Encorafenib

SKU: orb1300725

描述

Encorafenib (LGX818) is a potent and selective oral inhibitor of the BRAF V600E mutation, with an IC50 of 0.3 nM. It is widely used in preclinical oncology research, demonstrating significant antitumor activity in both in vitro cellular assays and in vivo models of melanoma and colorectal cancer.

研究领域

Pharmacology & Drug Discovery, Signal Transduction

图片与验证

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关键属性

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CAS 号	1269440-17-6
MW	540.01
纯度	99.87% (May vary between batches)
分子式	C₂₂H₂₇ClFN₇O₄S
SMILES	COC(=O)N[C@@H](C)CNc1nccc(n1)-c1cn(nc1-c1cc(Cl)cc(NS(C)(=O)=O)c1F)C(C)C
靶点	Raf
溶解性	H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:9.3 mg/mL (17.22 mM);DMSO:257 mg/mL (475.92 mM);Ethanol:93 mg/mL (172.22 mM)

生物活性

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靶点 IC50	B-Raf (V600E):0.3 nM
体内	Encorafenib treatment at oral doses as low as 6 mg/kg resulted in strong (75%) and sustained (>24 hours) decrease in phospho-MEK, even following clearance of drug from circulation in single dose PK/PD studies in human melanoma xenograft models (BRAFV600E). Encorafenib induces tumor regression in multiple BRAF mutant human tumor xenograft models grown in immune compromised mice and rats at doses as low as 1 mg/kg. Consistent with the in vitro data, Encorafenib is inactive against BRAF wild-type tumors at doses up to 300 mg/kg bid, with good tolerability and linear increase in exposure. Efficacy is also achieved in a more disease-relevant spontaneous metastatic melanoma and a model of melanoma brain metastasis. Encorafenib is a potent and selective RAF kinase inhibitor with unique biochemical properties that contribute to an excellent pharmacological profile.
体外	In the A375 (BRAFV600E) human melanoma cell line Encorafenib suppresses phospho-ERK (EC50 = 3 nM) leading to potent inhibition of proliferation (EC50 = 4 nM). No significant activity is observed against a panel of 100 kinases (IC50 > 900 nM) and Encorafenib does not inhibit proliferation of > 400 cell lines expressing wild-type BRAF. Contributing to the high potency of Encorafenib is the extremely slow off-rate from BRAFV600E which is not observed with other RAF inhibitors. In biochemical assays the dissociation half-life is >24 hours which translated into sustained target inhibition in cells following drug wash-out.
细胞研究	LGX818 is dissolved in DMSO. A375 is a melanoma cell line that harbors the B-Raf V600E mutation. A375-luc cells engineered to express luciferase is plated to 384-well white clear bottom plates as 1,500 cells/50 μL/well in DMEM containing 10% FBS. Test compounds, dissolved in 100% DMSO at appropriate concentrations, are transferred to the cells by a robotic Pin Tool (100 mL). The cells are incubated for 2 days at 25°C, then 25 μL of BrightGloTM is added to each well and the plates are read by luminescence. The concentration of each compound for 50% inhibition (IC50) is calculated by non-linear regression using XL Fit data analysis software. wild type and V600E B-Raf.

储存与操作

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储存	-20°C
有效期	12 months from date of receipt.
免责声明	For research use only

别名

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Raf, Raf kinases, B-Raf (V600E), Inhibitor, LGX 818, LGX818, LGX-818, Encorafenib, inhibit

相似产品

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MS1 peptide [orb3212339]
MW:
2850.22
可选规格： 50 mg, 10 mg
Encorafenib [orb1222780]
纯度：
>98% (HPLC)
CAS 号：
1269440-17-6
MW:
540.01
分子式：
C₂₂H₂₇ClFN₇O₄S
可选规格： 5 mg, 10 mg, 25 mg, 100 mg, 200 mg, 500 mg, 1 g, 50 mg

质量保证

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our 条款与条件和选购指南.

化合物标识

PubChem CID

50922675 ↗

关键属性

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暂无计算属性。

实验方案信息

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纯度：	>98% (HPLC)
CAS 号：	1269440-17-6
MW:	540.01
分子式：	C₂₂H₂₇ClFN₇O₄S

Encorafenib

描述

研究领域

图片与验证

关键属性

生物活性

储存与操作

别名

相似产品

MS1 peptide [orb3212339]

Encorafenib [orb1222780]

质量保证

化合物标识

关键属性

实验方案信息

可选规格