AAPK-25


Catalog No. Size PriceQuantity
M23698-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

AAPK-25 is a potent and selective Aurora/PLK dual inhibitor with anti-tumor activity, which can cause mitotic delay and arrest cells in a prometaphase, reflecting by the biomarker histone H3Ser10 phosphorylation and followed by a surge in apoptosis. AAPK-25 targets Aurora-A, -B, and -C with Kd values ranging from 23-289 nM, as well as PLK-1, -2, and -3 with Kd values ranging from 55-456 nM.

Product information

CAS Number: 2247919-28-2

Molecular Weight: 519.08

Formula: C30H35ClN4O2

Chemical Name: 4-[(6-chloro-2-methoxyacridin-9-yl)methyl]-2-({4-[2-(dimethylamino)ethyl]piperazin-1-yl}methyl)phenol

Smiles: CN(C)CCN1CCN(CC2=CC(CC3C4=CC(=CC=C4N=C4C=C(Cl)C=CC4=3)OC)=CC=C2O)CC1

InChiKey: FOMOXWWUGIIVIV-UHFFFAOYSA-N

InChi: InChI=1S/C30H35ClN4O2/c1-33(2)10-11-34-12-14-35(15-13-34)20-22-16-21(4-9-30(22)36)17-26-25-7-5-23(31)18-29(25)32-28-8-6-24(37-3)19-27(26)28/h4-9,16,18-19,36H,10-15,17,20H2,1-3H3

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

AAPK-25 inhibits HCT-116, Calu6, A549 and MCF-7 cells growth with IC50s of 0.4, 5.3, 11.6, and 2.3 μM, respectively. AAPK-25 induces apoptosis as a dose-dependent manner in HCT-116 cell line. AAPK-25 has significantly increased histone H3Ser10 phosphorylation, indicating a markedly mitotic block. AAPK-25 is in notably inhibition of the mitotic spindle checkpoint, which is mainly mediated by cell cycle signaling and mitotic pathways.

In Vivo:

AAPK-25 enhances survival rate in the BALB/c nude mice tumor xenograft model.

Products are for research use only. Not for human use.

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