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product name Dabrafenib (GSK2118436)


Description: Dabrafenib (GSK2118436) is a specific inhibitor of BRAF V600 mutants with IC50 of 0.8 nM in cell-free assays and is 4- and 6-fold less potent against B-Raf (wildype) and c-Raf, respectively. It potently inhibits BRAFV600E, BRAFV600K and BRAFV600D with IC50 values of 0.5nM, 0.6nM and 1.9nM, respectively. Dabrafenib is currently approved by FDA and is widely used in cancer patients harboring BRAF mutations. It is reported that treatment of dabrafenib shrinks the overall size of brain metastases in patients. 

References: Arch Pharm Res. 2011 May;34(5):699-701.



Molecular Weight (MW)

519.56
Formula

C23H20F3N5O2S2
CAS No.

1195765-45-7
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

DMSO: 30 mg/mL (57.74 mM)
Water: <1 mg/mL (slightly soluble or insoluble)
Ethanol: <1 mg/mL
Solubility (In vivo)

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

other peoduct :

General Dabrafenib (orally administrated) inhibits the growth of B-RafV600E mutant melanoma (A375P) and colon cancer (Colo205) human tumor xenografts, growing subcutaneously in immuno-compromised mice.
Animal model A375P cells were implanted subcutaneously in female CD1 nu/nu mice and grown to form tumors [1]; Dabrafenib (orally gavage) inhibits the growth of B-RafV600E mutant melanoma (A375P) and colon cancer (Colo205) human tumor xenografts, growing subcutaneously in immuno-compromised mice [2].
Formulation Dissolved in 0.5% hydroxypropylmethylcellulose, 0.2% Tween 80 in pH 8.0 distilled water
Dosages 10, 30, and 100 mg/kg
Administration Administered orally once daily
Reference [1] PLoS One. 2013; 8(7): e67583; [2] Sylvie Laquerre, et al. 2009, EORTC International Conference. Abst B88.

Cichoric Acid