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[CAS NO. 1420477-60-6] Acalabrutinib

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Catalog:	HY-17600
Brand:	MCE
CAS:	1420477-60-6

Overview

MDL	MFCD29472294
Molecular Weight	465.51
Molecular Formula	C26H23N7O2
SMILES	O=C(NC1=NC=CC=C1)C2=CC=C(C3=C4C(N)=NC=CN4C([C@H]5N(C(C#CC)=O)CCC5)=N3)C=C2

For research use only. We do not sell to patients.

15 Publications Citing Use of MCE

[1]Signal Transduct Target Ther. 2020 Sep 14;5(1):200.
[2]Matrix Biol. 2022 Aug 25;S0945-053X(22)00104-4.
[3]J Med Chem. 2021 Oct 21.
[4]J Med Chem. 2019 Jul 25;62(14):6561-6574.
[5]Cancers (Basel). 2020 Dec 11;12(12):3731.
[6]Stem Cell Reports. 2019 May 14;12(5):996-1006.
[7]Pharmacol Res. 2020 Jan;151:104512.
[8]Int J Biol Macromol. 2019 Apr 15;127:536-543.
[9]Acta Pharmacol Sin. 2020 Aug 27.
[10]Pharmaceutics. 2022, 14(9), 1876.
[11]Eur J Immunol. 2021 Jul 29.
[12]Cell Signal. 2022 May 18;96:110358.
[13]BMC Cancer. 2021 Jun 26;21(1):732.
[14]Fundam Clin Pharmacol. 2021 Feb 1.
[15]Eur J Drug Metab Pharmacokinet. 2021 Jul 18;1-11.

Summary

Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor. Acalabrutinib binds covalently to Cys481 in the ATP-binding pocket of BTK . Acalabrutinib demonstrates potent on-target effects and efficacy in mouse models of chronic lymphocytic leukemia (CLL) ^[1] ^[2] .

IC50 & Target

IC50: 3 nM (BTK in CD69 B cell) ^[2]

