A-7337 Acalabrutinib, Free Base, >99%

Synonyms : [ACP196]

Related Terms : [Calquence]

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  • 500 mg
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  • 1 g
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  • 2 g
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  • 5 g
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  • M.W. 465.51
  • C26H23N7O2
  • [1420477-60-6]

Solubility: DMSO.

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  • Acalabrutinib, also known as ACP-196, is an irreversible Bruton tyrosine kinase (BTK) inhibitor.  It binds covalently to Cys481 with improved selectivity and in vivo target coverage.   Acalabrutinib inhibited BTK with an IC50 of 3 nM and had 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.  Wu J., et al. "Acalabrutinib (ACP-196): a selective second-generation BTK inhibitor." J. Hematol. Oncol. 9: 21 (2016).
  • Acalabrutinib avoided major platelet dysfunction in non-Hodgkin lymphoma (NHL) patients associated with ibrutinib treatment.  Bye A.P., et al. "Severe platelet dysfunction in NHL patients receiving ibrutinib is absent in patients receiving acalabrutinib. Blood Adv. 1: 2610-2623 (2017).
  • In an uncontrolled, phase 1-2, multicenter study, the selective and irreversible BTK inhibitor acalabrutinib demonstrated promising safety and efficacy profiles in patients with relapsed chronic lymphocytic leukemia (CLL), including those with chromosome 17p13.1 deletion. Byrd J.C., et al. "Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia." N. Engl. J. Med. 374: 323-332 (2016).
  • Acalabrutinib is the active ingredient in the drug product sold under the trade name Calquence®.  This drug is currently approved in a least one country for treatment of adult patients with mantle cell lymphoma.  NOTE:  THE ACALABRUTINIB SOLD BY LC LABORATORIES FOR RESEARCH IS NOT CALQUENCE®, AND IS NOT FOR HUMAN USE.

  • Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.
  • This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.
  • Not available in some countries; not available to some institutions; not available for some uses.
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