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CAS No.: 1492952-76-7

Asciminib Catalog No. CSN18872

Synonyms: ABL001;AB -001;asciminib

Asciminib is a potent and selective allosteric Bcr-Abl inhibitor and inhibits Ba/F3 cells grown with an IC50 of 0.25 nM.

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生物活性

描述Bcr-Abl fusion tyrosine kinase is formed because of a reciprocal chromosomal translocation between chromosomes 9 and 22, producing the Philadelphia chromosome. Bcr-Abl is expressed in chronic myeloid leukemia (CML) and a chronic of acute lymphocytic leukemia^[2]. Asciminib is an allosteric inhibitor of the tyrosine kinase activity of Bcr-Abl with IC50 value of 0.5 nM. In vitro, Asciminib inhibited the proliferation of Luc-Ba/F3 cells transformed to express of Bcr-Abl ^WT and Bcr-Abl ^T315I with IC50 values of 1.0 nM and 25 nM, respectively^[3]. Asciminib was selectively active against Bcr-Abl lines with IC50 values ranging in 1-20 nM, irrespective of the presence of either the p210 or the p190 Bcr-Abl isoformWylie A, Schoepfer J, Jahnke W, et al. The allosteric inhibitor ABL001 enables dual targeting of BCR–ABL1|Nature, 2017, 543(7647): 733-737|https://www.ncbi.nlm.nih.gov/pubmed/28329763. In vivo, single doses of 7.5, 15 and 30 mg/kg Asciminib, administered to mice bearing KCL-22 xenografts, inhibited pSTAT5 (Tyr694), which returned to baseline at 10, 12 and 16–20h after administration of the dose, respectivelyWylie A, Schoepfer J, Jahnke W, et al. The allosteric inhibitor ABL001 enables dual targeting of BCR–ABL1|Nature, 2017, 543(7647): 733-737|https://www.ncbi.nlm.nih.gov/pubmed/28329763. Oral administration of 3 mg/kg once daily with Asciminib for 7 days afforded 68-70% tumor growth inhibition, and oral administration of 3 mg/kg twice daily showed tumor regression in KCL-22 mouse xenograft model^[3].
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
NCT02643888	-	-	Not yet recruiting	December 2019	-
NCT03292783	Advanced Solid Tumors	Phase 1	Recruiting	December 27, 2019	Korea, Republic of ... more >> Samsung Medical Center Recruiting Gangnam-gu, Seoul, Korea, Republic of, 135-710 Contact: Ji-Yeon Lee jyun.lee@samsung.com Principal Investigator: Ji-Yeon Lee Collapse <<
NCT03549897	Asthma	Phase 3	Recruiting	September 2018	United States, New York ... more >> Amneal Pharmaceuticals LLC Recruiting Brookhaven, New York, United States, 11719 Contact: Irshad Haque 631-952-0214 ihaque@amneal.com Collapse <<

更多
参考文献

[1] Wylie AA, Schoepfer J, et al. The allosteric inhibitor ABL001 enables dual targeting of BCR-ABL1. Nature. 2017 Mar 30;543(7647):733-737.
[2] Skorski T. BCR-ABL1 Kinase: Hunting an Elusive Target with New Weapons. Chemistry & Biology, 2011, 18(11): 1352-1353
[3] Schoepfer J, Jahnke W, Berellini G, et al. Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. Journal of Medicinal Chemistry, 2018, 61(18): 8120-8135

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
- 2.2230 mL
- 11.1151 mL
- 22.2302 mL
- 5 mM
- 0.4446 mL
- 2.2230 mL
- 4.4460 mL
- 10 mM
- 0.2223 mL
- 1.1115 mL
- 2.2230 mL

技术信息

CAS号

1492952-76-7

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H18ClF2N5O3

运输

蓝冰

分子量

449.84

别名

ABL001;AB -001;asciminib;asciminib free base

溶解度

DMSO	89.0 mg/mL (197.8 mM)

