化合物 Crenolanib|T2677|TargetMol

Crenolanib
670220-88-9

￥464 2mg 起订

￥698 5mg 起订

￥1198 10mg 起订

上海更新日期：2024-09-29

TargetMol中国（陶术生物）

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联系人：邵小姐

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产品详情:

中文名称：: 化合物 Crenolanib

英文名称：: Crenolanib

CAS号：: 670220-88-9

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.28%

产品类别：: 抑制剂

货号：: T2677

Product Introduction

Bioactivity

Name	Crenolanib
Description	Crenolanib (ARO 002) is an orally bioavailable type III tyrosine kinases inhibitor of PDGFRα/β and FLT3 (IC50s: 11, 3.2, and 4 nM).
Cell Research	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].
Kinase Assay	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].
Animal Research	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].
In vitro	Crenolanib是一种特异性和强效的RTK抑制剂。对于野生型受体PDGFRA、PDGFRB和FLT3，Crenolanib的Kd分别为3.2、2.1和0.74 nmol/L。在EOL-1细胞系中，Crenolanib强效抑制融合癌基因的激酶活性（IC50值为21 nmol/L），并且显著抑制EOL-1细胞的增殖（IC50: 0.2 pmol/L）[1]。Crenolanib是ABCB1的底物，这一点由ABCB1过表达细胞对Crenolanib的大约五倍的抗性、ABCB1特异性抑制剂PSC-833对这种抗性的逆转以及Crenolanib对ABCB1 ATP酶活性的刺激所证明。相反，Crenolanib不是ABCG2或ABCC1的底物。此外，用药理学相关浓度的500 nM Crenolanib处理FLT3-ITD AML细胞系MV4-11和MOLM-14，并未诱导ABCB1细胞表面表达的上调[2]。Crenolanib治疗消除了HB119细胞以及源于AML患者的FLT3-ITD+细胞系Molm14中FLT3和ERK的磷酸化。50 nmol/L的Crenolanib抑制了包括一位Quizartinib耐药患者（其疾病出现了FLT3-ITD/D835Y突变）的白血病细胞中FLT3的磷酸化[3]。
In vivo	Crenolanib 显著抑制了肿瘤质量的增长，且在20 mg/kg的治疗剂量下观察到最强的抑制效果。Crenolanib 引发了肿瘤细胞大量的凋亡。此外，应用的 Crenolanib 剂量被接受鼠良好地耐受，治疗期间没有观察到体重损失[4]。来自正在进行的临床试验的相关数据显示，急性髓细胞性白血病患者能够达到足够的 Crenolanib 水平，以体内抑制 FLT3/ITD 及抵抗性赋予的 FLT3/D835 突变体[5]。
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	DMSO : 89 mg/mL (200.65 mM), Heating is recommended. Ethanol : 7 mg/mL (15.78 mM)
Keywords	Inhibitor \| FLT3 \| Platelet-derived growth factor receptor \| CD135 \| ARO002 \| PDGFR \| CP868596 \| CP 868596 \| Crenolanib \| Cluster of differentiation antigen 135 \| Autophagy \| inhibit \| Fms like tyrosine kinase 3 \| ARO-002
Inhibitors Related	Oxyresveratrol \| Guanidine hydrochloride \| Naringin \| Taurine \| Gefitinib \| Xylitol \| Hydroxychloroquine \| Curcumin \| Stavudine \| Myricetin \| Paeonol \| Sodium 4-phenylbutyrate
Related Compound Libraries	Inhibitor Library \| Bioactive Compound Library \| Anti-Cancer Active Compound Library \| Anti-Cancer Approved Drug Library \| Highly Selective Inhibitor Library \| Membrane Protein-targeted Compound Library \| Tyrosine Kinase Inhibitor Library \| Drug Repurposing Compound Library \| Anti-Cancer Clinical Compound Library \| Anti-Cancer Drug Library

CP-868596|||ARO 002|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

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