UNC2025 hydrochloride | whatman (沃特曼)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

UNC2025 hydrochloride 纯度: 99.41%

UNC2025 hydrochloride 是一种强效、ATP 竞争性，高口服活性的 Mer/Flt3 抑制剂，IC₅₀ 值分别为 0.74 nM 和 0.8 nM。UNC2025 hydrochloride 对 MERTK 的选择性是 Axl 的 45 倍(IC₅₀=122nM; K_i=13.3 nM)。UNC2025 hydrochloride 具有良好的 PK 特性，可用于急性白血病的研究。

UNC2025 hydrochloride Chemical Structure

CAS No. : 2070015-17-5

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1129	In-stock
2 mg	￥600	In-stock
5 mg	￥1000	In-stock
10 mg	￥1700	In-stock
25 mg	￥2800	In-stock
50 mg	￥4800	In-stock
100 mg	￥8000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

UNC2025 hydrochloride 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Kinase Inhibitor Library
Protein Tyrosine Kinase Compound Library
Anti-Cancer Compound Library
Orally Active Compound Library
Anti-Blood Cancer Compound Library

生物活性

UNC2025 hydrochloride is a potent, ATP-competitive, and highly orally active Mer/Flt3 inhibitor with IC₅₀ values of 0.74 nM and 0.8 nM, respectively. UNC2025 hydrochloride is >45-fold selectivity for MERTK relative to Axl (IC₅₀= 122 nM; K_i = 13.3 nM). UNC2025 hydrochloride exhibits an excellent PK properties, and can be used for the investigation of acute leukemia^[1].

IC₅₀ & Target

IC50: 0.74 nM (Mer); 0.8 nM (Flt3)^[1]

体外研究
(In Vitro)

UNC2025 is against FLT3, MER, AXL, TRKA, TRKC, QIK, TYRO3, SLK, NuaK1, KIT and Met with IC₅₀ values of 0.35 nM, 0.46 nM, 1.65 nM, 1.67 nM, 4.38 nM, 5.75 nM, 5.83 nM, 6.14 nM, 7.97 nM , 8.18 nM and 364 nM, respectively^[1].
UNC2025 (0-60 nM; 1 hour) mediates potent inhibition of Mer phosphorylation with an IC₅₀ of 2.7 nM in 697 B-ALL cells^[1].
UNC2025 (0-60 nM; 1 hour) results in decreased phosphorylation of Flt3 with an IC₅₀ of 14 nM in Flt3-ITD positive Molm-14 acute myeloid leukemia cells^[1].
UNC2025 (3 nM-3 μM; 1 hour) decreases p-MEK, p-AXL, p-TYRO3 expression as a concentration manner in 32D Cells^[1].
UNC2025 (14 nM–10 μM; 48 hours) inhibits MERTK signaling and colony-forming potential in a MERTK-expressing patient sample with a 20-fold difference in sensitivity of MERTK-expressing leukemia blasts relative to normal cord or marrow blood mononuclear cells^[2].
UNC2025 (25-300 nM; 1 hour) mediates potent and dose-dependent decreases in MERTK phosphorylation/activation in both cell lines and inhibition of MERTK correlated with decreased phosphorylation of previously reported MERTK-dependent signaling components STAT6, AKT, and ERK1/2^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:	32D Cells
Concentration:	0 nM, 3 nM, 10 nM, 20 nM, 30 nM, 100 nM, 1000 nM, 3000 nM
Incubation Time:	1 hour
Result:	Inhibited p-MEK, p-AXL, p-TYRO3 expression.

Cell Proliferation Assay^[1]

Cell Line:	Mononuclear cells
Concentration:	14 nM–10 μM
Incubation Time:	48 hours
Result:	Showed IC₅₀ values ranged from 9.0 nM to >10 μM with a median IC₅₀ of 2.38 μM.

Western Blot Analysis^[2]

Cell Line:	Kasumi-1 AML and 697 B-ALL cells
Concentration:	25-300 nM
Incubation Time:	48 hours
Result:	Decresed p-MERTK, p-STAT6, p- AKT and p-ERK1/2 expression as a dose-dependent manner.

体内研究
(In Vivo)

UNC2025 (intravenous injection or oral adminstration; 3 mg/kg) exhibits an excellent PK properties: low clearance (9.2 mL/min kg), longer half-life (3.8 h), and high oral exposure (100%), it shows T_max, C_max, and AUClast 0.50 hour, 1.6 μM, and 9.2 h μM, respectively^[2].
UNC2025 (orally adminstration; 50 or 75 mg/kg; 34 and 70 days) mediates a statistically significant dose-dependent reduction in tumor burden relative to vehicle. mediates dose-dependent increases in median survival from 26 days after initiation of treatment in vehicle-treated mice, to 34 and 70 days in mice treated with 50 or 75 mg/kg UNC2025, respectively^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	NSG mice injected with 697 B-ALL cells^[2]
Dosage:	50 or 75 mg/kg
Administration:	Oral adminstration
Result:	Delayed the disease progression.

分子量

513.12

Formula

C₂₈H₄₁ClN₆O

CAS 号

2070015-17-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

H₂O : 55 mg/mL (107.19 mM; Need ultrasonic)

DMSO : 10 mg/mL (19.49 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9489 mL	9.7443 mL	19.4886 mL
5 mM	0.3898 mL	1.9489 mL	3.8977 mL
10 mM	0.1949 mL	0.9744 mL	1.9489 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 (sealed storage, away from moisture)。-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： PBS

Solubility: 100 mg/mL (194.89 mM); Clear solution; Need ultrasonic
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 1 mg/mL (1.95 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (1.95 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 1 mg/mL (1.95 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (1.95 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 10.0 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。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Zhang W, et al. UNC2025, a Potent and Orally Bioavailable MER/FLT3 Dual Inhibitor. J Med Chem. 2014 Aug 28;57(16):7031-41.

[2]. DeRyckere D, et al. UNC2025, a MERTK Small-Molecule Inhibitor, Is Therapeutically Effective Alone and in Combination with CL14377 in Leukemia Models.Clin Cancer Res. 2017 Mar 15;23(6):1481-1492.

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