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UNC2881 Sale

目录号 : GC13500

A Mer kinase inhibitor

UNC2881 Chemical Structure

Cas No.:1493764-08-1

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥898.00
现货
10mg
¥923.00
现货
50mg
¥3,600.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

UNC2881 is a selective inhibitor of Mer tyrosine kinase [1].

Mer is a member of the TAM (Tyro3, Axl and Mer) receptor tyrosine kinase (RTK) subfamily with growth-arrest-specific-6 (Gas6) as an endogenous ligand. Mer plays an important role in platelet aggregation and macrophage activity.

UNC2881 is a novel and specific Mer tyrosine kinase inhibitor. In kinase inhibition assays, UNC2881 (430 nM) inhibited MER, FGFR1, KDR, EGFR, ITK and TRKA by greater than 50%. In 697 B-ALL cells, UNC2881 inhibited Mer phosphorylation with IC50 value of 22 nM. Also, UNC2881 inhibited ligand-dependent phosphorylation of a chimeric protein consisting of the intracellular domain of Mer and the extracellular domain of the epidermal growth factor receptor (EGFR). In human platelet-rich plasma, UNC2881 inhibited platelet aggregation induced by fibrillar Type I equine collagen by greater than 25%. UNC2881 also inhibited ATP release, a marker of platelet activation [1].

In mice, UNC2881 exhibited 14% oral bioavailability and high systemic clearance. UNC2881 was sufficient for in vitro or short-term in vivo studies [1].

Reference:
[1].  Zhang W, McIver AL, Stashko MA, et al. Discovery of Mer specific tyrosine kinase inhibitors for the treatment and prevention of thrombosis. J Med Chem, 2013, 56(23): 9693-9700.

Chemical Properties

Cas No. 1493764-08-1 SDF
Canonical SMILES O[C@H]1CC[C@H](CC1)NC2=NC(NCCCC)=NC=C2C(NCC(C=C3)=CC=C3N4C=CN=C4)=O
分子式 C25H33N7O2 分子量 463.58
溶解度 ≥ 13.55mg/mL in DMSO 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

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1 mg 5 mg 10 mg
1 mM 2.1571 mL 10.7856 mL 21.5712 mL
5 mM 0.4314 mL 2.1571 mL 4.3142 mL
10 mM 0.2157 mL 1.0786 mL 2.1571 mL
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