In Vitro

Acalabrutinib (ACP-196) inhibits tyrosine phosphorylation of downstream targets of ERK, IKB, and AKT, in the in vitro signaling assay on primary human CLL cells. In the human CLL NSG xenograft model, Acalabrutinib demonstrates on-target effects including decreased phosphorylation of PLCγ2, ERK and significant inhibition of CLL cell proliferation ^[1] .
Acalabrutinib inhibits purified BTK with an IC ₅₀ of 3 nM and an EC ₅₀ of 8 nM in a human whole-blood CD69 B cell activation assay. Acalabrutinib has improved target specificity over ibrutinib with 323-, 94-, 19-, and 9-fold selectivity over the other TEC kinase family members (ITK, TXK, BMX, and TEC , respectively) and no activity against EGFR ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Acalabrutinib (100 mg twice per day) assessed for thrombus formation at injured arterioles of the mice, exhibits more selective for inhibiting BTK and has virtually no inhibition of platelet activity ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT04722172	Memorial Sloan Kettering Cancer Center\|AstraZeneca\|Genentech, Inc.	Chronic Lymphocytic Leukemia\|Small Lymphocytic Lymphoma	May 21, 2021	Phase 2
NCT04626791	Academic and Community Cancer Research United\|National Cancer Institute (NCI)	Mantle Cell Lymphoma	August 3, 2021	Phase 2
NCT04529772	Acerta Pharma BV\|AstraZeneca	Diffuse Large B-Cell Lymphoma	October 8, 2020	Phase 3
NCT04016805	TG Therapeutics, Inc.	Chronic Lymphocytic Leukemia	August 5, 2019	Phase 2
NCT05336812	Ohio State University Comprehensive Cancer Center	Chronic Lymphocytic Leukemia\|Small Lymphocytic Lymphoma	September 13, 2022	Phase 2
NCT04783415	City of Hope Medical Center\|National Cancer Institute (NCI)	Mantle Cell Lymphoma	March 26, 2021	Phase 2
NCT05197192	German CLL Study Group\|AstraZeneca	Chronic Lymphocytic Leukemia	April 19, 2022	Phase 3
NCT04604067	Swiss Group for Clinical Cancer Research	Diffuse Large B-cell Lymphoma	June 25, 2021	Phase 2
NCT03198650	AstraZeneca	Part1: Advanced B-cell Malignancies\|Part2: r+rCLL and r+rMCL\|Part3: Untreated CLL	June 27, 2017	Phase 1
NCT04548648	UNC Lineberger Comprehensive Cancer Center\|AstraZeneca	Central Nervous System Lymphoma	October 15, 2020	Phase 2
NCT02180711	Acerta Pharma BV\|AstraZeneca	Non Hodgkin Lymphoma	December 29, 2014	Phase 1
NCT02029443	Acerta Pharma BV	Chronic Lymphocytic Leukemia\|Small Lymphocytic Lymphoma\|Richter´s Syndrome\|Prolymphocytic Leukemia	January 30, 2014	Phase 1\|Phase 2
NCT04564040	AstraZeneca\|Parexel	Mantle Cell Lymphoma\|COVID-19	October 12, 2020	Phase 1
NCT04189952	University of Miami\|AstraZeneca	Diffuse Large B Cell Lymphoma\|Chronic Lymphocytic Leukemia\|Small Lymphocytic Leukemia\|Marginal Zone Lymphoma	September 22, 2020	Phase 2
NCT05205252	Epizyme, Inc.	Relapsed+Refractory	December 22, 2021	Phase 1\|Phase 2
NCT03527147	Acerta Pharma BV\|AstraZeneca	NHL\|DLBCL\|Non-hodgkin´s Lymphoma\|Diffuse Large B Cell Lymphoma	June 19, 2018	Phase 1
NCT04462328	Washington University School of Medicine\|AstraZeneca	Primary Central Nervous System Lymphoma	April 29, 2021	Phase 1
