Home > Transferase & > Tipifarnib

Tipifarnib

替吡法尼,R115777，R-115777,Zarnestra,IND 58359,IND58359,IND-58359,

Tipifarnib是特异的法尼基转移酶抑制剂，IC50为0.6 nM。

目录号
EY0326
EY0326
EY0326
纯度
99.31%
99.31%
99.31%
规格
2 mg
5 mg
10 mg
原价
570
1060
1750
售价
570
1060
1750
库存
现货
现货
现货
订购
订购
订购
订购
订购
订购
具体折扣请咨询客服

  • 生物活性

    Tipifarnib (R115777) is a potent and specific farnesyltransferase (FTase) inhibitor with IC50 of 0.6 nM, its anti-proliferative effects are most prominent in H-ras or N-ras mutant cells. Phase 3.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    2.5, 10, 25，50 nM

  • 动物实验

    50 mg/kg 口服饲喂

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Margolin KA, et al. Clin Cancer Res. 2012, 18(4), 1129-1137.
    [2] Ken S,et al. Voxel-based evidence of perfusion normalization in glioblastoma patients included in a phase I-II trial of radiotherapy/tipifarnib combination. J Neurooncol. 2015 Sep;124(3):465-73. doi: 10.1007/s11060-015-1860-8.
    [3] Tanaka T,et al. Low-Dose Farnesyltransferase Inhibitor Suppresses HIF-1α and Snail Expression in Triple-Negative Breast Cancer MDA-MB-231 Cells In Vitro. J Cell Physiol. 2017 Jan;232(1):192-201. doi: 10.1002/jcp.25411.

