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首页 / 抑制剂/激动剂 / 代谢酶 / Transferase / Tipifarnib/替吡法尼

Tipifarnib/替吡法尼 {[allProObj[0].p_purity_real_show]}

货号：A412936 同义名： 提法法尼 / R115777; IND 58359

Tipifarnib是一种farnesyltransferase (Ftase) 的抑制剂，IC50为0.86 nM, 具有一定的抗肿瘤和抗寄生虫活性。

Tipifarnib/替吡法尼 化学结构 CAS号：192185-72-1
Tipifarnib/替吡法尼 化学结构
CAS号：192185-72-1
Tipifarnib/替吡法尼 3D分子结构
CAS号：192185-72-1
Tipifarnib/替吡法尼 化学结构 CAS号：192185-72-1
Tipifarnib/替吡法尼 3D分子结构 CAS号：192185-72-1
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Tipifarnib/替吡法尼 纯度/质量文件 产品仅供科研

货号：A412936 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 Transferase ↓ 其他靶点 纯度
Tipifarnib +++

FTase, IC50: 0.6 nM

 		99%+
Tolcapone +

COMT, Ki: 30 nM

 		99%+
Lonafarnib +++

K-ras-4B, IC50: 2.8 nM

H-ras, IC50: 1.9 nM

 		99%+
(E)-Daporinad ++++

NMPRTase, Ki: 0.4 nM

 		99%+
FTI-277 HCl ++++

FTase, IC50: 500 pM

 		98%
A 922500 ++

mouse DGAT-1, IC50: 24 nM

human DGAT-1, IC50: 7 nM

 		98%
Lomeguatrib ++

O6-alkylguanine-DNA-alkyltransferas, IC50: 5 nM

 		99%+
PF-04620110 +

DGAT1, IC50: 19 nM

 		99%
LB42708 +++

FTase (N-ras), IC50: 1.2 nM

FTase (K-Ras), IC50: 0.8 nM

 		98%
GGTI298 Trifluoroacetate ✔ 98%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Tipifarnib/替吡法尼 生物活性

靶点

  • Transferase

    FTase, IC50:0.6 nM
描述 Farnesylation is a posttranslational modification of proteins by which an isoprenyl group is added to a cysteine residue. In mammalian cells, newly synthesized proteins like Ras must be posttranslationally modified by farnesylation through farnesyl protein transferase to allow its proper membrane localization. Tipifarnib is a potent and selective farnesyl protein transferase (FPT) inhibitor with IC50 values of 0.86 nM and 7.9 nM for inhibition of the farnesylation of lamin B and K-RasB peptide substrates, respectively. Treatment with Tipifarnib at concentration ranging in 5-50nM for 3 days inhibited Ras (p21ras) processing in intact NIH 3T3 cells stably transfected with the T24 H-ras oncogene cells, observed by ratio of soluble and total particulate fractions. Tipifarnib exhibited a panel of human tumor cell lines of various tissue types with wide-type ras gene with IC50 values ranging in 2.7-111nM. Oral administration of Tipifarnib at dose ranging in 6.25–100 mg/kg, b.i.d, dose-dependently inhibited the growth of tumors bearing mutant H-ras, mutant K-ras, and wild-type ras genes in nude mice bearing s.c. tumors.

Tipifarnib/替吡法尼 细胞实验

Cell Line
Concentration Treated Time Description References
Sarcoma cell lines 0.1 to 10 µM 24 to 72 hours Significant inhibition of cell proliferation Nat Commun. 2022 Jun 15;13(1):3405.
Human pulmonary artery endothelial cells (HPAEC) 0.1 mM 24-72 hours Inhibited hypoxia-induced cell proliferation without affecting cell viability or apoptosis Cardiovasc Res. 2017 Mar 1;113(3):276-287.
Human pulmonary artery smooth muscle cells (HPASMC) 0.1 mM 24-72 hours Inhibited hypoxia-induced cell proliferation without affecting cell viability or apoptosis Cardiovasc Res. 2017 Mar 1;113(3):276-287.
U937, ML-1, HL-60 800 nM, 3200 nM 48 hours Investigate tipifarnib-induced apoptosis and determine changes in gene expression Haematologica. 2014 Jan;99(1):60-9.
C643 and Hth83 100 nM 6 days To evaluate the sensitivity of cancer cells to tipifarnib and resistance mechanisms. Cancer Res. 2018 Aug 15;78(16):4642-4657.
Calu-1 KRASG12C mutant cell line 1 µM Tipifarnib prevented stress-fiber formation and increased sensitivity to sotorasib. Nat Commun. 2024 Jun 27;15(1):5345.
MCF-7 cells 5.9 nM 5 days R115777 enhances tamoxifen inhibition of MCF-7 cell growth through estrogen receptor dependent and independent pathways Breast Cancer Res. 2005;7(6):R1159-67.