NCT04978584	M.D. Anderson Cancer Center	Diffuse Large B-Cell Lymphoma	March 3, 2022	Phase 2
NCT04435483	AstraZeneca\|Acerta Pharma, LLC	Pharmacokinetics\|Bioavailability	May 22, 2020	Phase 1
NCT04169737	M.D. Anderson Cancer Center\|National Cancer Institute (NCI)	Recurrent Chronic Lymphocytic Leukemia\|Recurrent Small Lymphocytic Lymphoma\|Refractory Chronic Lymphocytic Leukemia\|Refractory Small Lymphocytic Lymphoma	July 29, 2020	Phase 2
NCT04662255	Loxo Oncology, Inc.\|Eli Lilly and Company	Lymphoma, Mantle-Cell	April 8, 2021	Phase 3
NCT02351739	Acerta Pharma BV\|Merck Sharp & Dohme LLC	Metastatic Urothelial Carcinoma	April 2015	Phase 2
NCT02296918	Acerta Pharma BV	Chronic Lymphocytic Leukemia\|Small Lymphocytic Lymphoma\|Prolymphocytic Leukemia	December 22, 2014	Phase 1
NCT02475681	Acerta Pharma BV	Chronic Lymphocytic Leukemia	September 2015	Phase 3
NCT02972840	Acerta Pharma BV\|AstraZeneca	Lymphoma, Mantle Cell	April 5, 2017	Phase 3
NCT04075292	AstraZeneca	Untreated Chronic Lymphocytic Leukemia	January 20, 2020	Phase 3
NCT04660045	Weill Medical College of Cornell University\|AstraZeneca	Chronic Lymphocytic Leukemia\|CLL+SLL	May 2022	Phase 2
NCT04765111	M.D. Anderson Cancer Center	Mantle Cell Lymphoma	June 30, 2021	Phase 2
NCT04836832	Narendranath Epperla\|Ohio State University Comprehensive Cancer Center	Recurrent Follicular Lymphoma\|Recurrent Marginal Zone Lymphoma\|Recurrent Nodal Marginal Zone Lymphoma\|Recurrent Splenic Marginal Zone Lymphoma\|Refractory Follicular Lymphoma\|Refractory Indolent Non-Hodgkin Lymphoma\|Refractory Marginal Zone Lymphoma\|Refractory Nodal Marginal Zone Lymphoma\|Refractory Splenic Marginal Zone Lymphoma	July 1, 2022	Phase 1
NCT05057494	AstraZeneca	Chronic Lymphocytic Leukemia or Small Lymphocytic Lymphoma	September 12, 2022	Phase 3
NCT02454179	Acerta Pharma BV\|Merck Sharp & Dohme LLC	Squamous Cell Carcinoma of the Head and Neck	May 2015	Phase 2
NCT04685915	Inhye Ahn, MD\|Bayer\|Dana-Farber Cancer Institute	Chronic Lymphocytic Leukemia (CLL)	February 18, 2021	Phase 2
NCT04484012	City of Hope Medical Center\|National Cancer Institute (NCI)	Recurrent Mantle Cell Lymphoma\|Refractory Mantle Cell Lymphoma	December 31, 2020	Phase 2
NCT05388006	Mayo Clinic\|National Cancer Institute (NCI)	Chronic Lymphocytic Leukemia\|Richter Syndrome\|Small Lymphocytic Lymphoma	June 15, 2022	Phase 2
NCT04546620	University Hospital Southampton NHS Foundation Trust\|AstraZeneca	Diffuse Large B Cell Lymphoma	October 19, 2021	Phase 2
NCT03571308	University Hospital Southampton NHS Foundation Trust	Non Hodgkin Lymphoma	June 2, 2017	Phase 1\|Phase 2
NCT04930536	AstraZeneca	Chronic Lymphocytic Leukemia and Relapsed and Refractory Mantle Cell Lymphoma	July 14, 2021	Phase 4
NCT03128879	M.D. Anderson Cancer Center	Chronic Lymphocytic Leukemia	June 16, 2017	Phase 2
NCT02586857	Acerta Pharma BV	Glioblastoma Multiforme	January 25, 2016	Phase 1\|Phase 2
NCT03968848	Acerta Pharma BV\|AstraZeneca	Hepatic Impairment\|Hepatic Insufficiency\|Healthy Subjects	November 12, 2018	Phase 1
NCT04178798	PETHEMA Foundation	Chronic Lymphocytic Leukemia- Binet Staging System	December 9, 2019	Phase 3
