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ACP-196

Catalog No.
B6185
不可逆的BTK抑制剂
组合的产品项目
规格价格库存 数量
5mg
¥ 750.00
现货
25mg
¥ 2,780.00
现货
100mg
¥ 6,980.00
现货

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Background

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 [1].

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 [1].

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 [1].

Reference:
[1] http://cancerres. aacrjournals.org/content/75/15_Supplement/2596

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt465.51
Cas No.1420477-60-6
FormulaC26H23N7O2
Solubility≥46.6mg/mL in DMSO with gentle warming
Chemical Name(S)-4-(8-amino-3-(1-(but-2-ynoyl)pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-N-(pyridin-2-yl)benzamide
SDFDownload SDF
Canonical SMILESO=C(NC1=NC=CC=C1)C2=CC=C(C3=C4C(N)=NC=CN4C([C@H]5N(C(C#CC)=O)CCC5)=N3)C=C2
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

质量控制

化学结构

ACP-196