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Acalabrutinib

Cat. No. M5306
Acalabrutinib Structure
Synonym:

ACP-196

Size Price Availability Quantity
5mg USD 80 In stock
10mg USD 140 In stock
50mg USD 410 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

In vitro: In the in vitro signaling assay on primary human CLL cells, acalabrutinib inhibits tyrosine phosphorylation of downstream targets of ERK, IKB, and AKT. Acalabrutinib demonstrates higher selectivity for BTK with IC50 determinations on nine kinases with a cysteine residue in the same position as BTK. Importantly, unlike ibrutinib, acalabrutinib does not inhibit EGFR, ITK, or TEC. acalabrutinib has no effect on EGFR phosphorylation on tyrosine residues Y1068 and Y1173. Compared with ibrutinib, acalabrutinib has much higher IC50(>1000 nM) or virtually no inhibition on kinase activities of ITK, EGFR, ERBB2, ERBB4, JAK3, BLK, FGR, FYN, HCK, LCK, LYN, SRC, and YES1. In vivo: oral administration of ACP-196 in mice results in dose-dependent inhibition of anti-IgM-induced CD86 expression in CD19+ splenocytes with an ED50 of 0.34 mg/kg compared to 0.91 mg/kg for ibrutinib. A similar model is used to compare the duration of Btk inhibition after a single oral dose of 25 mg/kg. ACP-196 inhibits CD86 expression >90% at 3h postdose.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 465.51
Formula C26H23N7O2
CAS Number 1420477-60-6
Purity >99%
Solubility 93 mg/mL in DMSO
Storage at -20°C
References

Acalabrutinib (ACP-196): a selective second-generation BTK inhibitor.
Wu J, et al. J Hematol Oncol. 2016 Mar 9;9:21. PMID: 26957112.

Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia.
Byrd JC, et al. N Engl J Med. 2016 Jan 28;374(4):323-32. PMID: 26641137.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Acalabrutinib, ACP-196 supplier, BTK, inhibitors

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