NCT04624633	Jennifer R. Brown, MD, PhD\|AstraZeneca\|TG Therapeutics, Inc.\|Dana-Farber Cancer Institute	Chronic Lymphocytic Leukemia\|Small Lymphocytic Lymphoma\|Relapsed Chronic Lymphocytic Leukemia\|Refractory Chronic Lymphocytic Leukemia	December 15, 2020	Phase 2
NCT04905043	Acerta Pharma BV	Healthy Volunteers	June 3, 2016	Phase 1
NCT04008706	AstraZeneca\|Parexel	Chronic Lymphocytic Leukemia	September 17, 2019	Phase 3
NCT04867941	Acerta Pharma BV	Hepatic Insufficiency	October 21, 2014	Phase 1
NCT02337829	Acerta Pharma BV\|National Institutes of Health (NIH)	Chronic Lymphocytic Leukemia\|Small Lymphocytic Lymphoma	January 12, 2015	Phase 2
NCT02362035	Acerta Pharma BV\|Merck Sharp & Dohme LLC	Follicular Lymphoma (FL)\|CLL\|Small Lymphocytic Lymphoma (SLL)\|Richter´s Syndrome\|Mantle Cell Lymphoma (MCL)\|Indolent Non Hodgkin Lymphoma\|Waldenström Macroglobulinemia\|Multiple Myeloma\|Hodgkin Lymphoma\|Burkitt Lymphoma\|Marginal Zone Lymphomas\|Mediastinal Large B Cell Lymphoma\|Hairy Cell Leukemia	February 20, 2015	Phase 1\|Phase 2
NCT05583149	Jeremy Abramson, MD\|AstraZeneca\|Massachusetts General Hospital	Refractory Aggressive B-cell Lymphomas\|Refractory B-Cell Non-Hodgkin Lymphoma\|Aggressive B-cell NHL\|Diffuse Large B-cell Lymphoma (DLBCL)\|De Novo or Transformed Indolent B-cell Lymphoma\|DLBCL, Nos Genetic Subtypes\|T Cell+Histiocyte-rich Large B-cell Lymphoma\|EBV-Positive DLBCL, Nos\|Primary Mediastinal [Thymic] Large B-cell Lymphoma (PMBCL)\|High-Grade B-Cell Lymphoma, Nos\|C-MYC+BCL6 Double-Hit High-Grade B-Cell Lymphoma\|Grade 3b Follicular Lymphoma\|C-MYC+BCL2 Double-Hit High-Grade B-Cell Lymphoma	October 2022	Phase 2
NCT03580928	Dana-Farber Cancer Institute\|Acerta Pharma, LLC\|Genentech, Inc.\|National Institutes of Health (NIH)\|National Cancer Institute (NCI)	Chronic Lymphocytic Leukemia (CLL)	August 7, 2018	Phase 2
NCT04094142	Seoul National University Hospital	Non-hodgkin Lymphoma,B Cell	July 9, 2019	Phase 2
NCT05038904	Johns Hopkins University\|AstraZeneca	Food Allergy\|Food Allergy Peanut	December 16, 2021	Phase 2
NCT03623373	Washington University School of Medicine\|Acerta Pharma BV	Mantle Cell Lymphoma	November 29, 2018	Phase 2
NCT02735876	Acerta Pharma BV	Mantle Cell Lymphoma	May 2016	Phase 3
NCT04198922	Fred Hutchinson Cancer Center\|AstraZeneca	Recurrent Moderate-Severe Chronic Graft Versus Host Disease\|Hematopoietic and Lymphoid Cell Neoplasm	December 12, 2020	Phase 2
NCT03836261	Acerta Pharma BV\|AstraZeneca	Chronic Lymphocytic Leukemia	February 25, 2019	Phase 3
NCT04901923	Acerta Pharma BV	Healthy Participants	March 15, 2014	Phase 1
NCT04867980	Acerta Pharma BV	Healthy Volunteers	April 1, 2016	Phase 1
NCT02717624	Acerta Pharma BV\|AstraZeneca	Mantle Cell Lymphoma (MCL)	April 20, 2016	Phase 1
NCT04624906	Sunnybrook Health Sciences Centre\|AstraZeneca	Waldenstrom Macroglobulinemia	March 2, 2021	Phase 2
NCT03863184	Weill Medical College of Cornell University\|AstraZeneca\|Celgene Corporation	Mantle Cell Lymphoma	October 11, 2019	Phase 2
