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Crenolanib

产品编号 T2677 CAS 670220-88-9

别名: ARO 002, CP-868596

Crenolanib (ARO 002) 是一种口服生物可利用的 III 型酪氨酸激酶抑制剂，抑制 FLT3和 PDGFRα/β的 IC50分别为 4、11和 3.2 nM。

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Crenolanib, CAS 670220-88-9

规格	价格/CNY	货期
2 mg	￥ 464	现货
5 mg	￥ 698	现货
10 mg	￥ 1,198	现货
25 mg	￥ 1,997	现货
50 mg	￥ 3,197	现货
100 mg	￥ 4,280	现货
1 mL * 10 mM (in DMSO)	￥ 777	现货

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其他形式的 Crenolanib:

Crenolanib besylate
询价

选择批次

纯度: 99.28%

纯度: 98.40%

纯度: 97.45%

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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	Crenolanib (ARO 002) is an orally bioavailable type III tyrosine kinases inhibitor of PDGFRα/β and FLT3 (IC50s: 11, 3.2, and 4 nM).
靶点活性	FLT3:0.74 nmol/L (Kd), PDGFRβ:2.1 nmol/L (Kd), PDGFRα:3.2 nmol/L (Kd)
体外活性	Crenolanib is a specific and potent inhibitor of RTK. The Kd of crenolanib for the wild-type receptors PDGFRA, PDGFRB, and FLT3 was 3.2, 2.1, and 0.74 nmol/L, respectively. In EOL-1 cell line, Crenolanib potently inhibits the kinase activity of the fusion oncogene with IC50 values of 21 nmol/L. In addition, it potently inhibits the proliferation of EOL-1 cells (IC50: 0.2 pmol/L) [1]. Crenolanib is a substrate of ABCB1, as evidenced by approximate five-fold resistance of ABCB1-overexpressing cells to crenolanib, reversal of this resistance by the ABCB1-specific inhibitor PSC-833 and stimulation of ABCB1 ATPase activity by crenolanib. In contrast, crenolanib was not a substrate of ABCG2 or ABCC1. Finally, incubation of the FLT3-ITD AML cell lines MV4-11 and MOLM-14 with crenolanib at a pharmacologically relevant concentration of 500 nM did not induce upregulation of ABCB1 cell surface expression [2]. Crenolanib treatment abolished phosphorylation of FLT3 and ERK in HB119 cells, as well as in the AML-patient–derived FLT3–ITD+ cell line Molm14. Fifty nanomolar crenolanib suppressed phosphorylation of FLT3 in primary isolates, including in leukemic blasts from a quizartinib-resistant patient whose disease had evolved an FLT3–ITD/D835Y mutation [3].
体内活性	Crenolanib significantly inhibited the growth of tumor mass, and the strongest inhibitory effect was observed with 20 mg/kg treatment. Crenolanib induced massive apoptosis in tumor cells. Furthermore, the dosage of crenolanib applied was well tolerated by recipient mice. No weight loss was observed during the course of treatment [4]. Correlative data from an ongoing clinical trial demonstrate that acute myeloid leukemia patients can achieve sufficient levels of crenolanib to inhibit both FLT3/ITD and resistance-conferring FLT3/D835 mutants in vivo [5].
激酶实验	Chinese hamster ovary (CHO) cells were transiently transfected with mutated KIT or PDGFRA cDNA constructs and treated with various concentrations of imatinib or crenolanib as previously described. Experiments involving recombinant DNA were carried out using biosafety level 2 conditions in accordance with published guidelines. Protein lysates from cell lines were prepared and subjected to immunoprecipitation using anti-KIT or anti-PDGFRA antibodies followed by sequential immunoblotting for phospho-KIT and total KIT, or phosphotyrosine or total PDGFRA, respectively, as previously reported. Densitometry was carried out to quantify drug effect using Photoshop 5.1 software, with the level of phospho-KIT or phospho-PDGFRA normalized to total protein. Densitometry and proliferation experimental results were analyzed using Calcusyn 2.1 software to mathematically determine the IC50 values. The Wilcoxon rank sum test was used to compare the IC50 values of imatinib and crenolanib for a given mutation [1].
细胞实验	Cells were added to 96-well plates at densities of 20,000 cells per well and incubated with imatinib or crenolanib for 72 hours before measuring cellular proliferation using a 2,3-bis[2-methoxyl-4-nitro-5-sulfophenyl]-2H-tetrazolium-5-carboxanilide (XTT)–based assay [1].
动物实验	A549 cells were injected into the axillary regions of mice (2×10^6 cells/mouse). When the tumor volumes reached 70 mm^3, the mice were randomly allocated to the control group, low-dose crenolanib group (10 mg/kg), or high-dose crenolanib group (20 mg/kg) (n=6 per group). The vehicle for crenolanib treatment consists of 10% 1-methyl-2-pyrrolidinone and 90% polyethylene glycol 300. The tumor size and mouse body weight were measured every other day for about 2 weeks. The tumor volume was calculated as follows: (mm^3) = (width × width × length)/2. After treatment, the mice were euthanized using carbon dioxide, and the tumors were harvested and analyzed [4].

