1. MAPK/ERK Pathway
  2. Raf
  3. Dabrafenib Mesylate

Dabrafenib Mesylate (Synonyms: GSK2118436 Mesylate; GSK 2118436B)

Cat. No.: HY-14660A Purity: 99.94%
Handling Instructions

Dabrafenib Mesylate is a potent and selective Raf kinase inhibitor with IC50s of 0.6 and 5.0 nM for RafV600E and c-Raf, respectively.

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

Dabrafenib Mesylate Chemical Structure

Dabrafenib Mesylate Chemical Structure

CAS No. : 1195768-06-9

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10 mM * 1 mL in DMSO USD 68 In-stock
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Customer Review

Based on 13 publication(s) in Google Scholar

Other Forms of Dabrafenib Mesylate:

Top Publications Citing Use of Products

    Dabrafenib Mesylate purchased from MCE. Usage Cited in: Int J Cancer. 2019 Mar 15;144(6):1379-1390.

    Western blot confirmed increased MAPK pathway activity in NEC-DUE2 cells when compared to NECDUE1. Treatment with Vemurafenib (1 μM), Dabrafenib (100 nM), or Trametinib (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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    Description

    Dabrafenib Mesylate is a potent and selective Raf kinase inhibitor with IC50s of 0.6 and 5.0 nM for RafV600E and c-Raf, respectively.

    IC50 & Target[4]

    BRafV600E

    0.6 nM (IC50)

    CRAF

    5 nM (IC50)

    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].

    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].

    Clinical Trial
    Molecular Weight

    615.67

    Formula

    C₂₄H₂₄F₃N₅O₅S₃

    CAS No.

    1195768-06-9

    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.CS(=O)(O)=O

    Shipping

    Room temperature in continental US; may vary elsewhere

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 36 mg/mL (58.47 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.6242 mL 8.1212 mL 16.2425 mL
    5 mM 0.3248 mL 1.6242 mL 3.2485 mL
    10 mM 0.1624 mL 0.8121 mL 1.6242 mL
    *Please refer to the solubility information to select the appropriate solvent.
    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

    Purity: 99.94%

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    Product Name:
    Dabrafenib Mesylate
    Cat. No.:
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