NCT03946878	M.D. Anderson Cancer Center\|National Cancer Institute (NCI)	Blastoid Variant Mantle Cell Lymphoma\|CCND1 Protein Overexpression\|CD20 Positive\|CD5 Positive\|FCER2 Negative\|Pleomorphic Variant Mantle Cell Lymphoma\|Recurrent Mantle Cell Lymphoma\|Refractory Mantle Cell Lymphoma\|t(11;14)(q13;q32)	August 13, 2019	Phase 2
NCT04002947	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	Non-Hodgkin´s Lymphoma\|Diffuse Large B-Cell Lymphoma\|DLBCL\|NHL	August 5, 2019	Phase 2
NCT05256641	Jonsson Comprehensive Cancer Center\|AstraZeneca	Diffuse Large B-Cell Lymphoma\|High-grade B-cell Lymphoma\|Transformed Lymphoma\|Secondary Central Nervous System Lymphoma	January 30, 2023	Phase 1\|Phase 2
NCT04380688	AstraZeneca\|Acerta Pharma BV	COVID-19	June 13, 2020	Phase 2
NCT02362048	Acerta Pharma BV\|Merck Sharp & Dohme LLC	Metastatic Pancreatic Cancer	May 2015	Phase 2
NCT03868722	Rigshospitalet, Denmark\|Stichting Hemato-Oncologie voor Volwassenen Nederland\|Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA)\|Karolinska Institutet	CLL	October 11, 2019	Phase 2\|Phase 3
NCT04346199	AstraZeneca\|Acerta Pharma BV	COVID-19	June 12, 2020	Phase 2
NCT04883437	Emory University\|AstraZeneca	Grade 1 Follicular Lymphoma\|Grade 2 Follicular Lymphoma\|Grade 3a Follicular Lymphoma\|Indolent Non-Hodgkin Lymphoma\|Lymphoplasmacytic Lymphoma\|Lymphoproliferative Disorder\|Mantle Cell Lymphoma\|Marginal Zone Lymphoma	September 3, 2021	Phase 2
NCT04630756	AstraZeneca\|Parexel	Advanced Haematological Malignancies	February 17, 2021	Phase 1\|Phase 2
NCT02537444	Acerta Pharma BV\|Merck Sharp & Dohme LLC	Ovarian Cancer	November 2015	Phase 2
NCT04566887	University Health Network, Toronto	Mantle Cell Lymphoma	March 1, 2021	Phase 2
NCT04402138	SCRI Development Innovations, LLC\|Acerta Pharma, LLC	Mantle Cell Lymphoma	August 7, 2020	Phase 2
NCT02387762	Acerta Pharma BV	Rheumatoid Arthritis	April 2015	Phase 2
NCT02570711	Acerta Pharma BV	Metastatic Pancreatic Cancer	October 13, 2015	Phase 2
NCT02157324	Acerta Pharma BV	Chronic Lymphocytic Leukemia	August 18, 2014	Phase 1
NCT05004064	University College, London\|AstraZeneca	Mantle Cell Lymphoma	January 1, 2023	Phase 2
NCT04419389	Aprea Therapeutics	Non Hodgkin Lymphoma\|Chronic Lymphocytic Leukemia\|Mantle Cell Lymphoma	March 2, 2021	Phase 1\|Phase 2
NCT04768985	AstraZeneca	Bioequivalence	February 25, 2021	Phase 1
NCT04497948	Acerta Pharma BV\|AstraZeneca	COVID-19	September 21, 2020	Phase 1
NCT03899337	University of Birmingham\|Bloodwise\|Acerta Pharma, LLC	Richter Syndrome	April 2019	Phase 2
NCT05024006	University of the Philippines	Covid19	April 23, 2020	Not Applicable
NCT05140096	Acerta Pharma BV	Healthy Volunteers	January 3, 2020	Phase 1
NCT04337827	Deepa Jagadeesh\|Case Comprehensive Cancer Center	Post-transplant Lymphoproliferative Disorder	September 2, 2020	Phase 2
NCT04855695	Austin I Kim\|AstraZeneca\|Genentech, Inc.\|Dana-Farber Cancer Institute	Mantle Cell Lymphoma\|Refractory Lymphoma	July 2, 2021	Phase 1\|Phase 2
NCT03205046	Acerta Pharma BV	DLBCL\|Richter Syndrome	June 29, 2017	Phase 1\|Phase 2
NCT02213926	Acerta Pharma BV	Mantle Cell Lymphoma (MCL)	March 2, 2015	Phase 2
