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

Dabrafenib  (Synonyms: GSK2118436A; GSK2118436)

Cat. No.: HY-14660 Purity: 99.90%
COA Handling Instructions

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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10 mM * 1 mL in DMSO USD 57 In-stock
Estimated Time of Arrival: December 31
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10 mg USD 70 In-stock
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50 mg USD 100 In-stock
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200 mg USD 190 In-stock
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Customer Review

Based on 36 publication(s) in Google Scholar

Other Forms of Dabrafenib:

Top Publications Citing Use of Products

35 Publications Citing Use of MCE Dabrafenib

WB

    Dabrafenib purchased from MCE. 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

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    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)

    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].

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

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

    519.56

    Appearance

    Solid

    Formula

    C23H20F3N5O2S2
    CAS No.
    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 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 33 mg/mL (63.52 mM)

    *"≥" 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
    10 mM 0.1925 mL 0.9624 mL 1.9247 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  30% PEG400  0.5% Tween80  5% Propanediol  64.5%H2O

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

    • 2.

      Add each solvent one by one:  0.5%HPMC

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

    • 3.

      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

    • 4.

      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

    • 5.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    • 6.

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% saline

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

    • 7.

      Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in saline)

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

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.91%

    COA (258 KB) HNMR (177 KB) LCMS (220 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
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    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.

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    Keywords:

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

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