Tipifarnib/替吡法尼 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice Rhabdomyosarcoma Intraperitoneal injection 10 mg/kg Once daily for 14 days Reduced tumor volume and improved survival rates Nat Commun. 2022 Jun 15;13(1):3405.
C57BL mice Hypoxia-induced pulmonary hypertension model Oral 100 mg/kg Twice daily for two weeks Tipifarnib prevented the development of hypoxia-induced pulmonary hypertension, reduced right ventricular hypertrophy and pulmonary arterial muscularization Cardiovasc Res. 2017 Mar 1;113(3):276-287.
NMRI mice PC9 xenograft model Subcutaneously 5 mg/kg 5 days a week Tipifarnib was tested for its efficacy in preventing relapse to targeted therapies. Nat Commun. 2024 Jun 27;15(1):5345.
Mice Hras;p53 mice Gavage 80 mg/kg Twice daily for 28 days To assess the anti-tumor effects of tipifarnib and resistance in mouse models. Cancer Res. 2018 Aug 15;78(16):4642-4657.

Tipifarnib/替吡法尼 动物研究

Dose Mice: 3 mg/kg[3] (s.c.); 10 mg/kg[4] (i.p.); 100 mg/kg[5] (p.o.)
Administration s.c., i.p., p.o.

Tipifarnib/替吡法尼 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
NCT00076102 Neurofibromatosis 1 ... 展开 >> Neurofibroma, Plexiform 收起 << Phase 2 Completed - United States, Alabama ... 展开 >> University of Alabama Birmingham, Alabama, United States, 35233 United States, District of Columbia Childrens National Medical Center Washington, District of Columbia, United States, 20010 United States, Illinois Childrens Memorial Hospital, Chicago Chicago, Illinois, United States, 60614 United States, Maryland Johns Hopkins Oncology Center Baltimore, Maryland, United States, 21287 National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 United States, Massachusetts Childrens Hospital, Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02115 United States, Minnesota Mayo Clinic, Rochester Rochester, Minnesota, United States, 55905 United States, Missouri St. Louis Children's Hospital Saint Louis, Missouri, United States, 63110 United States, New York Beth Israel Medical Center New York, New York, United States, 10003 SUNY Upstate Medical University Syracuse, New York, United States, 13210 United States, Ohio Cleveland Clinic Cleveland, Ohio, United States, 44195 United States, Oregon Oregon Health Sciences University Portland, Oregon, United States, 97201-3098 United States, Pennsylvania Childrens Hospital, Philadelphia Philadelphia, Pennsylvania, United States, 19104 Childrens Hospital, Pittsburgh Pittsburgh, Pennsylvania, United States, 15213 United States, Texas Texas Children's Hospital Houston, Texas, United States, 77030 收起 <<
NCT00076102 - Completed - -
NCT02845232 - Completed - France ... 展开 >> Hospices Civils de Lyon - Centre Hospitalier Lyon Sud, 165 Chemin du Grand Revoyet Pierre-benite, France, 69310 收起 <<

Tipifarnib/替吡法尼 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.04mL

0.41mL

0.20mL

10.22mL

2.04mL

1.02mL

20.43mL

4.09mL

2.04mL

Tipifarnib/替吡法尼 技术信息

CAS号192185-72-1
分子式C27H22Cl2N4O
分子量 489.4
SMILES Code O=C1N(C)C2=C(C=C([C@@](C3=CC=C(Cl)C=C3)(N)C4=CN=CN4C)C=C2)C(C5=CC=CC(Cl)=C5)=C1
MDL No. MFCD07772347
别名 提法法尼 ;R115777; IND 58359
运输蓝冰
InChI Key PLHJCIYEEKOWNM-HHHXNRCGSA-N
Pubchem ID 159324
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C
溶解方案

DMSO: 105 mg/mL(214.55 mM)，配合低频超声助溶，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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一

Tags: Tipifarnib | 192185-72-1 | IND 58359 | R115777 | IND58359 | IND-58359 | R115777 | R 115777 | R-115777 | FTase Inhibitor | Metabolic Enzyme/Protease | Farnesyl Transferase | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Tipifarnib/替吡法尼 纯度/质量文件 | Tipifarnib/替吡法尼 亚型比较 | Tipifarnib/替吡法尼 生物活性 | Tipifarnib/替吡法尼 动物研究 | Tipifarnib/替吡法尼 临床数据 | Tipifarnib/替吡法尼 实验方案 | Tipifarnib/替吡法尼 技术信息

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