CAS NO: | 1423119-98-5 |
包装: | 1mg |
市场价: | 8845元 |
Cas No. | 1423119-98-5 |
别名 | 达帕菲尼杂质,GSK2118436A-d9; GSK2118436-d9 |
Canonical SMILES | FC1=C(C2=C(C3=CC=NC(N)=N3)SC(C(C([2H])([2H])[2H])(C([2H])([2H])[2H])C([2H])([2H])[2H])=N2)C=CC=C1NS(C4=C(F)C=CC=C4F)(=O)=O |
分子式 | C23H11D9F3N5O2S2 |
分子量 | 528.6 |
溶解度 | DMSO: soluble,Methanol: soluble |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | Dabrafenib-d9is intended for use as an internal standard for the quantification of dabrafenib by GC- or LC-MS. Dabrafenib is an ATP-competitive inhibitor of Raf kinases (IC50s = 0.64, 0.68 and 5 nM for wild-type B-RAF kinase, mutant B-RAFV600E, and wild-type C-RAF kinase, respectively).1It also inhibits the tyrosine kinase-like kinases ALK5 and LIMK1 (IC50s = 11 and 15 nM, respectively) and the calcium/calmodulin-dependent protein kinases SIK2 and PDK2 (IC50s = 27 and 57 nM, respectively), as well as NEK11, CK1, and BRK (IC50s = 20, 41, and 79 nM, respectively) in a panel of 270 kinases at 300 nM. Dabrafenib inhibits the growth of 16 cancer cell lines expressing mutant B-RAFV600E(GI50s =<200 nm), five cell lines expressing other b-raf mutants (gi50s =<30 nm), and 19 cell lines expressing wild-type ras raf (gi50s =<7,000 nM). However, it does not inhibit the growth of four cancer cell lines expressing mutant B-RAFV600E, 133 cell lines expressing wild-type Ras and Raf, or 18 cell lines expressing mutant Ras (GI50s = >10 µM) in a panel of 195 cancer cell lines. Dabrafenib (8 nM) inhibits MAPK signaling, inhibiting phosphorylation of MEK and ERK, and activates caspase-3/7 in B-RAFV600E-expressing A375P melanoma cells but not in wild-type B-RAF-expressing human foreskin fibroblasts (EC200s =71 and >10,000 nM, respectively). It reduces tumor growth in an A375P mouse xenograft model when administered at doses ranging from 3 to 100 mg/kg. Formulations containing dabrafenib have been used in the treatment of B-RAFV600E-expressing cancers. 1.King, A.J., Arnone, M.R., Bleam, M.R., et al.Dabrafenib; Preclinical characterization, increased efficacy when combined with trametinib, while BRAF/MEK tool combination reduced skin lesionsPLoS One8(7)e67583(2013) |