| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: =99.5%
| Targets |
BRafV600E (IC50 = 0.6 nM); CRAF (IC50 = 5 nM); B-Raf (IC50 = 5.2 nM)
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|---|---|
| ln Vitro |
Dabrafenib has a 400-fold preference for B-Raf over 91% of the other kinases tested when it comes to Raf kinase selectivity. Dabrafenib reduces ERK phosphorylation and inhibits cell proliferation by initially arresting the cell cycle in the G1 phase in cancer cells that specifically encode the B-RafV600E mutation. [1]
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| ln Vivo |
Dabrafenib (orally administrated) inhibits the development of B-RafV600E mutant colon cancer (Colo205) and melanoma (A375P) human tumor xenografts that are grown subcutaneously in immunodeficient mice. [1]
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| Cell Assay |
For longer-term proliferation assays, cells are plated in 10% FBS-containing RMPI-1640 for 12 days and treated with a single compound or a combination of compounds. The assay involves at least one compound treatment replacement. Using 0.5% methylene blue in 50% ethanol, cells are stained after 12 days. Using a flatbed scanner, pictures are taken.
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| Animal Protocol |
The 26 10-week-old, time-mated, virus-antibody-free SD (Crl:CD[SD]) female rats that were chosen as the test system gave birth to the rat pups. From Day 20 to Day 23 postpartum, mated females are monitored for spontaneous deliveries (the day parturition is complete is designated PND 0). When parturition is complete, on PNDs 3 and 6, litter examinations are carried out. These examinations include external morphologic examinations, gender determination, and individual pup weights. Clinical signs and body weights are used to select parturient dams and their litters for the study, and chosen dams and their litters are then randomly assigned to study groups based on clinical observations and PND 3 litter mean body weights. On PND 3 or 4, litters are reduced to four or five males and females, with only a small amount of fostering required to achieve the desired sex ratio. This helps to preserve natural litter sizes as much as possible. Records of the pups raised by the original and foster dams are kept. Paw tattoos are used to identify each puppy. Nonlittermates are placed in subsets to the greatest extent possible. DAB is administered to young male and female rats by oral gavage at a dose volume of 5 ml/kg, based on daily body weight, in a suspension of vehicle, 0.5% hydroxypropylmethylcellulose K15M, and 0.1% (v/v) Tween80 in purified water.
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| References |
| Molecular Formula |
C23H20F3N5O2S2
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|---|---|
| Molecular Weight |
519.56
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| Exact Mass |
519.10
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| Elemental Analysis |
C, 53.17; H, 3.88; F, 10.97; N, 13.48; O, 6.16; S, 12.34
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| CAS # |
1195765-45-7
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| Related CAS # |
Dabrafenib Mesylate;1195768-06-9;Dabrafenib-d9;1423119-98-5
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| Appearance |
White to off-white solid powder
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| SMILES |
CC(C)(C)C1=NC(=C(S1)C2=NC(=NC=C2)N)C3=C(C(=CC=C3)NS(=O)(=O)C4=C(C=CC=C4F)F)F
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| InChi Key |
BFSMGDJOXZAERB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H20F3N5O2S2/c1-23(2,3)21-30-18(19(34-21)16-10-11-28-22(27)29-16)12-6-4-9-15(17(12)26)31-35(32,33)20-13(24)7-5-8-14(20)25/h4-11,31H,1-3H3,(H2,27,28,29)
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| Chemical Name |
N-[3-[5-(2-aminopyrimidin-4-yl)-2-tert-butyl-1,3-thiazol-4-yl]-2-fluorophenyl]-2,6-difluorobenzenesulfonamide
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| Synonyms |
GSK2118436A; GSK-2118436B; GSK 2118436A; GSK2118436B (Dabrafenib Mesylate ); GSK-2118436A; GSK 2118436B. Trade name: Tafinlar
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9247 mL | 9.6235 mL | 19.2471 mL | |
| 5 mM | 0.3849 mL | 1.9247 mL | 3.8494 mL | |
| 10 mM | 0.1925 mL | 0.9624 mL | 1.9247 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04452877 | Active Recruiting |
Drug: Dabrafenib Drug: Trametinib |
Carcinoma, Non-Small-Cell Lung | Novartis Pharmaceuticals | August 19, 2020 | Phase 2 |
| NCT03944356 | Active Recruiting |
Drug: Dabrafenib and Trametinib | Melanoma | EuMelaReg gGmbH | July 1, 2019 | |
| NCT01972347 | Active Recruiting |
Drug: Dabrafenib Drug: Trametinib |
Melanoma | Melanoma Institute Australia | October 2014 | Phase 2 |
| NCT02967692 | Active Recruiting |
Biological: Spartalizumab Drug: Dabrafenib |
Melanoma | Novartis Pharmaceuticals | February 17, 2017 | Phase 3 |
| NCT02858921 | Active Recruiting |
Drug: Dabrafenib Drug: Trametinib |
Melanoma | Melanoma Institute Australia | November 8, 2017 | Phase 2 |
Dabrafenib inhibits MAPK signalling in BRAFV600E cells and is abrogated by ARAF or CRAF depletion. PLoS One. 2013; 8(7): e67583. |
Modulation of pharmacodynamic markers by dabrafenib in BRAFV600E tumors. |
Inhibition of BRAFV600E tumor xenograft growth by dabrafenib. |
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