|N4-(4-([1,2,4]三唑基[1,5-a]吡啶-7-酰氧基)-3-甲基苯基)-N6-(4,4-二甲基-4,5-二氢噁唑-2-基)喹唑啉-4,6-二胺|CsnPharm

CAS No.: 937263-43-9

N4-(4-([1,2,4]Triazolo[1,5-a]pyridin-7-yloxy)-3-methylphenyl)-N6-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine Catalog No. CSN18606

Synonyms: Irbinitinib;ARRY-380;ONT-380

Irbinitinib is a potent and selective HER2 inhibitor with IC50 of 8 nM, equipotent against truncated p95-HER2, 500-fold selective for HER2 versus EGFR.

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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 HER2 (p95)

IC50:8nM HER2

IC50:8nM
描述Human epidermal growth factor receptor (EGFR; HER1,erbB1), human epidermal growth factor r eceptor 2 (HER2; erbB2), HER3 (erbB3) and HER4 (erbB4) are members of the ErbB family of transmembrane receptor tyrosine kinases. Among them, HER2 is a validated and high-value target. Approximately 30% of breast cancers have an amplification of the HER2/neu gene or overexpression of its protein product, HER2. Also, overexpression of HER2 occurs in gastric, colorectal, NSCLC and ovarian cancers. Irbinitinib is a selective and potent HER2 inhibitor with IC50 value of 8nM, ~500-fold selective for HER2 than EGFR, thus avoiding EGFR-related side effects^[1]. Irbinitinib had very good PK/ADME properties both in vitro and in vivo and showed excellent activity in numerous mouse tumor models, including breast (BT-474, MDA-MB-453), ovarian (SKOV-3) and gastric (N87) carcinoma models. Daily oral treatment with Irbinitinib for 90 days achieved tumor growth inhibition by 50% at 50mg/kg and 96% at 100mg/kg in BT-474 model. Daily oral treatment with Irbinitinib, BID, for 90 days achieved tumor growth inhibition by 39% at 50 mg/kg and by 96% at 100 mg/kg in an SKOV-3 model^[2].
作用机制ARRY-380 an ATP-competitive inhibitor.^[1]
动物研究
剂量
Mice^[2] (p.o.): 50 mg/kg - 200 mg/kg

给药途径
p.o.
临床研究

动物研究
剂量	Mice^[2] (p.o.): 50 mg/kg - 200 mg/kg
给药途径	p.o.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01042379	Breast Neoplasms ... more >> Breast Cancer Breast Tumors Collapse <<	Phase 2	Recruiting	-	-
NCT03424473	-	-	-	-	-
NCT03722823	Hepatic Impairment	Phase 1	Recruiting	May 2019	United States, California ... more >> Orange County Research Center Recruiting Tustin, California, United States, 92780 Contact: Rebecca Lopez rebecca.lopez@ocresearchcenter.com Principal Investigator: Joel Neutel United States, Florida Orlando Clinical Research Center Recruiting Orlando, Florida, United States, 32809 Contact: Jennie Jimenez jjimenez@ocrc.net Principal Investigator: Thomas Marbury United States, Tennessee NOCCR Knoxville and Volunteer Research Group Recruiting Knoxville, Tennessee, United States, 37920 Contact: Ben Brooks ben.brooks@amrllc.com Principal Investigator: William Smith United States, Texas Texas Liver Institute Recruiting San Antonio, Texas, United States, 78215 Contact: Mary Lou Hernandez mhernandez@txliver.com Principal Investigator: Eric Lawitz Collapse <<

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
- 2.0811 mL
- 10.4054 mL
- 20.8107 mL
- 5 mM
- 0.4162 mL
- 2.0811 mL
- 4.1621 mL
- 10 mM
- 0.2081 mL
- 1.0405 mL
- 2.0811 mL

技术信息

CAS号

937263-43-9

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H24N8O2

运输

蓝冰

分子量

480.52

别名

Irbinitinib;ARRY-380;ONT-380;ONT-380. Irbinitinib

溶解度

DMSO	34.0 mg/mL (70.8 mM) warming
Water	insoluble

动物实验配方

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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

