Acalabrutinib [1420477-60-6]
Cat# T3626-10mg
Size : 10mg
Marca : TargetMol
Acalabrutinib
Contact us for more batch information
Purity:99.95%
Resource Download
COA HPLC HNMR
Acalabrutinib
Catalog No. T3626Cas No. 1420477-60-6
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.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose. Pack Size | |
---|---|
5 mg | |
10 mg | |
25 mg | |
50 mg | |
100 mg | |
200 mg | |
500 mg | |
1 mL x 10 mM (in DMSO) |
Product Introduction
Bioactivity
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. |
Alias | 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 | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | Ethanol: 53 mg/mL (113.9 mM) DMSO: 86 mg/mL (184.7 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
|
Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSO
main solution, add 300 μLPEG300
mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O
mix well and clarify
Dose Conversion
You can also refer to dose conversion for different animals. More
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
Keywords
on-targetAcalabrutinibCLLphosphorylationorallychronicleukemiaInhibitorERKACP196ACP 196AKTtyrosinelymphocyticBtkinhibitCys481PLCγ2Bruton tyrosine kinaseirreversibleIKB
Related Tags: buy Acalabrutinib | purchase Acalabrutinib | Acalabrutinib cost | order Acalabrutinib | Acalabrutinib chemical structure | Acalabrutinib in vivo | Acalabrutinib in vitro | Acalabrutinib formula | Acalabrutinib molecular weight