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Dabrafenib-d9

CAT: 0804-HY-14660SSize: 1 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-14660SSize:1 mg
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Description
Dabrafenib-d9 is the deuterium labeled Dabrafenib. 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].
CAS Number
1423119-98-5
Product Name Alternative
GSK2118436A-d9; GSK2118436-d9
UNSPSC
12352005
Hazard Statement
H302+H312+H332-H315-H319
Target
Isotope-Labeled Compounds; Raf
Type
Isotope-Labeled Compounds
Related Pathways
MAPK/ERK Pathway; Others
Field of Research
Cancer
Solubility
10 mM in DMSO
Smiles
O=S(C1=C(F)C=CC=C1F)(NC2=CC=CC(C3=C(C4=NC(N)=NC=C4)SC(C(C([2H])([2H])[2H])(C([2H])([2H])[2H])C([2H])([2H])[2H])=N3)=C2F)=O
Molecular Formula
C23H11D9F3N5O2S2
Molecular Weight
528.62
Precautions
P261-P264-P270-P271-P280-P302+P352-P304+P340-P305+P351+P338-P330-P362+P364-P501
References & Citations
[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216. |[2]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.|[3]Lee S, et al. Anti-inflammatory effects of dabrafenib on polyphosphate-mediated vascular disruption. Chem Biol Interact. 2016 Jul 22.|[4]Jung B, et al. Anti-septic effects of dabrafenib on HMGB1-mediated inflammatory responses. BMB Rep. 2016 Apr;49 (4) :214-9.|[5]Alexander M Menzies, et al. Dabrafenib and its potential for the treatment of metastatic melanoma. Drug Des Devel Ther. 2012; 6: 391–405.|[6]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.
Shipping Conditions
Room temperature
Scientific Category
Isotope-Labeled Compounds
Clinical Information
No Development Reported

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