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

NCT02643888	-	-	Not yet recruiting	December 2019	-
NCT03292783	Advanced Solid Tumors	Phase 1	Recruiting	December 27, 2019	Korea, Republic of ... more >> Samsung Medical Center Recruiting Gangnam-gu, Seoul, Korea, Republic of, 135-710 Contact: Ji-Yeon Lee jyun.lee@samsung.com Principal Investigator: Ji-Yeon Lee Collapse <<
NCT03549897	Asthma	Phase 3	Recruiting	September 2018	United States, New York ... more >> Amneal Pharmaceuticals LLC Recruiting Brookhaven, New York, United States, 11719 Contact: Irshad Haque 631-952-0214 ihaque@amneal.com Collapse <<
NCT03595917	B-cell Acute Lymphoblastic Leu... more >>kemia Chronic Myeloid Leukemia (CML) in Lymphoid Blast Crisis Philadelphia Chromosome Positive Acute Lymphoblastic Leukemia Ph+ ALL Collapse <<	Phase 1	Recruiting	November 1, 2024	United States, Massachusetts ... more >> Dana Farber Cancer Institute Recruiting Boston, Massachusetts, United States, 02115 Contact: Marlise R Luskin, MD Contact: Jeremy Stewart 617-582-8063 jstewart13@partners.org Principal Investigator: Marlise Luskin, MD Collapse <<
NCT03106779	Chronic Myelogenous Leukemia	Phase 3	Recruiting	March 19, 2025	-
NCT03605277	Renal Impairment	Phase 1	Recruiting	January 2, 2020	Bulgaria ... more >> Novartis Investigative Site Recruiting Sofia, Bulgaria, 1612 Germany Novartis Investigative Site Recruiting Berlin, Germany, 14050 Collapse <<
NCT03578367	CML Chronic M... more >>yelogenous Leukemia Leukemia, Myeloid Chronic Hematologic Diseases Collapse <<	Phase 2	Recruiting	October 11, 2021	United States, Maryland ... more >> Saint Agnes Healthcare Cancer Institute Recruiting Baltimore, Maryland, United States, 21229 Contact: Chris Hopmann 410-368-2966 chopmann@ascension.org Principal Investigator: Carole Miller Australia, South Australia Novartis Investigative Site Recruiting Adelaide, South Australia, Australia, 5000 Czechia Novartis Investigative Site Recruiting Brno - Bohunice, Czechia, 639 01 France Novartis Investigative Site Recruiting Bordeaux, France, 33076 Hong Kong Novartis Investigative Site Recruiting Hong Kong, Hong Kong Spain Novartis Investigative Site Recruiting Sevilla, Andalucia, Spain, 41009 United Kingdom Novartis Investigative Site Recruiting London, United Kingdom, W12 0HS Collapse <<
NCT02081378	Chronic Myelogenous Leukemia ... more >> Philadelphia Chromosome-positive Acute Lymphoblastic Leukemia Collapse <<	Phase 1	Recruiting	December 20, 2022	United States, Massachusetts ... more >> Dana Farber Cancer Institute Hematology / Oncology Recruiting Boston, Massachusetts, United States, 02215 Contact: Shannon Milillo 617-632-6840 shannon_milillo@dfci.harvard.edu Principal Investigator: Daniel J. DeAngelo United States, Michigan University of Michigan Comprehensive Cancer Center SC Recruiting Ann Arbor, Michigan, United States, +1 48109 0944 Contact: Shelagh L. Elliott 734-232-0759 shelagh@med.umich.edu Principal Investigator: Moshe Talpaz United States, New York Memorial Sloan Kettering Cancer Center Memorial Sloan Kettering Recruiting New York, New York, United States, 10065 Contact: Michael Mauro J. Mauro, MD 212-639-3107 maurom@mskcc.org Principal Investigator: Michael J. Mauro United States, Oregon Oregon Health and Science University SC-6 Recruiting Portland, Oregon, United States, 97239 Contact: Bianca Gille 503-494-4603 gille@ohsu.edu Principal Investigator: Michael J. Heinrich United States, Texas University of Texas/MD Anderson Cancer Center UT MD Anderson Recruiting Houston, Texas, United States, 77030-4009 Contact: Jorge E Cortes, MD 713-794-5783 Jcortes@mdanderson.org Principal Investigator: Jorge E. Cortes United States, Utah Huntsman Cancer Institute SC Recruiting Salt Lake City, Utah, United States, 84112 Contact: Aaron Ernst aaron.ernst@hci.utah.edu Principal Investigator: Michael W. Deininger Australia, South Australia Novartis Investigative Site Recruiting Adelaide, South Australia, Australia, 5000 France Novartis Investigative Site Recruiting Paris Cedex 10, Cedex 10, France, 75475 Novartis Investigative Site Recruiting Bordeaux, France, 33076 Germany Novartis Investigative Site Recruiting Berlin, Germany, 13353 Novartis Investigative Site Recruiting Frankfurt, Germany, 60590 Novartis Investigative Site Recruiting Jena, Germany, 07740 Italy Novartis Investigative Site Recruiting Roma, RM, Italy, 00161 Japan Novartis Investigative Site Recruiting Kobe-shi, Hyogo, Japan, 650-0017 Korea, Republic of Novartis Investigative Site Recruiting Seoul, Seocho-gu, Korea, Republic of, 06591 Netherlands Novartis Investigative Site Recruiting Amsterdam, Netherlands, 1081 HV Singapore Novartis Investigative Site Recruiting Singapore, Singapore, 169608 Spain Novartis Investigative Site Recruiting Madrid, Spain, 28006 Collapse <<
NCT02857868	Hepatic Impairment	Phase 1	Completed	-	United States, Florida ... more >> University of Miami / Clinical Research Services, Inc. Miami, Florida, United States, 33136 Orlando Clinical Research Center Orlando, Florida, United States, 32809 United States, Minnesota DaVita Clinical Research Minneapolis, Minnesota, United States, 55404 Collapse <<

Asciminib Catalog No. CSN18872

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