2. MAPK/ERK Pathway
  3. Raf
  4. Dabrafenib

Dabrafenib  (Synonyms: GSK2118436A; GSK2118436)

Cat. No.: HY-14660 Purity: 99.94%
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Dabrafenib (GSK2118436A) est un inhibiteur compétitif de l'ATP de Raf avec des IC50s de 5 nM et 0,6 nM pour C-Raf et B-RafV600E, respectivement.

Dabrafenib (GSK2118436A) ist ein ATP-kompetitiver Inhibitor von Raf mit IC50-Werten von 5 nM und 0,6 nM für C-Raf bzw. B-RafV600E.

Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-RafV600E, respectively.

For research use only. We do not sell to patients.

Dabrafenib Chemical Structure

Dabrafenib Chemical Structure

CAS No. : 1195765-45-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 57 In-stock
Solution
10 mM * 1 mL in DMSO USD 57 In-stock
Solid
5 mg USD 50 In-stock
10 mg USD 70 In-stock
50 mg USD 100 In-stock
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200 mg USD 190 In-stock
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Based on 54 publication(s) in Google Scholar

Other Forms of Dabrafenib:

Dabrafenib Related Antibodies

Top Publications Citing Use of Products

53 Publications Citing Use of MCE Dabrafenib

WB

    Dabrafenib purchased from MedChemExpress. Usage Cited in: Int J Cancer. 2019 Mar 15;144(6):1379-1390.  [Abstract]

    Western blot confirmed increased MAPK pathway activity in NEC-DUE2 cells when compared to NECDUE1. Treatment with PLX4032 (1 μM), Dabrafenib (100 nM), or GSK1120212 (100 nM) for 4 hours leads to decreased MAPK signaling in NEC-DUE2 cells. Lysates are immunoblotted for the proteins indicated.

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    BRaf c-Raf Raf

    • Biological Activity

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    Description

    Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-RafV600E, respectively[4].

    IC50 & Target[4]

    BRafV600E

    0.6 nM (IC50)

