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Acalabrutinib

Catalog No. T3626 CAS 1420477-60-6

Synonyms: ACP-196

Acalabrutinib (ACP-196), also known as ACP-196, is an orally available inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity. Upon administration, ACP-196 inhibits the activity of BTK and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. This prevents both B-cell activation and BTK-mediated activation of downstream survival pathways. This leads to an inhibition of the growth of malignant B cells that overexpress BTK. BTK, a member of the src-related BTK/Tec family of cytoplasmic tyrosine kinases, is overexpressed in B-cell malignancies; it plays an important role in B lymphocyte development, activation, signaling, proliferation and survival.

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Acalabrutinib, CAS 1420477-60-6

Pack Size	Availability	Price/USD
5 mg	In stock	$ 39.00
10 mg	In stock	$ 55.00
25 mg	In stock	$ 75.00
50 mg	In stock	$ 97.00
100 mg	In stock	$ 155.00
200 mg	In stock	$ 239.00
500 mg	In stock	$ 395.00
1 mL * 10 mM (in DMSO)	In stock	$ 43.00

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Purity: 99.95%

Purity: 99.43%

Purity: 99.02%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Acalabrutinib (ACP-196), also known as ACP-196, is an orally available inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity. Upon administration, ACP-196 inhibits the activity of BTK and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. This prevents both B-cell activation and BTK-mediated activation of downstream survival pathways. This leads to an inhibition of the growth of malignant B cells that overexpress BTK. BTK, a member of the src-related BTK/Tec family of cytoplasmic tyrosine kinases, is overexpressed in B-cell malignancies; it plays an important role in B lymphocyte development, activation, signaling, proliferation and survival.
Targets&IC50	BTK:3nM
In vitro	When administered orally to mice, ACP-196 demonstrably inhibits the expression of CD86 in CD19+ spleen cells induced by anti-IgM in a dose-dependent manner, with an ED50 of 0.34 mg/kg. This inhibition exceeded 90% of CD86 expression levels after 3 hours post-treatment.
In vivo	Acalabrutinib does not inhibit EGFR, ITK, and TEC, and does not affect the phosphorylation of EGFR at the Y1068 and Y1173 sites. It has a higher IC50 value than ibrutinib and shows almost no inhibitory activity on the kinase activities of ITK, EGFR, ERBB2, ERBB4, JAK3, BLK, FGR, FYN, HCK, LCK, LYN, SRC, and YES1. In in vitro signal detection in primary human chronic lymphocytic leukemia cells, Acalabrutinib inhibits the tyrosine phosphorylation of downstream targets ERK, IKB, and AKT.

Synonyms	ACP-196
Molecular Weight	465.51
Formula	C26H23N7O2
CAS No.	1420477-60-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 53 mg/mL(113.9 mM)

DMSO: 86 mg/mL (184.7 mM)

References and Literature

1. Wu J, et al. J Hematol Oncol. 2016, 9:21. 2. Heather L. Gardner, et al .Cancer Res. 2014, 74(19 Supplement):1744. 3. Todd Covey, et al. Cancer Res. 2015, 75 (15 Supplement):2596.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Tyrosine Kinase Inhibitor Library Anti-Cancer Clinical Compound Library EMA Approved Drug Library Anti-Cancer Active Compound Library Anti-Cancer Approved Drug Library Highly Selective Inhibitor Library Inhibitor Library Drug Repurposing Compound Library Bioactive Compounds Library Max

Related Products

Related compounds with same targets

GDC-0834 JAK3/BTK-IN-1 JDB175 JNJ-64264681 Sunvozertinib (±)-Zanubrutinib BTK-IN-25 QL47

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Keywords

Acalabrutinib 1420477-60-6 Angiogenesis Tyrosine Kinase/Adaptors BTK on-target CLL phosphorylation orally chronic leukemia Inhibitor ERK ACP196 ACP 196 AKT tyrosine lymphocytic Btk inhibit Cys481 ACP-196 PLCγ2 Bruton tyrosine kinase irreversible IKB inhibitor

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