BI-882370
Based on 1 Customer Validation
BI-882370 is a potent and selective RAF kinase inhibitor that binds to the ATP binding site of the kinase positioned in the DFG-out (inactive) conformation of the BRAF kinase. BI-882370 (BI 882370) inhibits the oncogenic BRAFV600E-mutant, the WT BRAF and CRAF kinases with IC50s of 0.4, 0.8, and 0.6 nM, respectively. BI-882370 also inhibits SRC family kinases.
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- Purity: 98.55%
- CAS No.: 1392429-79-6
- 화학식: C28H33F2N7O2S
- 분자량:569.67
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
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Braf 0.6 nM (IC50) |
C-Raf 0.8 nM (IC50) |
BRafV600E 0.4 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| A-375 | IC50 |
0.9 nM
Compound: 9; BI882370
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Cytotoxicity against human A375 cells harboring BRAF V600E mutant after 72 hrs by alamar blue assay
Cytotoxicity against human A375 cells harboring BRAF V600E mutant after 72 hrs by alamar blue assay
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[PMID: 29461827] |
| A-375 | IC50 |
6.3 nM
Compound: 4; BI882370
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Cytotoxicity in human A375 cells assessed as reduction in cell viability by Cell-titer-Lumi assay
Cytotoxicity in human A375 cells assessed as reduction in cell viability by Cell-titer-Lumi assay
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[PMID: 32223235] |
| HT-29 | IC50 |
1.7 nM
Compound: 4; BI882370
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Cytotoxicity in human HT-29 cells assessed as reduction in cell viability by Cell-titer-Lumi assay
Cytotoxicity in human HT-29 cells assessed as reduction in cell viability by Cell-titer-Lumi assay
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[PMID: 32223235] |
BI-882370 (0.9-6000 nM; 3 days) inhibits the BRAF-mutant human melanoma and colorectal cancer cells proliferation with a EC50 range of 1-10 nM[1]. BI 882370 (0.1-100 nM, 0.1-3000 nM; 2 hours) results in a reduction of p-MEK1/2, p-ERK1/2 and cyclin D1/D2 expression in BRAFV600E-mutant A375 cells; induces phosphorylation of MEK1/2 and enhanced phosphorylation of ERK1/2 in WT BRO cells (3-300 nM)[1]. BI 882370 (0.1-100 nM, 0.1-3000 nM; 24 hours) suppresses cyclin D1/D2 expression, induces Kip1/p27 expression at concentrations of 1 nM or higher in BRAFV600E-mutant A375 cells, expression of cyclins D1/D2 or Kip1/p27 is not affected in WT BRO cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BRAF-mutant and WT melanoma cell lines (A101D, A375, SK-MEL-28, G-361, and BRO); Colorectal cancer cell lines (COLO 205, HT-29, LS411N, and HCT-116)
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Concentration:0.9-6000 nM
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Incubation Time:3 days
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Result:Showed a EC50 range of 1-10 nM in an extended panel of BRAF-mutant human melanoma and colorectal cancer cell; while proliferation of BRAF WT cells was inhibited with EC50 >1 μM.
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Cell Line:BRAFV600E-mutant A375 cells; BRAF WT, NRAS-mutant BRO (WT BRO) cells
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Concentration:0.1-100 nM; 0.1-3000 nM
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Incubation Time:2 hours; 24 hours
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Result:Resulted in a reduction of phospho-MEK1/2 signals and cyclin D1/D2 expression in BRAFV600E-mutant A375 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Human melanoma xenografts in nude mice with BRAF-mutant melanomas and colorectal carcinomas cells (A375, COLO 205; G-361, HT-29 cells)[1]
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Dosage:25 mg/kg; 50 mg/kg
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Administration:Deliver orally; 25 mg/kg, 50 mg/kg; twice daily; 2 weeks
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Result:Regressed tumors partially, upon discontinuation, tumor regrowth was markedly delayed.
Chemical Information
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CAS No. 1392429-79-6
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Appearance Solid
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분자량 569.67
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화학식 C28H33F2N7O2S
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Color Off-white to gray
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SMILES
CCCS(=O)(NC1=CC=C(F)C(N2C=C(C3=CN=CN=C3)C4=NC(N(C5CCN(CC)CC5)C)=CC=C42)=C1F)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
용액&용해도
DMSO : 17.86 mg/mL (31.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.79 mg/mL (3.14 mM); Clear solution
This protocol yields a clear solution of ≥ 1.79 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (17.9 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.79 mg/mL (3.14 mM); Clear solution
This protocol yields a clear solution of ≥ 1.79 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (17.9 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (279 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 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, 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7554 mL | 8.7770 mL | 17.5540 mL | 43.8851 mL |
| 5 mM | 0.3511 mL | 1.7554 mL | 3.5108 mL | 8.7770 mL | |
| 10 mM | 0.1755 mL | 0.8777 mL | 1.7554 mL | 4.3885 mL | |
| 15 mM | 0.1170 mL | 0.5851 mL | 1.1703 mL | 2.9257 mL | |
| 20 mM | 0.0878 mL | 0.4389 mL | 0.8777 mL | 2.1943 mL | |
| 25 mM | 0.0702 mL | 0.3511 mL | 0.7022 mL | 1.7554 mL | |
| 30 mM | 0.0585 mL | 0.2926 mL | 0.5851 mL | 1.4628 mL |
BI-882370 Related Classifications
HY-107779 Related Classifications
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