| Chemical & Physical Properties | |
|---|---|
| CAS Number | 303727-31-3 |
| Catalog No. | 2A-9059588 |
| Chinese Name | 4-(4-氯-3-羟基苯基)-2-苯基-5-(吡啶-4-基)-1H-咪唑 |
| Synonyms | Chlormethiazole hydrochloride; L-779450; 2-(Phenyl)-4-(3-hydroxy-4-chlorophenyl)-5-(4-pyridyl)-1H-imidazole |
| Molecular Formula | C20H14ClN3O |
| Molecular Weight | 347.80 |
| Purity | ≥97 (HPLC) |
| Density | 1.335g/cm3 |
| Boiling Point | 579.783ºC at 760 mmHg |
| Appearance | solid |
| Storage Condition | Store at +4°C |
| Application | L-779450 is a potent and selective B-Raf inhibitor with a Kd of 2.4 nM. |
| HTC | 2933990090 |
| MDL Number | MFCD12828750 |
| SMILES | Clc1c(cc(cc1)c2nc([nH]c2c4ccncc4)c3ccccc3)O |
| InChI | 1S/C20H14ClN3O/c21-16-7-6-15(12-17(16)25)19-18(13-8-10-22-11-9-13)23-20(24-19)14-4-2-1-3-5-14/h1-12,25H,(H,23,24) |
| InChI Key | WXJLXRNWMLWVFB-UHFFFAOYSA-N |
| NACRES Code | NA.54 |
| UNSPSC | 12352200 |
| MSDS | msds/59588_1_303727_31_3.pdf |
| Use of | L-779450 is a potent and selective B-Raf kinase inhibitor with a Kd of 2.4 nM. Properties Name 2-chloro-5-(2-phenyl-5-pyridin-4-yl-1H-imidazol-4-yl)phenol Synonym More Synonyms L-779450 Biological Activity 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 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]. 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. Chemical & Physical Properties Exact Mass 347.08300 PSA 61.80000 LogP 5.16470 Index of Refraction 1.671 InChIKey WXJLXRNWMLWVFB-UHFFFAOYSA-N Safety Information Signal Word Danger Hazard Statements H301-H315-H319-H335 Precautionary Statements P280-P301 + P310 + P330-P304 + P340 + P312-P305 + P351 + P338-P337 + P313 HS Code 2933990090 |
| Tax Rebate | 13.0% |
| Supervision | None. MFN tariff: 6.5%. Ordinary tariff: 20.0% |
| Transport Info | Product name: 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% |
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