|N-苄基-2-(5-(4-(2-吗啉代乙氧基)苯基)吡啶-2-基)乙酰胺|CsnPharm

CAS No.: 897016-82-9

Tirbanibulin/特班布林 Catalog No. CSN16540

Synonyms: KX2-391;KX-01;KX01.

KX2-391 is an inhibitor of Src with IC50 of 9 nM-60 nM in cancer cells. It is the first clinical and peptidomimetic class Src inhibitor.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Src

GI50:9-60nM
描述KX2-391, the first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
mouse NIH3T3 cells	-	Function assay	3 days	Inhibition of constitutively active human c-SRC527F mutant-induced growth inhibition in mouse NIH3T3 cells after 3 days by MTT assay	21852023

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
NCT00646139	Lymphoma Lymp... more >>hoproliferative Disorder Small Intestine Cancer Unspecified Adult Solid Tumor, Protocol Specific Collapse <<	Phase 1	Completed	-	United States, New York ... more >> Roswell Park Cancer Institute Buffalo, New York, United States, 14263-0001 Collapse <<
NCT00658970	Solid Tumors ... more >>Lymphoma Collapse <<	Phase 1	Completed	-	United States, Pennsylvania ... more >> Fox Chase Cancer Center Philadelphia, Pennsylvania, United States, 19111 United States, Texas MD Anderson Cancer Center Houston, Texas, United States, 77030 Collapse <<
NCT01074138	Bone-Metastatic, Castration-Re... more >>sistant Prostate Cancer Collapse <<	Phase 2	Completed	-	United States, Illinois ... more >> University of Chicago Chicago, Illinois, United States, 60637 United States, Maryland Johns Hopkins University Baltimore, Maryland, United States, 21205 United States, Michigan Wayne State University-Karmanos Cancer Center Detroit, Michigan, United States United States, Washington University of Washington Seattle, Washington, United States, 98109 United States, Wisconsin University of Wisconsin Madison, Wisconsin, United States, 53792 Collapse <<

更多
参考文献

[1] Fallah-Tafti A, Foroumadi A, et al. Thiazolyl N-benzyl-substituted acetamide derivatives: synthesis, Src kinase inhibitory and anticancer activities. Eur J Med Chem. 2011 Oct;46(10):4853-8.
[2] Lau GM, Lau GM, et al. Expression of Src and FAK in hepatocellular carcinoma and the effect of Src inhibitors on hepatocellular carcinoma in vitro. Dig Dis Sci. 2009 Jul;54(7):1465-74.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3173 mL
- 11.5867 mL
- 23.1734 mL
- 5 mM
- 0.4635 mL
- 2.3173 mL
- 4.6347 mL
- 10 mM
- 0.2317 mL
- 1.1587 mL
- 2.3173 mL

技术信息

CAS号

897016-82-9

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H29N3O3

运输

蓝冰

分子量

431.53

别名

KX2-391;KX-01;KX01.

溶解度

DMSO	86.0 mg/mL (199.3 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

4% DMSO+30% PEG 300+water

5 mg/mL

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT00646139	Lymphoma Lymp... more >>hoproliferative Disorder Small Intestine Cancer Unspecified Adult Solid Tumor, Protocol Specific Collapse <<	Phase 1	Completed	-	United States, New York ... more >> Roswell Park Cancer Institute Buffalo, New York, United States, 14263-0001 Collapse <<
NCT00658970	Solid Tumors ... more >>Lymphoma Collapse <<	Phase 1	Completed	-	United States, Pennsylvania ... more >> Fox Chase Cancer Center Philadelphia, Pennsylvania, United States, 19111 United States, Texas MD Anderson Cancer Center Houston, Texas, United States, 77030 Collapse <<
NCT01074138	Bone-Metastatic, Castration-Re... more >>sistant Prostate Cancer Collapse <<	Phase 2	Completed	-	United States, Illinois ... more >> University of Chicago Chicago, Illinois, United States, 60637 United States, Maryland Johns Hopkins University Baltimore, Maryland, United States, 21205 United States, Michigan Wayne State University-Karmanos Cancer Center Detroit, Michigan, United States United States, Washington University of Washington Seattle, Washington, United States, 98109 United States, Wisconsin University of Wisconsin Madison, Wisconsin, United States, 53792 Collapse <<
NCT01397799	Acute Myelogenous Leukemia	Phase 1	Completed	-	United States, New York ... more >> Roswell Park Cancer Institute Buffalo, New York, United States, 14263 Weill Cornell Medical College New York, New York, United States, 10065 United States, Pennsylvania Thomas Jefferson University Philadelphia, Pennsylvania, United States, 19107 Collapse <<
NCT03285490	Actinic Keratosis	Phase 3	Active, not recruiting	June 29, 2019	-
NCT03285477	Actinic Keratoses	Phase 3	Active, not recruiting	June 28, 2019	-
NCT03575780	Actinic Keratoses	Phase 1	Recruiting	August 2019	United States, New Jersey ... more >> TKL Research Recruiting Fair Lawn, New Jersey, United States, 07410 Contact: Principal Investigator 201-587-0500 Principal Investigator: Regina Yavel, MD Collapse <<
NCT02838628	Actinic Keratosis	Phase 2	Unknown	December 2017	United States, California ... more >> Center for Dermatology Clinical Research Fremont, California, United States, 94538 eStudy Site La Mesa, California, United States, 91942 Palmtree Clinical Research, Inc. Palm Springs, California, United States, 92262 United States, Colorado Horizons Clinical Research Center Denver, Colorado, United States, 80220 United States, Florida Clinical Research of South Florida Coral Gables, Florida, United States, 33134 International Dermatology Research Miami, Florida, United States, 33144 Compass Research Orlando, Florida, United States, 32806 Forward Clinical Trials, Inc. Tampa, Florida, United States, 33624 Palm Beach Research Center West Palm Beach, Florida, United States, 33409 United States, Minnesota Minnesota Clinical Study Center Fridley, Minnesota, United States, 55432 United States, South Carolina Dermatology and Laser Center of Charleston Charleston, South Carolina, United States, 29414 United States, Tennessee Institute of Clinical Research - Tennessee, LLC Murfreesboro, Tennessee, United States, 37130 United States, Texas J&S Studies, Inc. College Station, Texas, United States, 77845 The Center for Skin Research Houston, Texas, United States, 77056 Clinical Trials of Texas, Inc. San Antonio, Texas, United States, 78229 Dermatology Clinical Research Center San Antonio, Texas, United States, 78229 Collapse <<
NCT02337205	Actinic Keratosis	Phase 1	Completed	-	United States, Texas ... more >> DermResearch, Inc. Austin, Texas, United States, 78759 Collapse <<
NCT01764087	Unspecified Adult Solid Tumor,... more >> Protocol Specific Gastric Cancer Breast Cancer Collapse <<	Phase 1 Phase 2	Unknown	May 2016	Korea, Republic of ... more >> Seoul National University Bundang Hospital Recruiting Seongnam, Gyeonggi-Do, Korea, Republic of, 463-707 Contact: Yun Jin Kim +82-31-787-1421 Seoul National University Hospital Recruiting Seoul, Korea, Republic of, 110-744 Contact: Eunkyung Kim +82-2-2072-7616 Collapse <<

Tirbanibulin/特班布林 Catalog No. CSN16540

靶点选择性

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