Cart
MAPK Raf Dabrafenib

Dabrafenib

Catalog No. T1903   CAS 1195765-45-7
Synonyms: GSK2118436, GSK2118436A

Dabrafenib is a selective inhibitor of mutated forms of BRAF kinase (IC50s: 0.7/5 nM for B-Raf (V600E)/C-Raf).

Dabrafenib, CAS 1195765-45-7
Pack Size Availability Price/USD Quantity
5 mg In stock 50.00
10 mg In stock 68.00
25 mg In stock 80.00
50 mg In stock 95.00
100 mg In stock 131.00
200 mg In stock 176.00
1 mL * 10 mM (in DMSO) In stock 56.00
Bulk Inquiry
Get quote
Select Batch  
Purity 100.00%
Purity 98.00%
Purity 98.00%
Biological Description
Chemical Properties
Storage & Solubility Information
Preparing Solutions
Description Dabrafenib is a selective inhibitor of mutated forms of BRAF kinase (IC50s: 0.7/5 nM for B-Raf (V600E)/C-Raf).
Targets&IC50 B-Raf ,   B-Raf (V600E) ,   C-Raf
In vivo GSK2118436 dramatically reduced tumor growth in mice bearing B-RafV600E human melanoma tumors. In this model, CD1 nu/nu mice bearing A375P F11 (B-RafV600E) tumors were dosed orally with GSK2118436 at doses of 0.1, 1, 10, and 100 mg/kg once daily for 14 days. Dose-proportional reductions in tumor growth were observed. In the 100 mg/kg group, complete tumor regression was observed in 50% of treated animals [1]. The vaginal opening (VO) occurred earlier in Dabrafenib (DAB) females than in controls; however, the timing of the first estrus was unaffected. DAB-treated females evaluated just before VO had mostly immature reproductive tracts with no evidence of ovulation, similar to age-matched controls; however, DAB-treated females had keratinized and histologically open vaginas [4].
Cell Research
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.
Synonyms GSK2118436 , GSK2118436A
Purity 100.00%
Molecular Weight 519.56
Formula C23H20F3N5O2S2
CAS No. 1195765-45-7

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 28 mg/mL (53.9 mM)

Ethanol: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

30% PEG400+0.5% Tween80+5% propylene glycol: 8 mg/mL

Citations

References and Literature
1. Rheault TR, et al. Discovery of Dabrafenib: A Selective Inhibitor of Raf Kinases with Antitumor Activity against B-Raf-Driven Tumors. ACS Med Chem Lett. 2013 Feb 7;4(3):358-62. 2. Jung B, et al. Anti-septic effects of dabrafenib on HMGB1-mediated inflammatory responses. BMB Rep. 2016 Apr;49(4):214-9. 3. Greger JG, et al. Combinations of BRAF, MEK, and PI3K/mTOR inhibitors overcome acquired resistance to the BRAF inhibitor GSK2118436 dabrafenib, mediated by NRAS or MEK mutations. Mol Cancer Ther, 2012, 11(4), 909-920. 4. Posobiec LM, et al. Early Vaginal Opening in Juvenile Female Rats Given BRAF-Inhibitor Dabrafenib Is Not Associated with Early Physiologic Sexual Maturation. Birth Defects Res B Dev Reprod Toxicol. 2015 Dec;104(6):244-52.

Related compound libraries

This product is contained In the following compound libraries:
Approved Drug Library Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Clinical Compound Library Stem cell Differentiation Compound Library Apoptosis Compound Library Autophagy Compound Library MAPK Inhibitor Library Tyrosine kinase inhibitor library FDA-approved Drug Library Kinase Inhibitor Library Anti-cancer Approved drug Library Anti-cancer Clinical Compound Library Fluorochemical Library Anti-cancer Metabolism Compound Library Anti-obesity Compound Library Anti-cancer Active Compound library Anti-cancer Drug library Drug Repurposing Library Target-Focused Phenotypic Screening Library Small Molecule Immuno-Oncology Compound Library HIF-1 Signaling Pathway Compound Library Anti-COVID-19 Compound Library Anti-Lung Cancer Compound Library Drug-induced Liver Injury (DILI) Compound Library FDA Approved & Pharmacopeial Drug Library Anti-Pancreatic Cancer Compound Library Glutamine Metabolism Compound Library

Related Products

Related compounds with same targets
I-49 free base I-37 free base( 2359690-13-2(free base)) Sorafenib Sorafenib tosylate I-37 Regorafenib monohydrate Locostatin Plx-4032

Dose Conversion

Safe and effective drug dosing is necessary, regardless of its purpose of administration. Learn More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below
Dosage
mg/kg
Average weight of animals
g
Dosing volume per animal
ul
Number of animals
Step Two: Enter the in vivo formulation
% DMSO
%
% Tween 80
% ddH2O
Calculate Reset

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculation
Molecular Weight Calculator
=
X
X

Molarity Calculator allows you to calculate the

  • Mass of a compound required to prepare a solution of known volume and concentration
  • Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Concentration of a solution resulting from a known mass of compound in a specific volume
See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

X
=
X

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

=
/

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Answers to questions you may have can be found in the Inhibitor Handling Instructions. Topics include how to prepare stock solutions, how to store Products, and issues that need special attention for cell-based assays and animal experiments.