ACP-196 (Synonyms: ACP-196) |
| Catalog No.GC15453 |
L'ACP-196 (ACP-196) est un inhibiteur de BTK de deuxième génération, actif par voie orale, irréversible et hautement sélectif. ACP-196 se lie de manière covalente À Cys481 dans la poche de liaison À l'ATP de BTK. L'ACP-196 démontre de puissants effets ciblés et une efficacité dans des modèles murins de leucémie lymphoÏde chronique (LLC).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1420477-60-6
Sample solution is provided at 25 µL, 10mM.
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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
| Cas No. | 1420477-60-6 | SDF | |
| Synonymes | 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
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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.
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 6 reference(s) in Google Scholar.)
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