Acalabrutinib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种新型、不可逆、共价第二代 BTK 抑制剂，IC50 为 3 nM。

A novel, irreversible, covalent second-generation BTK inhibitor with IC50 of 3 nM; more potent and selective than ibrutinib, and does not inhibit EGFR, Itk or Txk; inhibits tyrosine phosphorylation of downstream targets of ERK, IKB, and AKT, in the in vitro signaling assay on primary human CLL cells; inhibits anti-IgM-induced CD86 expression in CD19+ splenocytes with an ED50 of 0.34 mg/kg in mice; has promising safety and efficacy profiles for CLL treatment; orally active.Blood Cancer Approved(In Vitro):Acalabrutinib (ACP-196) inhibits tyrosine phosphorylation of downstream targets of ERK, IKB, and AKT, in the in vitro signaling assay on primary human CLL cells. In the human CLL NSG xenograft model, Acalabrutinib demonstrates on-target effects including decreased phosphorylation of PLCγ2, ERK and significant inhibition of CLL cell proliferation.Acalabrutinib inhibits purified BTK with an IC50 of 3 nM and an EC50 of 8 nM in a human whole-blood CD69 B cell activation assay. Acalabrutinib has improved target specificity over ibrutinib with 323-, 94-, 19-, and 9-fold selectivity over the other TEC kinase family members (ITK, TXK, BMX, and TEC , respectively) and no activity against EGFR.(In Vivo):Acalabrutinib (100 mg twice per day) assessed for thrombus formation at injured arterioles of the mice, exhibits more selective for inhibiting BTK and has virtually no inhibition of platelet activity.

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ACP-196 | APC196

Tyrosine Kinase

BTK

BTK

Cancer

Blood cancer

1420477-60-6

465.5065

C26H23N7O2

>98% (HPLC)

DMSO: ≥ 31 mg/mL

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

Benzamide, 4-[8-amino-3-[(2S)-1-(1-oxo-2-butyn-1-yl)-2-pyrrolidinyl]imidazo[1,5-a]pyrazin-1-yl]-N-2-pyridinyl-

(-20℃)

With Ice Pack

≥ 2 years