DC Chemicals Limited
China
Product Name: L-779,450
Price: $350.0/100mg $700.0/250mg $1600.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: Raf Kinase Inhibitor IV
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

303727-31-3

303727-31-3 structure

303727-31-3 structure

Name: L-779450
Chemical Name: 2-chloro-5-(2-phenyl-5-pyridin-4-yl-1H-imidazol-4-yl)phenol
CAS Number: 303727-31-3
Molecular Formula: C₂₀H₁₄ClN₃O
Molecular Weight: 347.79800
Catalog: Pharmaceutical intermediate Heterocyclic compound Pyridine compound Hydroxypyridine
Create Date: 2018-12-18 01:08:54
Modify Date: 2024-01-03 11:17:14
L-779450 is a potent and selective B-Raf kinase inhibitor with a Kd of 2.4 nM.

Name	2-chloro-5-(2-phenyl-5-pyridin-4-yl-1H-imidazol-4-yl)phenol
Synonyms	Chlormethiazole hydrochloride L-779450 2-(Phenyl)-4-(3-hydroxy-4-chlorophenyl)-5-(4-pyridyl)-1H-imidazole

Description	L-779450 is a potent and selective B-Raf kinase inhibitor with a Kd of 2.4 nM.
Related Catalog	Signaling Pathways >> Autophagy >> Autophagy Research Areas >> Cancer
Target	B-Raf:2.4 nM (Kd)
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.

Density	1.335g/cm3
Boiling Point	579.783ºC at 760 mmHg
Molecular Formula	C₂₀H₁₄ClN₃O
Molecular Weight	347.79800
Flash Point	304.442ºC
Exact Mass	347.08300
PSA	61.80000
LogP	5.16470
Index of Refraction	1.671
Storage condition	Store at +4°C

Symbol	GHS06
Signal Word	Danger
Hazard Statements	H301-H315-H319-H335
Precautionary Statements	P280-P301 + P310 + P330-P304 + P340 + P312-P305 + P351 + P338-P337 + P313
RIDADR	UN 2811 6.1 / PGIII
HS Code	2933990090

HS Code	2933990090
Summary	2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%