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DDR1-IN-2

产品编号 T5402 CAS 1429617-90-2

别名: DDR1 inhibitor 7rh

DDR1-IN-2 (DDR1 inhibitor 7rh) 是盘状结构域受体 1 抑制剂 (IC50:13.1 nM)，对 DDR2 的抑制作用相对较弱 (IC50:203 nM)。

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DDR1-IN-2, CAS 1429617-90-2

规格	价格/CNY	货期
1 mg	￥ 523	现货
5 mg	￥ 1,230	现货
10 mg	￥ 1,990	现货
25 mg	￥ 3,990	现货
50 mg	￥ 5,680	现货
100 mg	￥ 7,930	现货
500 mg	￥ 15,900	现货
1 mL * 10 mM (in DMSO)	￥ 1,480	现货

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	DDR1-IN-2 (DDR1 inhibitor 7rh) (DDR1 inhibitor 7rh) is a potent, selective, ATP-competitive Discoidin domain receptor 1 (DDR1) inhibitor (IC50: 6.8 nM in cell-free kinase assays).
靶点活性	DDR2:101.4 nM (cell free), DDR1:6.8 nM (cell free)
体外活性	DDR1-IN-2 inhibited the enzymatic activity of DDR1, with IC50 values of 6.8 nM, but were significantly less potent in suppressing the kinase activities of DDR2, Bcr-Abl, and c-Kit. It bound with DDR1 with a Kd value of 0.6 nM, while it was significantly less potent to the other 455 kinases tested. It also potently inhibited the proliferation of cancer cells expressing high levels of DDR1 and strongly suppressed cancer cell invasion, adhesion, and tumorigenicity [1]. Pharmacologic inhibition of DDR1 with an ATP-competitive orally available small-molecule kinase inhibitor (DDR1-IN-2) abrogated collagen-induced DDR1 signaling in pancreatic tumor cells and consequently reduced colony formation and migration [2].
体内活性	DDR1-IN-2 possessed good PK profiles, with oral bioavailabilities of 67.4% [1]. The inhibition of DDR1 with DDR1-IN-2 showed striking efficacy in combination with chemotherapy in orthotopic xenografts and autochthonous pancreatic tumors where it significantly reduced DDR1 activation and downstream signaling, reduced primary tumor burden, and improved chemoresponse [2].
激酶实验	The functional assays of compounds on the kinase activities of c-kit and Abl were determined using the FRET-based Z'-Lyte assay system according to the manufacturer's instructions. Tyrosine 2 Peptide was used as Abl substrate and Ser/Thr 6 peptide was used as the substrate for c-kit. The reactions were carried out in 384-well plates in a 10 μl of reaction volume with an appropriate amount of kinases in 50 mM HEPES (pH 7.5), 10 mM MgCl2, 1 mM EGTA, and 0.01% Brij-35. The reactions were incubated 1 hour at room temperature in the presence of 2 μM of substrate with 10 μM of ATP (for Abl1 assays) or 300 μM of ATP (kit assay) and in the presence of various concentrations of the compounds. The development reagent was then added for further 2 hours room temperature incubation followed by the addition of stop solution. Fluorescence signal ratio of 445 nm (Coumarin)/520 nm (fluorescin) was examined on EnVision Multilabel Reader. The effects of compounds on the kinases DDR1 and DDR2 were assessed by using a LanthaScreen Eu kinase activity assay technology. Kinase reactions are performed in a 10 μL volume in low-volume 384-well plates. The kinases in reaction buffer consist of 50 mM HEPES pH 7.5, 0.01% BRIJ-35, 10 mM MgCl2, and 1 mM EGTA, the concentration of Fluorescein-Poly GAT Substrate in the assay is 100 nM, Kinase reactions were initiated with the addition of 100 nM ATP in the presence of serials of dilutions of compounds. The reactions were allowed to proceed for 1 hour at room temperature before a 10 μL preparation of EDTA (20 mM) and Eu-labeled antibody (4 nM) in TR-FRET dilution buffer are added. The final concentration of antibody in the assay well is 2 nM, and the final concentration of EDTA is 10 mM. The plate is allowed to incubate at room temperature for one more hour before the TR-FRET emission ratios of 665 nm/340 nm were acquired on a PerkinElmer EnVision Multilabel Reader [1].
细胞实验	Adherent Cells were plated in 96-well culture plates with a cell density of 3000-4000 cells/well and treated with indicated compounds by adding 100μL medium containing compounds of various concentrations on the second day. After 72-hour's treatment, MTT was added to each well and incubated for additional 4-5 hours, and the absorbance was measured on a microplate reader at 570nm. Cell growth inhibition was evaluated as the ratio of the absorbance of the sample to that of the control. The results are representative of at least 4 independent experiments [1].
动物实验	Compounds 7rh and 7rj were dissolved in mixed solvents (DMSO : EtOH:Cremophor EL : H2O = 2 : 4 : 4 : 90) as clear solution. The final concentrations were 2.5 mg/mL. Sprague Dawley (SD) rats (male, 4 animals per group) weighted 180~220g were injected intravenously or administrated orally at doses of 5 mg/kg (i.v.) or 25mg/kg (p.o.), respectively. After dose administration, 0.3 mL of the orbital blood was taken at 2.0 min, 10.0 min, 30.0 min, 1.0 h, 2.0 h, 3.0 h, 4.0 h, 6.0 h, 8.0 h, 12.0 h, 21.0 h, 24.0 h, 30.0 h, 36.0 h, 48.0 h, and 72.0 h. Samples were stored at -70℃ until shipment to the analytical laboratory and tested by HPLC/MS using propranolol as internal standard to measure the compound concentration in the blood [1].

别名	DDR1 inhibitor 7rh
分子量	546.59
分子式	C30H29F3N6O
CAS No.	1429617-90-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 12 mg/mL (21.95 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8295 mL	9.1476 mL	18.2952 mL	45.7381 mL
	5 mM	0.3659 mL	1.8295 mL	3.659 mL	9.1476 mL
	10 mM	0.183 mL	0.9148 mL	1.8295 mL	4.5738 mL
	20 mM	0.0915 mL	0.4574 mL	0.9148 mL	2.2869 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Gao M, et al. Discovery and optimization of 3-(2-(Pyrazolo[1,5-a]pyrimidin-6-yl)ethynyl)benzamides as novel selective and orally bioavailable discoidin domain receptor 1 (DDR1) inhibitors. J Med Chem. 2013 Apr 25;56(8):3281-95. 2. Aguilera KY, et al. Inhibition of Discoidin Domain Receptor 1 Reduces Collagen-mediated Tumorigenicity in Pancreatic Ductal Adenocarcinoma. Mol Cancer Ther. 2017 Nov;16(11):2473-2485.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

DDR1-IN-2 1429617-90-2 Tyrosine Kinase/Adaptors Discoidin Domain Receptor (DDR) DDR1 IN 2 Discoidin Domain Receptor Inhibitor DDR1 inhibitor 7rh 7rh inhibit DDR-1-IN-2 DDR1IN2 inhibitor

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DDR1-IN-2

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords