In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50: 3 nM
ACP-196 is an irreversible BTK inhibitor.
Bruton's tyrosine kinase (BTK) is a critical component of B cell receptor signalling and functions as an key regulator of cell proliferation and survival in various B cell malignancies.
In vitro: 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 .
In vivo: Oral administration of ACP-196 in mice led to the dose-dependent inhibition of anti-IgM-induced CD86 expression in CD19+ splenocytes. In addition, a similar model was used to compare the duration of Btk inhibition after a single oral dose of 25 mg/kg, and the results showed that ACP-196 and ibrutinib inhibited CD86 expression >90% at 3h and around 50% at 24h postdose .
Clinical trial: Previous study found that ACP-196 at an oral dose of 100 mg/day showed more than 90% target coverage over a 24h period in healthy volunteers. Moreover, the Btk occupancy and regulation of CD69 and CD86 correlated with PK exposure. In CLL patients, 7 days of dosing with ACP-196 at 200 mg QD resulted in a 94% Btk target occupancy .
 http://cancerres. aacrjournals.org/content/75/15_Supplement/2596
|Physical Appearance||A solid|
|Storage||Store at -20°C|
|Solubility||≥46.6 mg/mL in DMSO with gentle warming; insoluble in H2O; ≥13.86 mg/mL in EtOH|
|Canonical SMILES||O=C(NC1=NC=CC=C1)C2=CC=C(C3=C4C(N)=NC=CN4C([[email protected]]5N(C(C#CC)=O)CCC5)=N3)C=C2|
|Shipping Condition||Evaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.|
|General tips||For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.|