    CRAF

    5 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    A-375 IC50
    0.011 μM
    Compound: 2
    Inhibition of BRAF V600E mutant in human A375 cells assessed as inhibition of ERK phosphorylation measured after 72 hrs by ELISA assay
    Inhibition of BRAF V600E mutant in human A375 cells assessed as inhibition of ERK phosphorylation measured after 72 hrs by ELISA assay
    		[PMID: 25965804]
    A-375 IC50
    0.457 nM
    Compound: DB
    Antiproliferative activity against human A-375 cells assessed as inhibition of cell growth measured after 5 days by MTT assay
    Antiproliferative activity against human A-375 cells assessed as inhibition of cell growth measured after 5 days by MTT assay
    		[PMID: 34958586]
    A-375 IC50
    1 nM
    Compound: 3
    Inhibition of B-Raf V600E mutant in human A375 cells assessed as ERK phosphorylation preincubated for 1 hr by Western blot method
    Inhibition of B-Raf V600E mutant in human A375 cells assessed as ERK phosphorylation preincubated for 1 hr by Western blot method
    		[PMID: 27085672]
    A-375 IC50
    150 nM
    Compound: 2
    Competitive binding affinity to CRAF in human A375 cells after 15 mins in presence of ATP analogue
    Competitive binding affinity to CRAF in human A375 cells after 15 mins in presence of ATP analogue
    		[PMID: 25965804]
    A-375 IC50
    26 nM
    Compound: 2
    Competitive binding affinity to ARAF in human A375 cells after 15 mins in presence of ATP analogue
    Competitive binding affinity to ARAF in human A375 cells after 15 mins in presence of ATP analogue
    		[PMID: 25965804]
    A-375 IC50
    6 nM
    Compound: 2
    Competitive binding affinity to BRAF in human A375 cells after 15 mins in presence of ATP analogue
    Competitive binding affinity to BRAF in human A375 cells after 15 mins in presence of ATP analogue
    		[PMID: 25965804]
    HCT-116 IC50
    5.88 μM
    Compound: 2
    Inhibition of KRAS G13D mutant in human HCT116 cells assessed as inhibition of ERK phosphorylation by ELISA
    Inhibition of KRAS G13D mutant in human HCT116 cells assessed as inhibition of ERK phosphorylation by ELISA
    		[PMID: 25965804]
    HepG2 IC50
    3.7 μM
    Compound: 12, GSK2118436, Dabrafenib
    Inhibition of Alk5 in TGF-beta-stimulated human HepG2 cells assessed as decrease in Smad2 phosphorylation treated for 45 mins prior to TGF-beta stimulation measured after 60 mins by odyssey blot scanner analysis
    Inhibition of Alk5 in TGF-beta-stimulated human HepG2 cells assessed as decrease in Smad2 phosphorylation treated for 45 mins prior to TGF-beta stimulation measured after 60 mins by odyssey blot scanner analysis
    		[PMID: 24900673]
    MIA PaCa-2 EC50
    529 nM
    Compound: 3
    Inhibition of wild type B-Raf in human MIAPaCa2 cells assessed as reduction in ERK phosphorylation preincubated for 1 hr by Western blot method
    Inhibition of wild type B-Raf in human MIAPaCa2 cells assessed as reduction in ERK phosphorylation preincubated for 1 hr by Western blot method
    		[PMID: 27085672]
    Sf9 IC50
    250 nM
    Compound: 58
    Inhibition of human full length N-terminal GST-tagged RIPK3 expressed in baculovirus infected sf9 insect cells assessed as reduction in MBP phosphorylation using MBP as substrate by kinase-Glo luminescence assay
    Inhibition of human full length N-terminal GST-tagged RIPK3 expressed in baculovirus infected sf9 insect cells assessed as reduction in MBP phosphorylation using MBP as substrate by kinase-Glo luminescence assay
    		[PMID: 31622096]
    Sf9 IC50
    9 nM
    Compound: 1
    Inhibition of recombinant human N-terminal GST-6His tagged BRAF V600E mutant (417 to 766 residues) expressed in baculovirus infected Sf9 cells preincubated with substrate followed by protein and ATP addition measured after 60 mins by scintillation counter
    Inhibition of recombinant human N-terminal GST-6His tagged BRAF V600E mutant (417 to 766 residues) expressed in baculovirus infected Sf9 cells preincubated with substrate followed by protein and ATP addition measured after 60 mins by scintillation counter
    		[PMID: 27774137]
    SK-MEL-28 IC50
    3 nM
    Compound: 12, GSK2118436, Dabrafenib
    Inhibition of B-Raf V600E mutant-driven SK-MEL-28 cell proliferation after 72 hrs by CellTiter-Glo luminescent assay
    Inhibition of B-Raf V600E mutant-driven SK-MEL-28 cell proliferation after 72 hrs by CellTiter-Glo luminescent assay
    		[PMID: 24900673]
    SK-MEL-28 IC50
    4 nM
    Compound: 12, GSK2118436, Dabrafenib
    Inhibition of B-Raf V600E mutant in human SK-MEL-28 cells assessed as decrease in ERK phosphorylation incubated for 1 hr by immunoassay
    Inhibition of B-Raf V600E mutant in human SK-MEL-28 cells assessed as decrease in ERK phosphorylation incubated for 1 hr by immunoassay
    		[PMID: 24900673]
    SK-MEL-28 IC50
    43 nM
    Compound: 6
    Cytotoxicity against human SK-MEL-28 cells after 72 hrs by CellTiter-Glo assay
    Cytotoxicity against human SK-MEL-28 cells after 72 hrs by CellTiter-Glo assay
    		[PMID: 29461827]
    In Vitro

    Dabrafenib (GSK2118436, 1 μM) with 0.01 μM GSK1120212 inhibits more than 90% of cell growth in the NRAS mutant clones. GSK2118436 is sufficient to reduce S6P phosphorylation in A375[1]. Dabrafenib suppresses the PolyP-mediated vascular barrier permeability, upregulation of inflammatory biomarkers, adhesion/migration of leukocytes, and activation and/or production of nuclear factor-κB, tumor necrosis factor-α, and interleukin-6[2]. Dabrafenib inhibits the release of HMGB1 and downregulates HMGB1-dependent inflammatory responses by enhancing the expressions of cell adhesion molecules (CAMs) in human endothelial cells[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Dabrafenib Related Antibodies
    In Vivo

