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L-779,450

  Cat. No.:  DC8362   Featured
Chemical Structure
303727-31-3
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More than 5000 active chemicals with high quality for research!
Field of application
L-779,450 is a potent, ATP-competitive Raf (Raf kinase) inhibitor (IC50 = 10 nM) that displays > 7, > 30 and > 70-fold selectivity over p38α, GSK3β and Lck respectively.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 303727-31-3
Chemical Name: 2-Chloro-5-(2-phenyl-5-(pyridin-4-yl)-1H-imidazol-4-yl)phenol
Synonyms: 2-Chloro-5-(2-phenyl-5-(pyridin-4-yl)-1H-imidazol-4-yl)phenol;L-779450;2-chloro-5-(2-phenyl-5-pyridin-4-yl-1H-imidazol-4-yl)phenol;2-chloro-5-[2-phenyl-4-(4-pyridinyl)-1H-imidazol-5-yl]Phenol;Phenol, 2-chloro-5-[2-phenyl-4-(4-pyridinyl)-1H-imidazol-5-yl]-;Raf Kinase Inhibitor IV;Chlormethiazole hydrochloride;2-Chloro-5-[2-phenyl-4-(4-pyridinyl)-1H-imidazol-5-yl]-phenol;L 779450
SMILES: OC1=CC(C2=C(C3=CC=NC=C3)N=C(C4=CC=CC=C4)N2)=CC=C1Cl
Formula: C20H14N3OCl
M.Wt: 347.79766
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: L-779450 is a potent and selective B-Raf kinase inhibitor with a Kd of 2.4 nM.
In Vitro: L-779450 (L-779,450) shows a high degree of specificity towards Raf. The only other tested kinase inhibited is p38MAPK, which has a kinase domain structurally related to Raf. L-779450 inhibits anchorage-independent growth of human tumor lines at doses ranging from 0.3 to 2 μM[2]. The effects of L-779450 (L-779,450) on TRAIL sensitivity are investigated here in melanoma cell lines with high TRAIL sensitivity (A-375 and SK-Mel-147), moderate sensitivity (Mel-HO, SK-Mel-13, and SK-Mel-28), and permanent resistance (MeWo, Mel-2a, and SK-Mel-103), as well as in TRAIL-selected cell lines with acquired resistance (A-375-TS and Mel-HO-TS). Despite only moderate direct effects of L-779450 on apoptosis, it strongly enhances TRAIL-induced apoptosis in sensitive melanoma cells and overrules TRAIL resistance in Mel-2a, SK-Mel-103, A-375-TS, and Mel-HO-TS. At 24 hours, 16-35% apoptosis induction is obtained[3].
Cell Assay: For induction of apoptosis, TRAIL (20 ng/mL), the pan-RAF inhibitor L-779450 (0.1-50 μM), the MEK inhibitor U0126 (20 μM), and the selective BRAF(V600E) inhibitor Vemurafenib/PLX4032 are used. For continuous monitoring cell growth, the xCELLigence system is applied. Relative cell indices correspond to attached cell numbers. Cell cycle analyses are performed for quantification of apoptosis and cell cycle arrest. Cells harvested by trypsinization are stained for 1 hour with propidium iodide (200 mg/mL), and sub-G1 fractions, corresponding to cells with fragmented DNA, are quantified by flow cytometry[3].
References: [1]. Takle AK, et al. The identification of potent, selective and CNS penetrant furan-based inhibitors of B-Raf kinase. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4373-6. [2]. Shelton JG, et al. Differential effects of kinase cascade inhibitors on neoplastic and cytokine-mediated cell proliferation. Leukemia. 2003 Sep;17(9):1765-82. [3]. Berger A, et al. RAF inhibition overcomes resistance to TRAIL-induced apoptosis in melanoma cells. J Invest Dermatol. 2014 Feb;134(2):430-440.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
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DC2098 Sorafenib (BAY-43-9006) Sorafenib Tosylate (Bay 43-9006, Nexavar) is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively.
DC7279 SB-590885 SB590885 is a potent B-Raf inhibitor with Ki of 0.16 nM, 11-fold greater selectivity for B-Raf over c-Raf, no inhibition to other human kinases.
DC9987 RAF709 RAF709 is a novel Raf kinase inhibitor extracted from patent WO2014151616A1, compound example 131, has an IC50 of 0.5 and 1.8 nM for c-Raf and b-Raf, respectively.
DC5049 RAF265 (CHIR-265) RAF265 (CHIR-265) is a highly selective B-Raf and VEGFR2 inhibitor with IC50 of 3-60 nM and EC50 of 30 nM, including B-Raf, C-Raf and mutant B-Raf.
DC9814 PLX7904(PB04) PLX7904(PB04) is a potent and selective paradox-breaker RAF inhibitor.
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