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Acalabrutinib(ACP-196)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Acalabrutinib(ACP-196)图片
CAS NO:1420477-60-6
规格:≥98%
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议
2g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)465.51
FormulaC26H23N7O2
CAS No.1420477-60-6
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 93 mg/mL (199.8 mM)
Water: <1 mg/mL
Ethanol: 93 mg/mL (199.8 mM)
Solubility (In vivo)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
SynonymsAcalabrutinib; ACP-196; ACP196; ACP 196
实验参考方法
In Vitro

In vitro activity: 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.


Kinase Assay: Previous study showed that ACP-196 had high selectivity for Btk when tested against a panel of 395 non-mutant kinases, which was associated with the reduced intrinsic reactivity of ACP-196's electrophile. Moreover, ACP-196 could not inhibit EGFR, Itk or Txk, which is unlike ibrutinib. In addition, the phosphoflow assays on EGFR expressing cell lines furthre confirmed ibrutinib's EGFR inhibition without inhibition observed for ACP-196.


Cell Assay: the phosphoflow assays on EGFR expressing cell lines furthre confirmed ibrutinib's EGFR inhibition without inhibition observed for ACP-196.

In VivoOral 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.
Animal modelMice
Formulation & Dosage 25 mg/kg; oral
ReferencesJ Hematol Oncol. 2016 Mar 9;9:21; Cancer Res. 2015, 75 (15 Supplement):2596