NCT04941716	Fred Hutchinson Cancer Center\|AstraZeneca	Recurrent Chronic Lymphocytic Leukemia\|Recurrent Small Lymphocytic Lymphoma\|Refractory Chronic Lymphocytic Leukemia\|Refractory Small Lymphocytic Lymphoma	January 1, 2023	Phase 2
NCT04115631	ECOG-ACRIN Cancer Research Group\|National Cancer Institute (NCI)\|Eastern Cooperative Oncology Group	Liver Lymphoma\|Mantle Cell Lymphoma	October 3, 2019	Phase 2
NCT05495464	M.D. Anderson Cancer Center\|Kite, A Gilead Company\|Acerta Pharma, LLC	Lymphoma\|Mantle Cell Lymphoma	November 18, 2022	Early Phase 1
NCT04257578	University of Washington\|AstraZeneca	B-Cell Non-Hodgkin Lymphoma\|Diffuse Large B-Cell Lymphoma, Not Otherwise Specified\|High Grade B-Cell Lymphoma\|Primary Mediastinal (Thymic) Large B-Cell Lymphoma\|Transformed Follicular Lymphoma to Diffuse Large B-Cell Lymphoma\|Grade 1 Follicular Lymphoma\|Grade 2 Follicular Lymphoma\|Grade 3a Follicular Lymphoma	December 2, 2020	Phase 1\|Phase 2
NCT03788291	University of Rochester	Chronic Lymphocytic Leukemia (CLL)\|Small Lymphocytic Lymphoma (SLL)	March 25, 2019	Phase 2
NCT04560322	Massachusetts General Hospital\|Genentech, Inc.	Chronic Lymphocytic Leukemia\|Small Lymphocytic Lymphoma	October 19, 2020	Phase 2
NCT04716075	Polish Lymphoma Research Group\|AstraZeneca	Chronic Lymphocytic Leukemia\|Chronic Graft-versus-host-disease\|Mantle Cell Lymphoma\|Adverse Event\|Response Rate	August 19, 2019	Phase 2
NCT04876807	Acerta Pharma BV	Healthy Volunteers	January 28, 2016	Phase 1
NCT02112526	Acerta Pharma BV	Activated B-cell Diffuse Large B-Cell Lymphoma (ABC DLBCL)	August 7, 2014	Phase 1
NCT02211014	Acerta Pharma BV\|Acerta Pharma, LLC	Multiple Myeloma (MM)	February 2015	Phase 1
NCT02180724	Acerta Pharma BV	Waldenström Macroglobulinemia (WM)	September 8, 2014	Phase 2
NCT03492125	MingSight Pharmaceuticals, Inc	Chronic Lymphocytic Leukemia\|Small Lymphocytic Lymphoma\|Aggressive Lymphoma	May 25, 2018	Phase 1\|Phase 2
NCT04883749	German CLL Study Group	Chronic Lymphoid Leukemia	June 1, 2021	Phase 2
NCT02328014	Acerta Pharma BV\|AstraZeneca	Non-Hodgkins Lymphoma\|Multiple Myeloma\|B-All	December 20, 2014	Phase 1\|Phase 2
NCT02477696	Acerta Pharma BV	Chronic Lymphocytic Leukemia	July 28, 2015	Phase 3
NCT04404088	M.D. Anderson Cancer Center\|National Cancer Institute (NCI)	Ann Arbor Stage III Grade 1 Follicular Lymphoma\|Ann Arbor Stage III Grade 2 Follicular Lymphoma\|Ann Arbor Stage III Grade 3 Follicular Lymphoma\|Ann Arbor Stage IV Grade 1 Follicular Lymphoma\|Ann Arbor Stage IV Grade 2 Follicular Lymphoma\|Ann Arbor Stage IV Grade 3 Follicular Lymphoma\|Grade 3a Follicular Lymphoma	July 16, 2020	Phase 2
NCT04502394	Kartos Therapeutics, Inc.	Diffuse Large B Cell Lymphoma\|Chronic Lymphocytic Leukemia\|Non Hodgkin Lymphoma	February 23, 2021	Phase 1\|Phase 2
NCT03787264	German CLL Study Group	Chronic Lymphoid Leukemia	January 14, 2019	Phase 2
NCT04489797	AstraZeneca\|Acerta Pharma BV	Infectious Disease	July 20, 2020	Phase 1
NCT04646395	International Extranodal Lymphoma Study Group (IELSG)	Marginal Zone Lymphoma	October 20, 2021	Phase 2
NCT04647669	The University of The West Indies	Covid19	June 1, 2021	Phase 3