    分子式
    C27H22Cl2N4O    		 分子量
    489.4    		 CAS号
    192185-72-1    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    ≥10 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    <1 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT02210858 Accelerated Phase of Disease|Atypical Chronic Myeloid Leukemia, BCR-ABL1 Negative|Chronic Myelogenous Leukemia, BCR-ABL1 Positive|Chronic Myelomonocytic Leukemia|Chronic Phase of Disease|Myelodysplastic/Myeloproliferative Neoplasm, Unclassifiable|Recurrent Disease Other: Laboratory Biomarker Analysis|Drug: Tipifarnib National Cancer Institute (NCI) Phase 1|Phase 2 2000-05-01 2016-12-26
    NCT00045396 Adult Acute Myeloid Leukemia in Remission|Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities|Adult Acute Myeloid Leukemia With Del(5q)|Adult Acute Myeloid Leukemia With Inv(16)(p13;q22)|Adult Acute Myeloid Leukemia With t(15;17)(q22;q12)|Adult Acute Myeloid Leukemia With t(16;16)(p13;q22)|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22)|de Novo Myelodysplastic Syndromes|Secondary Myelodysplastic Syndromes Drug: tipifarnib National Cancer Institute (NCI) Phase 2 2002-06-01 2013-01-08
    NCT00079339 Untreated Childhood Brain Stem Glioma Radiation: radiation therapy|Drug: tipifarnib National Cancer Institute (NCI) Phase 1|Phase 2 2004-01-01 2014-04-29
    NCT02807272 Leukemia, Myelomonocytic, Chronic Drug: Tipifarnib Kura Oncology, Inc. Phase 2 2016-10-01 2016-10-20
    NCT00027872 Acute Myeloid Leukemia With Multilineage Dysplasia Following Myelodysplastic Syndrome|Adult Acute Basophilic Leukemia|Adult Acute Eosinophilic Leukemia|Adult Acute Erythroid Leukemia (M6)|Adult Acute Megakaryoblastic Leukemia (M7)|Adult Acute Minimally Differentiated Myeloid Leukemia (M0)|Adult Acute Monoblastic Leukemia (M5a)|Adult Acute Monoblastic Leukemia and Acute Monocytic Leukemia (M5)|Adult Acute Monocytic Leukemia (M5b)|Adult Acute Myeloblastic Leukemia With Maturation (M2)|Adult Acute Myeloblastic Leukemia Without Maturation (M1)|Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities|Adult Acute Myeloid Leukemia With Del(5q)|Adult Acute Myeloid Leukemia With Inv(16)(p13;q22)|Adult Acute Myeloid Leukemia With t(16;16)(p13;q22)|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22)|Adult Acute Myelomonocytic Leukemia (M4)|Adult Erythroleukemia (M6a)|Adult Pure Erythroid Leukemia (M6b)|Cellular Diagnosis, Adult Acute Myeloid Leukemia|Untreated Adult Acute Myeloid Leukemia Drug: tipifarnib|Other: laboratory biomarker analysis National Cancer Institute (NCI) Phase 2 2001-10-01 2013-03-22
    NCT02535650 Urothelial Carcinoma Drug: tipifarnib Samsung Medical Center Phase 2 2015-11-12 2017-02-20
    NCT02227901 Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma Drug: Tipifarnib|Radiation: External Beam Radiation Therapy|Drug: Temozolomide|Other: Laboratory Biomarker Analysis National Cancer Institute (NCI) Phase 1 2002-09-01 2014-12-19
    NCT00972712 Multiple Myeloma Drug: Bortezomib and Tipifarnib Emory University|Millennium Pharmaceuticals, Inc.|Ortho Biotech, Inc. Phase 1 2006-12-01 2015-03-09
    NCT00082888 Anaplastic Large Cell Lymphoma|Extranodal Marginal Zone Lymphoma of Mucosa-Associated Lymphoid Tissue|Mature T-Cell and NK-Cell Non-Hodgkin Lymphoma|Nodal Marginal Zone Lymphoma|Recurrent Adult Diffuse Large Cell Lymphoma|Recurrent Adult Diffuse Mixed Cell Lymphoma|Recurrent Adult Hodgkin Lymphoma|Recurrent Adult T-Cell Leukemia/Lymphoma|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Recurrent Mantle Cell Lymphoma|Recurrent Small Lymphocytic Lymphoma|Splenic Marginal Zone Lymphoma Other: Laboratory Biomarker Analysis|Drug: Tipifarnib National Cancer Institute (NCI) Phase 2 2004-03-01 2017-03-06
    NCT01361464 Adult Acute Megakaryoblastic Leukemia|Adult Acute Monoblastic Leukemia|Adult Acute Monocytic Leukemia|Adult Acute Myeloid Leukemia With Inv(16)(p13.1q22); CBFB-MYH11|Adult Acute Myeloid Leukemia With Maturation|Adult Acute Myeloid Leukemia With Minimal Differentiation|Adult Acute Myeloid Leukemia With t(16;16)(p13.1;q22); CBFB-MYH11|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22); RUNX1-RUNX1T1|Adult Acute Myeloid Leukemia With t(9;11)(p22;q23); MLLT3-MLL|Adult Acute Myeloid Leukemia Without Maturation|Adult Acute Myelomonocytic Leukemia|Adult Erythroleukemia|Adult Pure Erythroid Leukemia|Alkylating Agent-Related Acute Myeloid Leukemia|Secondary Acute Myeloid Leukemia|Untreated Adult Acute Myeloid Leukemia Drug: Tipifarnib|Other: Laboratory Biomarker Analysis National Cancer Institute (NCI) Phase 2 2011-05-01 2015-03-19
    NCT00060125 Recurrent Melanoma|Stage IV Melanoma Drug: tipifarnib|Other: laboratory biomarker analysis National Cancer Institute (NCI) Phase 2 2003-05-01 2013-06-04
    NCT02464228 Relapsed Peripheral T-Cell Lymphoma|Refractory Peripheral T-Cell Lymphoma Drug: Tipifarnib Kura Oncology, Inc. Phase 2 2015-09-01 2016-09-14
    NCT00048503 Acute Myeloid Leukemia Drug: ZARNESTRA, tipifarnib, R115777 Johnson & Johnson Pharmaceutical Research & Development, L.L.C. Phase 2 2002-06-01 2010-04-23
    NCT00077363 Recurrent Breast Cancer|Stage IV Breast Cancer Drug: tipifarnib|Drug: capecitabine National Cancer Institute (NCI) Phase 2 2004-05-01 2013-02-26
    NCT02779777 Myelodysplastic Syndromes Drug: Tipifarnib Kura Oncology, Inc. Phase 2 2016-05-01 2016-06-21
    NCT00112853 Adult Acute Megakaryoblastic Leukemia (M7)|Adult Acute Minimally Differentiated Myeloid Leukemia (M0)|Adult Acute Monoblastic Leukemia (M5a)|Adult Acute Monocytic Leukemia (M5b)|Adult Acute Myeloblastic Leukemia With Maturation (M2)|Adult Acute Myeloblastic Leukemia Without Maturation (M1)|Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities|Adult Acute Myeloid Leukemia With Inv(16)(p13;q22)|Adult Acute Myeloid Leukemia With t(16;16)(p13;q22)|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22)|Adult Acute Myelomonocytic Leukemia (M4)|Adult Erythroleukemia (M6a)|Adult Pure Erythroid Leukemia (M6b)|Secondary Acute Myeloid Leukemia|Untreated Adult Acute Myeloid Leukemia Drug: tipifarnib|Drug: etoposide National Cancer Institute (NCI) Phase 1 2005-03-01 2013-01-08
    NCT00093470 Adult Acute Myeloid Leukemia|Adult Acute Myeloid Leukemia in Remission Procedure: Clinical Observation|Drug: Tipifarnib National Cancer Institute (NCI) Phase 3 2004-08-01 2016-11-14
    NCT00093418 Adult Acute Megakaryoblastic Leukemia (M7)|Adult Acute Minimally Differentiated Myeloid Leukemia (M0)|Adult Acute Monoblastic Leukemia (M5a)|Adult Acute Monocytic Leukemia (M5b)|Adult Acute Myeloblastic Leukemia With Maturation (M2)|Adult Acute Myeloblastic Leukemia Without Maturation (M1)|Adult Acute Myeloid Leukemia in Remission|Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities|Adult Acute Myeloid Leukemia With Del(5q)|Adult Acute Myeloid Leukemia With Inv(16)(p13;q22)|Adult Acute Myeloid Leukemia With t(16;16)(p13;q22)|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22)|Adult Acute Myelomonocytic Leukemia (M4)|Adult Erythroleukemia (M6a)|Adult Pure Erythroid Leukemia (M6b)|Recurrent Adult Acute Myeloid Leukemia|Untreated Adult Acute Myeloid Leukemia Drug: tipifarnib National Cancer Institute (NCI) Phase 2 2004-09-01 2013-01-14
    NCT00058097 Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma Drug: tipifarnib|Radiation: radiation therapy National Cancer Institute (NCI) Phase 2 2003-08-01 2013-04-08
    NCT00082810 Estrogen Receptor-positive Breast Cancer|Recurrent Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer Drug: fulvestrant|Drug: tipifarnib National Cancer Institute (NCI) Phase 2 2004-03-01 2015-08-03

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

  • 相关化合物库

  • 使用AMQUAR产品发表文献后请联系我们

相关推荐

X
  • 联系人 ：
  • 收件地址 ：
  • 电话号码 ：
  • 单位名称 ：
  • 产品货号 ：
  • 产品规格 ：
  • 发票抬头以及单位税号 ：