |
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Formula |
C27H27N5O2 |
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CAS No. |
405554-55-4 |
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Appearance |
Solid |
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Color |
White to yellow |
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SMILES |
O/N=C1CCC2=CC(C3=C(NC(C4=CC=C(C=C4)OCCN(C)C)=N3)C5=CC=NC=C5)=CC=C/12 |
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Shipping | Room temperature in continental US; may vary elsewhere. |
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Storage |
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Solvent & Solubility |
In Vitro:
DMSO : 10 mg/mL (22.05 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) Preparing
Stock Solutions
View the 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.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume Number of animals Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO
+
%
+
%
Tween-80
+
%
Saline
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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Purity & Documentation | |||||||||||||
References |
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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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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DMSO | 1 mM | 2.2049 mL | 11.0244 mL | 22.0488 mL | 55.1219 mL |
5 mM | 0.4410 mL | 2.2049 mL | 4.4098 mL | 11.0244 mL | |
10 mM | 0.2205 mL | 1.1024 mL | 2.2049 mL | 5.5122 mL | |
15 mM | 0.1470 mL | 0.7350 mL | 1.4699 mL | 3.6748 mL | |
20 mM | 0.1102 mL | 0.5512 mL | 1.1024 mL | 2.7561 mL |
SB-590885 Related Classifications
- MAPK/ERK Pathway
- Raf