    Dabrafenib-treated females have mostly immature reproductive tracts with no evidence of ovulation, similar to age-matched controls; however, DAB-treated females have keratinized and histologically open vaginas[5].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    519.56

    Formula

    C23H20F3N5O2S2
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CC(C)(C)C1=NC(C2=C(F)C(NS(C3=C(F)C=CC=C3F)(=O)=O)=CC=C2)=C(C4=CC=NC(N)=N4)S1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 33 mg/mL (63.52 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    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.
    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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    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:
    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.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.81 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (4.81 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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.

    • Protocol 1

      Add each solvent one by one:  30% PEG400    0.5% Tween-80    5% Propanediol    64.5% H2O

      Solubility: 5 mg/mL (9.62 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  0.5% HPMC in Water

      Solubility: 2.5 mg/mL (4.81 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    % 
    +
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    Tween-80 +
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    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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.
    Purity & Documentation

    Purity: 99.94%

    SDS (480 KB)

    COA (259 KB) HNMR (268 KB) RP-HPLC (244 KB) LCMS (105 KB) Elemental Analysis Report (117 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1]

    For longer term proliferation assays, cells are plated and treated with compound or combination of compounds in RMPI-1640 containing 10% FBS for 12 days. Compound treatments are replaced at least once during the assay. After 12 days, cells are stained with 0.5% methylene blue in 50% ethanol. Images are captured using flatbed scanner.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [5]

    The rat pups selected as the test system are derived from 26 10-week-old, time-mated, virus-antibody-free SD (Crl:CD[SD]) female rats. Mated females are observed for natural deliveries from Day 20 to 23 pc (day parturition completed is designated PND 0). Litter examinations are conducted when parturition is complete, on PNDs 3 and 6, and included gender identification, individual pup weights, and external morphologic examinations. Parturient dams and their litters are selected for study based on clinical signs and body weights, and selected dams and their litters are randomized into study groups based on clinical observations and PND 3 litter mean body weights. On PND 3 or 4, litters are culled to four males and five females, with minimal fostering only when necessary to obtain the desired sex ratio, such that natural litters are maintained as much as possible. Records are kept of fostered pups of original and foster dams. All pups are identified by paw tattoo. To the extent possible, nonlittermates are assigned to subsets. DAB is formulated as a suspension in vehicle, 0.5% hydroxypropylmethylcellulose K15M, and 0.1% (v/v) Tween80 in purified water, and is given to juvenile male and female rats orally by gavage at a dose volume of 5 ml/kg, based on daily body weight.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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 1.9247 mL 9.6235 mL 19.2471 mL 48.1176 mL
    5 mM 0.3849 mL 1.9247 mL 3.8494 mL 9.6235 mL
    10 mM 0.1925 mL 0.9624 mL 1.9247 mL 4.8118 mL
    15 mM 0.1283 mL 0.6416 mL 1.2831 mL 3.2078 mL
    20 mM 0.0962 mL 0.4812 mL 0.9624 mL 2.4059 mL
    25 mM 0.0770 mL 0.3849 mL 0.7699 mL 1.9247 mL
    30 mM 0.0642 mL 0.3208 mL 0.6416 mL 1.6039 mL
    40 mM 0.0481 mL 0.2406 mL 0.4812 mL 1.2029 mL
    50 mM 0.0385 mL 0.1925 mL 0.3849 mL 0.9624 mL
    60 mM 0.0321 mL 0.1604 mL 0.3208 mL 0.8020 mL
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    Dabrafenib Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Dabrafenib1195765-45-7GSK2118436A GSK2118436GSK2118436GSK 2118436GSK-2118436RafRaf kinasesInhibitorinhibitorinhibit

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