Reagenti e strumenti per immunologia, biologia cellulare e biologia molecolare

Acalabrutinib [1420477-60-6]

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Cat# T3626-1mL

Size : 1mL

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Acalabrutinib

Purity:99.95%

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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.

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Pack Size
5 mg
10 mg
25 mg
50 mg
100 mg
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500 mg
1 mL x 10 mM (in DMSO)

Product Introduction

Bioactivity

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

Chemical Properties

Molecular Weight	465.51
Formula	C26H23N7O2
Cas No.	1420477-60-6

Storage & Solubility Information

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

	1mg	5mg	10mg	50mg
1 mM	2.1482 mL	10.7409 mL	21.4818 mL	107.4091 mL
5 mM	0.4296 mL	2.1482 mL	4.2964 mL	21.4818 mL
10 mM	0.2148 mL	1.0741 mL	2.1482 mL	10.7409 mL
20 mM	0.1074 mL	0.5370 mL	1.0741 mL	5.3705 mL
50 mM	0.0430 mL	0.2148 mL	0.4296 mL	2.1482 mL
100 mM	0.0215 mL	0.1074 mL	0.2148 mL	1.0741 mL

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Keywords

on-targetAcalabrutinibCLLphosphorylationorallychronicleukemiaInhibitorERKACP196ACP 196AKTtyrosinelymphocyticBtkinhibitCys481PLCγ2Bruton tyrosine kinaseirreversibleIKB