NCT01042379	Breast Neoplasms ... more >> Breast Cancer Breast Tumors Collapse <<	Phase 2	Recruiting	-	-
NCT03424473	-	-	-	-	-
NCT03722823	Hepatic Impairment	Phase 1	Recruiting	May 2019	United States, California ... more >> Orange County Research Center Recruiting Tustin, California, United States, 92780 Contact: Rebecca Lopez rebecca.lopez@ocresearchcenter.com Principal Investigator: Joel Neutel United States, Florida Orlando Clinical Research Center Recruiting Orlando, Florida, United States, 32809 Contact: Jennie Jimenez jjimenez@ocrc.net Principal Investigator: Thomas Marbury United States, Tennessee NOCCR Knoxville and Volunteer Research Group Recruiting Knoxville, Tennessee, United States, 37920 Contact: Ben Brooks ben.brooks@amrllc.com Principal Investigator: William Smith United States, Texas Texas Liver Institute Recruiting San Antonio, Texas, United States, 78215 Contact: Mary Lou Hernandez mhernandez@txliver.com Principal Investigator: Eric Lawitz Collapse <<
NCT03777761	Healthy	Phase 1	Not yet recruiting	March 2019	United States, Texas ... more >> Covance Clinical Research Unit Not yet recruiting Dallas, Texas, United States, 75247 Principal Investigator: Jennifer Zon, MD Collapse <<
NCT02614794	HER2 Positive Breast Cancer	Phase 2	Recruiting	July 2021	-
NCT03043313	Colorectal Adenocarcinoma ... more >> ERBB2 Gene Amplification HER2/Neu Positive KRAS wt Allele NRAS wt Allele Recurrent Colorectal Carcinoma Stage III Colorectal Cancer AJCC v7 Stage IIIA Colorectal Cancer AJCC v7 Stage IIIB Colorectal Cancer AJCC v7 Stage IIIC Colorectal Cancer AJCC v7 Stage IV Colorectal Cancer AJCC v7 Stage IVA Colorectal Cancer AJCC v7 Stage IVB Colorectal Cancer AJCC v7 Collapse <<	Phase 2	Recruiting	June 30, 2019	United States, Arizona ... more >> Mayo Clinic Hospital Recruiting Phoenix, Arizona, United States, 85054 Contact: Clinical Trials Referrals Office 855-776-0015 Principal Investigator: Tanios S. Bekaii-Saab Mayo Clinic in Arizona Recruiting Scottsdale, Arizona, United States, 85259 Contact: Clinical Trials Referrals Office 855-776-0015 Principal Investigator: Tanios S. Bekaii-Saab United States, Georgia Emory University Hospital/Winship Cancer Institute Recruiting Atlanta, Georgia, United States, 30322 Contact: Meredith Renfroe 404-778-2670 meredith.ann.renfroe@emory.edu Principal Investigator: Christina S. Wu United States, Massachusetts Dana-Farber Cancer Institute Recruiting Boston, Massachusetts, United States, 02215 Contact: Christopher Graham 617-632-5960 Christopher_Graham@DFCI.harvard.edu Principal Investigator: Kimmie Ng United States, Minnesota Mayo Clinic Recruiting Rochester, Minnesota, United States, 55905 Contact: Clinical Trials Referrals Office 855-776-0015 Principal Investigator: Joleen M. Hubbard United States, New York Roswell Park Cancer Institute Recruiting Buffalo, New York, United States, 14263 Contact: Karen A. Hicks 716-845-8947 karen.hicks@roswellpark.org Principal Investigator: Patrick M. Boland Memorial Sloan Kettering Cancer Center Recruiting New York, New York, United States, 10065 Contact: Derek Alexander 646-888-1381 alexandd@mskcc.org Principal Investigator: Andrea Cercek United States, North Carolina Duke University Medical Center Recruiting Durham, North Carolina, United States, 27710 Contact: Ireka Burrus 919-668-1861 Ireka.burrus@duke.edu Principal Investigator: John H. Strickler United States, Wisconsin Aurora Cancer Care-Milwaukee West Recruiting Wauwatosa, Wisconsin, United States, 53226 Contact: Jennifer Mathieu 414-302-2312 jennifer.mathieu@aurora.org Principal Investigator: Federico Augusto H. Sanchez Collapse <<
NCT03723395	Drug-drug Interaction	Phase 1	Recruiting	November 2018	United States, Florida ... more >> Covance Clinical Research Unit Recruiting Daytona Beach, Florida, United States, 32117 Contact: Michelle Saint Pierre 386-366-6428 michelle.saintpierre@covance.com Principal Investigator: Hugh Coleman United States, Texas Covance Clinical Research Unit Recruiting Dallas, Texas, United States, 75247 Contact: Iona Tihina 469-513-6716 Ioana.Tihina@covance.com Principal Investigator: Jennifer Zon Collapse <<
