UNC569 - CAS:1350547-65-7

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UNC569

目录号 : KM8074 CAS No. : 1350547-65-7 纯度 : 98%

Data Sheet 产品使用指南

UNC569 是一种有效、可逆、ATP 竞争性且具有口服活性的 Mer 激酶抑制剂，IC₅₀ 为 2.9 nM，K_i 为 4.3 nM。UNC569 还抑制 Axl 和 Tyro3，IC₅₀ 分别为 37 nM 和 48 nM。UNC569 可用于急性淋巴细胞白血病 (ALL) 和非典型畸胎瘤/横纹肌瘤的研究。

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生物活性

UNC569 is a potent, reversible, ATP-competitive and orally active Mer kinase inhibitor with an IC₅₀ of 2.9 nM and a K_i of 4.3 nM. UNC569 also inhibits Axl and Tyro3 with IC₅₀s of 37 nM and 48 nM, respectively. UNC569 can be used for acute lymphoblastic leukemia (ALL) and atypical teratoid/rhabdoid tumors research

体外研究

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.

Apoptosis Analysis

Cell 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 Analysis

Cell 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.

体内研究

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.

分子式

C₂₂H₂₉FN₆

分子量

396.50

CAS号

1350547-65-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 31.25 mg/mL (78.81 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5221 mL	12.6103 mL	25.2207 mL
5 mM	0.5044 mL	2.5221 mL	5.0441 mL
10 mM	0.2522 mL	1.2610 mL	2.5221 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.31 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.31 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。