Lonafarnib

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Chemical Structure| 193275-84-2 同义名 : 氯那法尼 ;Sch66336; Sarasar
CAS号 : 193275-84-2
货号 : A257211
分子式 : C27H31Br2ClN4O2
纯度 : 99%+
分子量 : 638.82
MDL号 : MFCD06795138
存储条件：

Pure form Sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(39.13 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • Transferase

    H-ras, IC50:1.9 nM

    K-ras-4B, IC50:2.8 nM
描述 Lonafarnib (Sch66336) effectively disrupts Ha-Ras processing in intact cells and inhibits the abnormal growth characteristics of fibroblasts and human cancer cell lines that carry active Ki-Ras proteins[1]. Groups treated with Lonafarnib (10 μM) exhibited a marked increase in the levels of unfarnesylated H-Ras (116-137%) when compared to those receiving the control treatment[2].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
Cos-1 monkey kidney cells Function assay Inhibition of Protein farnesyltransferase in Cos-1 monkey kidney cells expressing H-Ras-val, IC50=0.0019 μM 12190309
COS-7 monkey cells Function assay Inhibiting the farnesylation of H-ras proteins in COS-7 monkey cells transiently expressing H-ras[Val12]-CVLS in the whole cell assay, IC50=0.01 μM 9822558
HCT116 Growth inhibition assay Compound was measured for inhibition of HCT116 tumor cell line in colon under soft agar assay, IC50=0.07 μM 9822558
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00040534 Neoplasms Phase 1 Terminated - -
NCT00040547 Neoplasms Phase 1 Completed - -
NCT00003956 Lymphoma Unsp... 展开 >>ecified Adult Solid Tumor, Protocol Specific 收起 << Phase 1 Completed - United States, New York ... 展开 >> Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10021 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.57mL

0.31mL

0.16mL

7.83mL

1.57mL

0.78mL

15.65mL

3.13mL

1.57mL
参考文献

[1]Liu M, et al. Antitumor activity of SCH 66336, an orally bioavailable tricyclic inhibitor of farnesyl protein transferase, in human tumor xenograft models and wap-ras transgenic mice. Cancer Res. 1998 Nov 1;58(21):4947-56.

[2]Chaponis D, et al. Lonafarnib (SCH66336) improves the activity of temozolomide and radiation for orthotopic malignant gliomas. J Neurooncol. 2011 Aug;104(1):179-89.

[3]Bailey TJ, et al. The inhibitor of phagocytosis, O-phospho-L-serine, suppresses Müller glia proliferation and cone cell regeneration in the light-damaged zebrafish retina. Exp Eye Res. 2010 Nov;91(5):601-12.