UNC569 - 10mM in DMSO , CAS No.1350547-65-7

CAS: 1350547-65-7 Cat. No.: U654519 分子式: C₂₂H₂₉FN₆ 分子量: 396.50 PubChem CID: 53355503

グレード＆純度 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

概要

UNC569 is a potent, reversible, ATP-competitive and orally active Mer kinase inhibitor with an IC 50 of 2.9 nM and a K i of 4.3 nM. UNC569 also inhibits Axl and Tyro3 with IC 50 s of 37 nM and 48 nM, respectively. UNC569 can be used for acute lymphoblastic leukemia (ALL) and atypical teratoid/rhabdoid tumors research

In Vitro

UNC569 (24 hours) induces apoptosis in ALL cell lines, and increases the levels of cleaved Caspase 3 and cleaved PARP. UNC569 (1 µM; 1.5 hours) treatment effectively inhibit the activation of Mer and downstream signaling, including the PI3K/AKT and MAPK/ERK pathways. UNC569 (1 hour) inhibits Mer phosphorylation levels with IC50 values of 141 nM and 193 nM in human B-ALL (acute lymphoblastic leukemia) 697 and Jurkat cell lines, respectively . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Apoptosis AnalysisCell Line: 697 and Jurkat cells Concentration: 0.4 µM, 0.8 µM, 1 µM, 1.2 µM, 1.4 µM, 1.6 µM, 1.8 µM, 2 µM Incubation Time: 24 hours Result: Induced apoptosis in ALL cell lines. Western Blot AnalysisCell Line: 697 and Jurkat cells Concentration: 1 µM Incubation Time: 1.5 hours Result: Inhibited Mer activation and downstream signaling through ERK1/2 and AKT.

In Vivo

The in vivo pharmacokinetic properties of UNC569 (3 mg/kg) are also assessed in mice via both intravenous (IV) and oral (PO) administration. UNC569 has low systemic clearance (19.5 mL/min/kg), high volume of distribution (V ss of 5.83 L/kg), and good oral bioavailability (57%) . Leukemic zebrafish are treated continuously for 2 weeks by immersion in 4 µM UNC569. the result shows that UNC569 induces more than 50% reduction in tumor burden compared with vehicle- and mock-treated fish. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50& Target:IC50: 2.9 nM (Mer), 37 nM (Axl), 48 nM (Tyro3), Ki: 4.3 nM (Mer)

仕様

仕様と純度

10mM in DMSO

生化学的・生理学的メカニズム

UNC569 is a potent, reversible, ATP-competitive and orally active Mer kinase inhibitor with an IC 50 of 2.9 nM and a K i of 4.3 nM. UNC569 also inhibits Axl and Tyro3 with IC 50 s of 37 nM and 48 nM, respectively. UNC569 can be used for acute lymphoblasti

保管条件

Store at -80°C

入荷

Dry ice packs + Cold packs

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

名前と識別子

異性体SMILES

CCCCNC1=NC=C2C(=NN(C2=N1)CC3CCC(CC3)N)C4=CC=C(C=C4)F

PubChem CID

53355503

MeSH用語

UNC569

分子量

396.50

よくある質問

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1350547-65-7, the molecular formula is C22H29FN6, and the molecular weight is 396.50 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.