Acalabrutinib (ACP196)

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Acalabrutinib (ACP196)

Acalabrutinib (ACP-196) is a clinical stage, second-generation irreversible inhibitor of BTK (Bruton's tyrosine kinase). The Optically Pure Acalabrutinib (ACP-196) potently inhibits BTK activity with an IC50 of 3 nM (enzymatic assay) and EC50 of 8 nM (human whole-blood CD69 B cell activation assay) (Ref. 2). Comparing with the first-generation BTK inhibitor Ibrutinib, ACP-196 is more selective. The improved selectivity is largely attributed to the reduced intrinsic reactivity of electrophile (ACP-196’s Propiolamide vs Ibrutinib’s Acrylamide). As a result, ACP-196 was shown to have improved target specificity and in vivo coverage, thus better therapeutic indexes, over Ibrutinib. It displays minimal, or no activities against off-target kinases such as ITK, EGFR, ERBB2, ERBB4, JAK3, BLK, FGR, FYN, HCK, LCK, LYN, SRC, and YES1 (Ref 1, 2). It is currently in clinical evaluation for the treatment of CCL (Chronic Lymphocytic Leukemia).

Catalog NO:	CT-ACP196
Synonym:	ACP-196, ACP 196
CAS NO:	1420477-60-6
Mol. Formula:	C26H23N7O2
MW:	465.5 (Refer to Certificate, batch-specific)

** A recrystallized white (with faint yellow tint) powder, clean (>99.8% by achiral HPLC), optically pure (100% by chiral HPLC) (Ref. 3), + clean 1H-NMR, + a high-precision quantitative elemental analysis. Bulk stock. Ship within 1 day.

Pricing and OrderingTechnical Data

QC & Certificates

References

NO	Size	Price	In Stock
1	10 mg	$100.00	YES
2	50 mg	$250.00	YES
3	100 mg	$350.00	YES
4	200 mg	$600.00	YES

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Solubility : Refer to Certificate

Storage : Refer to Certificate

Purity : >99.5% chem and optical purity by achiral and chiral HPLCs

Original QC Data : HPLC-MS, Chiral HPLC, 1HNMR and Quantitative Elemental Analysis

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ACP-196 (Acalabrutinib)), Lot 02, Certificate of Analysis.pdf
CHEMIETEK, ACP196, Lot 02, HPLC-MS.pdf
CHEMIETEK, ACP196, Lot 02, Chiral HPLC.pdf
CHEMIETEK, ACP196, Lot 02, (1-2) 1H-NMR.pdf
ACP-196 (Acalabrutinib), Lot 02, (2.1), Appearance (color).pdf

1. JC Byrd, et al, Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia. N Engl J Med. 2016 Jan 28;374(4):323-32

2. Covey T, et al, Abstract 2596: ACP-196: a novel covalent Bruton’s tyrosine kinase (Btk) inhibitor with improved selectivity and in vivo target coverage in chronic lymphocytic leukemia (CLL) patients. Cancer Res. 2015;75 (15 Supplement):2596.

3. Buyer Beware: Many other vendors, if not all, offer the product Acalabrutinib (ACP-196) (S- enantiomer) without reporting optical purity (by chiral HPLC) – trying to hide something? - too poor to report? No clue? The wrong isomer (R-enantiomer, an inactive ingredient) formed irresistibly (3-5%) during the synthesis, is to stay with the product if not removed, and only detectable by Chiral HPLC.