NCT01983501	HER2 Positive Breast Cancers	Phase 1	Active, not recruiting	July 2019	United States, Alabama ... more >> University of Alabama Birmingham, Alabama, United States, 35294 United States, Colorado University of Colorado Cancer Center Aurora, Colorado, United States, 80045 United States, Kansas University of Kansas Kansas City, Kansas, United States, 66160 United States, Massachusetts Dana Farber Cancer Institute Boston, Massachusetts, United States, 02215 United States, Oregon Providence Cancer Center Portland, Oregon, United States, 97213 United States, Tennessee Sarah Cannon Research Institute Nashville, Tennessee, United States, 37203 United States, Washington Northwest Medical Specialties Tacoma, Washington, United States, 98045 Canada, Ontario London Health Sciences Centre London, Ontario, Canada, N6A 5W9 Princess Margaret Cancer Centre Toronto, Ontario, Canada, M5T 2M9 Canada, Quebec Hospital de la Cite-de-la-Sante Laval, Quebec, Canada, H7M 3L9 Jewish General Hospital Montreal, Quebec, Canada, H3T 1E2 Collapse <<
NCT03501979	Metastatic Breast Cancer ... more >> Leptomeningeal Disease Collapse <<	Phase 2	Not yet recruiting	September 2023	United States, Alabama ... more >> University of Alabama at Birmingham Not yet recruiting Birmingham, Alabama, United States, 35294 Contact: Erica M Stringer-Reasor, MD 205-975-2816 esreasor@uabmc.edu United States, Texas University of Texas MD Anderson Cancer Center Not yet recruiting Houston, Texas, United States, 77030 Contact: Rashmi K Murthy, MD, MBE rmurthy1@mdanderson.org Collapse <<
NCT03054363	Breast Cancer	Phase 1 Phase 2	Recruiting	October 2020	United States, Arizona ... more >> University of Arizona Recruiting Tucson, Arizona, United States, 85724 Contact: Dana Lewallen 520-626-2175 DLewallen@uacc.arizona.edu Principal Investigator: Pavani Chalasani United States, Colorado University of Colorado Denver Recruiting Aurora, Colorado, United States, 80045 Contact: Tiffany Colvin 720-848-0664 tiffany.colvin@ucdenver.edu Principal Investigator: Elena Shagisultanova, MD, PhD United States, Illinois Northwestern University Recruiting Chicago, Illinois, United States, 60611 Contact: Peggy Gilbertsen 312-695-1102 cancertrials@northwestern.edu Principal Investigator: William Gradishar United States, New Mexico New Mexico Cancer Care Alliance Recruiting Albuquerque, New Mexico, United States, 87131 Contact: Karwyn Gustafson 505-925-0380 KSGustafson@salud.unm.edu Principal Investigator: Ursa Brown-Glaberman United States, New York Stony Brook University Recruiting Stony Brook, New York, United States, 11794 Contact: Pushpa Talanki 631-638-0815 Pushpa.talanki@stonybrookmedicine.edu Principal Investigator: Alison Stopeck United States, Texas University of Texas Health Science Center San Antonio Recruiting San Antonio, Texas, United States, 78229 Contact: CTRC 210-450-5798 CTRCReferral@uthscsa.edu Principal Investigator: Andrew Brenner Collapse <<
NCT02025192	HER2 Positive Metastatic Breas... more >>t Cancers Collapse <<	Phase 1	Active, not recruiting	July 2019	United States, Colorado ... more >> University of Colorado Aurora, Colorado, United States, 80045 United States, Oregon Providence Cancer Center Portland, Oregon, United States, 97213 United States, Tennessee Sarah Cannon Research Institute Nashville, Tennessee, United States, 37203 United States, Texas MD Anderson Cancer Center Houston, Texas, United States, 77030 United States, Washington Northwest Medical Specialties Tacoma, Washington, United States, 98405 Collapse <<
NCT03758339	Healthy	Phase 1	Completed	-	United States, Wisconsin ... more >> Covance Clinical Research Unit Madison, Wisconsin, United States, 53704 Collapse <<

靶点	Description	IC50
HER2 (p95)		IC50:8nM
HER2		IC50:8nM

N4-(4-([1,2,4]Triazolo[1,5-a]pyridin-7-yloxy)-3-methylphenyl)-N6-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)quinazoline-4,6-diamine Catalog No. CSN18606

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