NCT02717611	Acerta Pharma BV	Chronic Lymphocytic Leukemia	March 8, 2016	Phase 2
NCT04189757	M.D. Anderson Cancer Center\|National Cancer Institute (NCI)	Mantle Cell Lymphoma	August 7, 2020	Phase 2
NCT02970318	Acerta Pharma BV	Chronic Lymphocytic Leukemia	February 2, 2017	Phase 3
NCT03516617	Mayo Clinic\|National Cancer Institute (NCI)	Chronic Lymphocytic Leukemia\|Small Lymphocytic Lymphoma	September 10, 2018	Phase 2
NCT04906902	Dana-Farber Cancer Institute	Central Nervous System Lymphoma\|Refractory Central Nervous System Lymphoma\|Recurrent Central Nervous System Lymphoma	August 23, 2021	Phase 1\|Phase 2
NCT03328273	Acerta Pharma BV	Chronic Lymphocytic Leukemia	July 15, 2020	Phase 1
NCT05557695	AstraZeneca\|UKCLL Forum	Chronic Lymphocytic Leukemia, CLL	October 17, 2022
NCT05065554	Jorge J. Castillo, MD\|AstraZeneca\|Dana-Farber Cancer Institute	IgM MGUS\|Waldenstrom Macroglobulinemia\|Neuropathy;Peripheral	November 16, 2021	Phase 2
NCT03736616	Swedish Medical Center\|Acerta Pharma BV	Diffuse Large B Cell Lymphoma	August 16, 2019	Phase 2
NCT02448303	Acerta Pharma BV\|Merck Sharp & Dohme LLC	Carcinoma, Non-Small-Cell Lung	May 2015	Phase 2
NCT04505254	M.D. Anderson Cancer Center\|National Cancer Institute (NCI)	Chronic Lymphocytic Leukemia\|Small Lymphocytic Lymphoma	August 25, 2020	Phase 2
NCT04898101	Acerta Pharma BV	Healthy Volunteers	March 3, 2016	Phase 1
NCT04914936	Acerta Pharma BV	Healthy Participants	September 21, 2014	Phase 1
NCT03932331	AstraZeneca	Phase I: Relapsed or Refractory B-cell Malignancies\|Phase II Cohort A: Relapsed or Refractory Mantle Cell Lymphoma\|Phase II Cohort B: Relapsed or Refractory Chronic Lymphocytic Leukemia	April 29, 2020	Phase 1\|Phase 2
NCT04657094	City of Hope Medical Center\|National Cancer Institute (NCI)	Autoimmune Hemolytic Anemia\|Chronic Lymphocytic Leukemia\|Chronic Lymphocytic Leukemia+Small Lymphocytic Lymphoma\|Warm Antibody Autoimmune Hemolytic Anemia	March 16, 2021	Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL ( 537.05 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1482 mL	10.7409 mL	21.4818 mL
5 mM	0.4296 mL	2.1482 mL	4.2964 mL
10 mM	0.2148 mL	1.0741 mL	2.1482 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (4.47 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (4.47 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (4.47 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[1] Wu J, et al. Acalabrutinib (ACP-196): a selective second-generation BTK inhibitor. J Hematol Oncol. 2016 Mar 9;9:21
[2] Herman SE, et al. The Bruton's tyrosine kinase (BTK) inhibitor acalabrutinib demonstrates potent on-target effects and efficacy in two mouse models of chronic lymphocytic leukemia. Clin Cancer Res. 2016 Nov 30

Synonyms

Benzamide, 4-[8-amino-3-[(2S)-1-(1-oxo-2-butyn-1-yl)-2-pyrrolidinyl]imidazo[1,5-a]pyrazin-1-yl]-N-2-pyridinyl-

4-[8-Amino-3-[(2S)-1-(1-oxo-2-butyn-1-yl)-2-pyrrolidinyl]imidazo[1,5-a]pyrazin-1-yl]-N-2-pyridinylbenzamide

Acalabrutinib

ACP 196

(S)-4-[8-Amino-3-[1-(but-2-ynoyl)pyrrolidin-2-yl]imidazo[1,5-a]pyrazin-1-yl]-N-(pyridin-2-yl)benzamide

Calquence

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