>>Signaling Pathways>> Angiogenesis>> BTK>>ACP-196

ACP-196 (Synonyms: ACP-196)

Catalog No.GC15453

ACP-196(ACP-196)은 경구 활성, 비가역적, 고도로 선택적인 2세대 BTK 억제제입니다. ACP-196은 BTK의 ATP 결합 주머니에 있는 Cys481에 공유 결합합니다. ACP-196은 만성 림프구성 백혈병(CLL) 마우스 모델에서 강력한 표적 효과와 효능을 보여줍니다.

Products are for research use only. Not for human use. We do not sell to patients.

ACP-196 Chemical Structure

Cas No.: 1420477-60-6

Size 가격 재고 수량
5mg
US$45.00
재고 있음
25mg
US$184.00
재고 있음
100mg
US$338.00
재고 있음

Tel:(909) 407-4943 Email: sales@glpbio.com

고객 리뷰

Based on customer reviews.

  • GlpBio Citations

    GlpBio Citations
  • Bioactive Compounds Premium Provider

    Bioactive Compounds Premium Provider

Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

View current batch:

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

Cas No. 1420477-60-6 SDF
Synonyms ACP-196
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
Canonical SMILES 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
Formula C26H23N7O2 M.Wt 465.51
Solubility ≥ 46.6mg/mL in DMSO with gentle warming Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.1482 mL 10.7409 mL 21.4818 mL
5 mM 0.4296 mL 2.1482 mL 4.2964 mL
10 mM 0.2148 mL 1.0741 mL 2.1482 mL
  • Molarity Calculator

  • Dilution Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
**When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / CoA (available online).

Calculate

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

리뷰

Review for ACP-196

Average Rating: 5 ★★★★★ (Based on Reviews and 6 reference(s) in Google Scholar.)

5 Star
100%
4 Star
0%
3 Star
0%
2 Star
0%
1 Star
0%
Review for ACP-196

GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.

Required fields are marked with *

You may receive emails regarding this submission. Any emails will include the ability to opt-out of future communications.