别名	ARO 002, CP-868596
化合物与蛋白结合的复合物	Crystal Structure of the Human CAMKK2B in complex with Crenolanib
分子量	443.54
分子式	C26H29N5O2
CAS No.	670220-88-9

存储

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

溶解度

DMSO: 89 mg/mL (200.65 mM), Heating is recommended.

Ethanol: 7 mg/mL (15.78 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 / Ethanol	1 mM	2.2546 mL	11.2729 mL	22.5459 mL	56.3647 mL
	5 mM	0.4509 mL	2.2546 mL	4.5092 mL	11.2729 mL
	10 mM	0.2255 mL	1.1273 mL	2.2546 mL	5.6365 mL
DMSO	20 mM	0.1127 mL	0.5636 mL	1.1273 mL	2.8182 mL
	50 mM	0.0451 mL	0.2255 mL	0.4509 mL	1.1273 mL
	100 mM	0.0225 mL	0.1127 mL	0.2255 mL	0.5636 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. Heinrich MC, et al.Crenolanib inhibits the drug-resistant PDGFRA D842V mutation associated with imatinib-resistant gastrointestinal stromal tumors. Clin Cancer Res, 2012, Jun 27. 2. Mathias TJ, et al. The FLT3 and PDGFR inhibitor crenolanib is a substrate of the multidrug resistance protein ABCB1 but does not inhibit transport function at pharmacologically relevant concentrations. Invest New Drugs. 2015 Apr;33(2):300-9. 3. Smith CC, et al. Crenolanib is a selective type I pan-FLT3 inhibitor. Proc Natl Acad Sci U S A. 2014 Apr 8;111(14):5319-24. 4. Wang P, et al. Crenolanib, a PDGFR inhibitor, suppresses lung cancer cell proliferation and inhibits tumor growth in vivo. Onco Targets Ther. 2014 Sep 26;7:1761-8. 5. Galanis A, et al. Crenolanib is a potent inhibitor of FLT3 with activity against resistance-conferring point mutants. Blood. 2014 Jan 2;123(1):94-100.

文献引用

1. Lin Q, Qin M, Zhao S, et al. The roles of PDGFRα signaling in the postnatal development and functional maintenance of the SMC‐ICC‐PDGFRα+ cell (SIP) syncytium in the colon. Neurogastroenterology & Motility. 2019, 31(5): e13568

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

Crenolanib 670220-88-9 Angiogenesis Autophagy Tyrosine Kinase/Adaptors FLT PDGFR Inhibitor FLT3 Platelet-derived growth factor receptor CD135 ARO002 ARO 002 CP868596 CP 868596 Cluster of differentiation antigen 135 CP-868596 inhibit Fms like tyrosine kinase 3 ARO-002 inhibitor

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Crenolanib

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

文献引用

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