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Submit ReviewLonafarnib
说明： Potent farnesyltransferase inhibitor
化学名： 4-[2-[4-[(11R)-3,10-Dibromo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl]-1-piperidinyl]-2-oxoethyl]-1-piperidinecarboxamide
纯度： ≥98% (HPLC)
生物活性 for Lonafarnib
Lonafarnib is a potent farnesyl transferase inhibitor (IC50 = 1.9 nM). Inhibits farnesylation of RAS. Also inhibits Pgp transport (IC50 < 3 μM) and increases potency and anticancer activity when used in conjunction with cytotoxic Pgp substrates. Inhibits neovascularization by affecting cell motility. Orally bioavailable.
技术数据 for Lonafarnib
| 分子量 | 638.82 |
| 公式 | C27H31Br2ClN4O2 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 193275-84-2 |
| PubChem ID | 148195 |
| InChI Key | DHMTURDWPRKSOA-RUZDIDTESA-N |
| Smiles | NC(N1CCC(CC1)CC(N2CCC([C@H]3C4=NC=C(C=C4CCC5=CC(Cl)=CC(Br)=C35)Br)CC2)=O)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Lonafarnib
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 6.39 | 10 |
制备储备液 for Lonafarnib
以下数据基于产品分子量 638.82。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 15.65 mL | 78.27 mL | 156.54 mL |
| 0.5 mM | 3.13 mL | 15.65 mL | 31.31 mL |
| 1 mM | 1.57 mL | 7.83 mL | 15.65 mL |
| 5 mM | 0.31 mL | 1.57 mL | 3.13 mL |
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产品说明书 for Lonafarnib
参考文献 for Lonafarnib
参考文献是支持产品生物活性的出版物。
Bowman et al (2015) Phosphorylation of FADD by the kinase CK1α promotes KRASG12D-induced lung cancer. Sci.Signal. 8 PMID: 25628462
Lo Cicero et al (2016) A high throughput phenotypic screening reveals compounds that counteract premature osteogenic differentiation of HGPS iPS-derived mesenchymal stem cells. Sci.Rep. 6 34798 PMID: 27739443
Sun et al (2015) Lonafarnib is a potential inhibitor for neovascularization. PLoS One. 10 e0122830 PMID: 25853815
Wang et al (2001) The farnesyl protein transferase inhibitor SCH66336 is a potent inhibitor of MDR1 product P-glycoprotein. Cancer.Res. 61 7525 PMID: 11606389
Nielsen et al (1999) Combination therapy with the farnesyl protein transferase inhibitor SCH66336 and SCH58500 (p53 adenovirus) in preclinical cancer models. Cancer Res. 59 5896 PMID: 10606231
Shen et al (2015) Farnesyltransferase and geranylgeranyltransferase I: structures, mechanism, inhibitors and molecular modeling. Drug Discov.Today. 20 267 PMID: 25450772
If you know of a relevant reference for Lonafarnib, please let us know.
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关键词: Lonafarnib, Lonafarnib supplier, Lonafarnib, SCH66336, farnesyl, transferase, inhibitors, inhibits, PgP, transport, anticancer, neovascularization, orally, bioavailable, Protein, Prenyltransferases, Post-translational, Modifications, 6265, Tocris Bioscience
1 篇 Lonafarnib 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Lonafarnib 的部分引用包括：
Daniel E et al (2022) Progerin-expressing endothelial cells are unable to adapt to shear stress. Biophys J 121 620-628 PMID: 34999130
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