氯那法尼|T6302

Lonafarnib
193275-84-2

￥362 1mg 起订

￥892 5mg 起订

￥1450 10mg 起订

上海更新日期：2024-09-14

TargetMol中国（陶术生物）

VIP12年

联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 氯那法尼

英文名称：: Lonafarnib

CAS号：: 193275-84-2

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.04%

产品类别：: 抑制剂

货号：: T6302

Product Introduction

Bioactivity

Name	Lonafarnib
Description	Lonafarnib (Sch66336) is an orally bioavailable FPTase inhibitor for H-ras, K-ras-4B, and N-ras (IC50: 1.9/5.2/2.8 nM).
Cell Research	The cells are seeded in 96-well cell-culture cluster plates at a density that allowed control cultures to grow exponentially for 5 days. After 24 hours, the cells are treated with different concentrations of SCH66336. SCH66336 is dissolved in DMSO. Control cultures received the same amount of DMSO as the treated cultures do. Cell numbers are estimated after 5 days of treatment by SRB assay. The percentage of growth inhibition is calculated by using the equation: percentage growth inhibition = (1 ? At/Ac) × 100, where At and Ac represent the absorbance in treated and control cultures, respectively. The drug concentration causing a 50% cell growth inhibition (IC50), is determined by interpolation from dose-response curves.(Only for Reference)
Kinase Assay	FPTactivity is determined by measuring the transfer of [3H]farnesyl from [3H]farnesyl PPi to trichloroacetic acid-precipitable Ha-Ras-CVLS. GGPT-1 activity is similarly determined using [3H]geranylgeranyl diphosphate and Ha-Ras-CVLL as substrates[1].
In vitro	SCH66336在0.1 μM至8 μM的浓度范围内，以剂量和时间依赖的方式抑制人头颈部鳞状细胞癌细胞(HNSCC)的生长并诱导凋亡。SCH66336（8 μM）抑制蛋白激酶B/Akt活性及其底物糖原合成激酶（GSK）-3β、叉头转录因子和BAD在SqCC/Y1细胞中的磷酸化。[2] SCH66336对细胞系表现出不同的抗增殖效果，IC50范围为0.6 μM至32.3 μM。[3] Lonafarnib通过CCAAT/增强子结合蛋白同源蛋白（CHOP）-依赖的方式激活DR5启动子的转录活化，从而诱导CHOP依赖性DR5上调。Lonafarnib（<10 μM）激活caspase-8及其下游caspases，因而在H1792细胞中诱导基于caspase-8的凋亡。Lonafarnib（5 μM）上调DR5表达，增加细胞表面DR5分布，并增强肿瘤坏死因子相关凋亡诱导配体诱导的凋亡。[4]
In vivo	Lonafarnib以剂量依赖的方式抑制裸鼠体内HTBI77人肺癌异种移植瘤的生长。[1] 通过口腔灌注，每日两次以50 mg/kg剂量给药的Lonafarnib，能在携带s.c.侧翼XEN01、XEN05或XEN08 GBM异种移植瘤的NOD/SCID小鼠中，经过21天的治疗后抑制肿瘤生长，达到最高69%的生长抑制。[3]
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	DMSO : 10 mg/mL (15.6 mM), Sonication is recommended.
Keywords	Ras \| Inhibitor \| Sch-66336 \| Sch 66336 \| inhibit \| Farnesyl Transferase \| Ftase \| Autophagy \| Lonafarnib
Inhibitors Related	Guanidine hydrochloride \| Hydroxychloroquine
Related Compound Libraries	Inhibitor Library \| Bioactive Compounds Library Max \| EMA Approved Drug Library \| Anti-Aging Compound Library \| FDA-Approved Drug Library \| Anti-Cancer Clinical Compound Library \| Anti-Cancer Drug Library

氯那法尼|||Sch66336|||Sarasar|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子