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Lifirafenib (Synonyms: BGB-283) 纯度: 98.02%
Lifirafenib (BGB-283) 是新型高效的Raf激酶和EGFR抑制剂,对重组BRafV600E 和EGFR的IC50值分别为23 和29 nM。
Lifirafenib Chemical Structure
CAS No. : 1446090-79-4
规格 | 价格 | 是否有货 | 数量 |
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Free Sample (0.1-0.5 mg) | Apply now | ||
10 mM * 1 mL in DMSO | ¥1631 | In-stock | |
2 mg | ¥1000 | In-stock | |
5 mg | ¥1550 | In-stock | |
10 mg | ¥2200 | In-stock | |
50 mg | ¥7700 | In-stock | |
100 mg | ¥13000 | In-stock | |
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Lifirafenib 相关产品
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生物活性 |
Lifirafenib (BGB-283) is a novel and potent Raf Kinase and EGFR inhibitor with IC50 values of 23 and 29 nM for recombinant BRafV600E and EGFR, respectively. |
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IC50 & Target[1] |
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体外研究 (In Vitro) |
Lifirafenib (BGB-283) potently inhibits BRafV600E-activated ERK phosphorylation and cell proliferation. It demonstrates selective cytotoxicity and preferentially inhibits proliferation of cancer cells harboring BRafV600E and EGFR mutation/amplification. In BRafV600E colorectal cancer cell lines, Lifirafenib (BGB-283) effectively inhibits the reactivation of EGFR and EGFR-mediated cell proliferation[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
Lifirafenib (BGB-283) treatment leads to dose-dependent tumor growth inhibition accompanied by partial and complete tumor regressions in both cell line-derived and primary human colorectal tumor xenografts bearing BRafV600E mutation[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Clinical Trial |
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分子量 |
478.42 |
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Formula |
C25H17F3N4O3 |
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CAS 号 |
1446090-79-4 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : ≥ 100 mg/mL (209.02 mM) * “≥” means soluble, but saturation unknown. 配制储备液
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
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参考文献 |
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Cell Assay [1] |
Melanoma, colon, breast, and lung cancer cells are left to attach for 16 hours and then treated with a 10-point dilution series in duplicate. CellTiter-Glo reagent is added in each well. Mixture is mixed on an orbital shaker for 2 minutes to allow cell lysing, followed by 10 minutes incubation at room temperature to allow development and stabilization of luminescent signal. Luminescent signal is measured using PHERAstar FS reader. EC50 values for cell viability are determined[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Animal Administration [1] |
Mice: When the average tumor size reaches 110 to 200 mm3, mice are randomized to treatment groups and treated twice per day or once daily by oral gavage (p.o.) with vehicle alone or 2.5 to 30 mg/kg of BGB-283. As control, mice are treated with erlotinib (100 mg/kg qd) or cetuximab (40 mg/kg twice weekly). Lifirafenib (BGB-283) and erlotinib are formulated at the desired concentration as a homogenous suspension in 0.5% (w/v) methylcellulose in purified water. Cetuximab is formulated by diluting the injection solution with saline before dosing[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
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