Sunitinib malate
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Sunitinib malate是一种新型的、可口服的和多靶点的小分子羟吲哚酪氨酸激酶抑制剂,抑制多种受体酪氨酸激酶,包括血小板衍生的生长因子受体、血管内皮生长因子受体1、2和3、C- KIT、FLT3激酶、集落刺激因子1受体和RET激酶[2] [3] [4]。在NB细胞系,Sunitinib malate的IC50值约为10-20 ng/ml [1]。
受体酪氨酸激酶激活了许多不同的细胞内信号通路[5]。在神经母细胞瘤(NB)细胞系、SKN-BE(2)、NUB-7、SH-SY5Y和LAN-5细胞系中,使用sunitinib malate处理48小时,sunitinib malate以浓度依赖性的方式显著抑制细胞增殖[1]。
使用20、30或40 mg/kg的sunitinib malate孵育接种异种移植肿瘤的NOD /SCID小鼠,原发肿瘤的生长显著减少(P < 0.05,SK-N-BE减少49%,NB12肿瘤减少55%,T / C:平均处理的肿瘤质量/平均对照肿瘤块)。将静脉注射106 SK-N-BE(2) 7天的小鼠使用不同剂量的sunitinib malate(20、30或40mg/kg)治疗14天,与对照组相比,肿瘤数量和转移部位明显减小,小鼠肝脏重量差异显著[1]。
参考文献:
[1]. Libo Zhang, Kristen M. Smith, Amy Lee Chong, et al. In Vivo Antitumor and Antimetastatic Activity of Sunitinib in Preclinical Neuroblastoma Mouse Model. Neoplasia, 2009, 11: 426-435.
[2]. Hassane Izzedine, Irina Buhaescu, Olivier Rixe, et al. Sunitinib malate. Cancer Chemother Pharmacol, 2007, 60: 357-364.
[3]. M. L. Telli, R. M. Witteles, G. A. Fisher, et al. Cardiotoxicity associated with the cancer therapeutic agent sunitinib malate. Annals of Oncology, 2008, 19: 1613–1618.
[4]. Edwin P. Rock, Vicki Goodman, Janet X. Jiang, et al. Food and Drug Administration Drug Approval Summary: Sunitinib Malate for the Treatment of Gastrointestinal Stromal Tumor and Advanced Renal Cell Carcinoma. The Oncologist, 2007, 12: 107-113.
[5]. C. J. Marshall. Specificity of Receptor Tyrosine Kinase Signaling: Transient versus Sustained Extracellular Signal-Regulated Kinase Activation. Cel, 1995, 80: 179-185.
- 1.Wu F, Wu D, et al. "Generation of hepato-biliary organoids from human induced pluripotent stem cells." J Hepatol. 2019 Jan 7. pii: S0168-8278(19)30002-9. PMID:30630011
- 2.Lin M, Chen B. "Advances in the drug therapies of acute myeloid leukemia (except acute wpromyelocytic leukemia)." Drug Des Devel Ther. 2018 Apr 30;12:1009-1017. PMID:29750014
Physical Appearance | A solid |
Storage | Store at 4°C |
M.Wt | 532.56 |
Cas No. | 341031-54-7 |
Formula | C22H27FN4O2·C4H6O5 |
Synonyms | SU 11248,SU11248,SU-11248,Sunitinib |
Solubility | ≥26.65 mg/mL in DMSO; insoluble in EtOH; ≥4.6 mg/mL in H2O with ultrasonic |
Chemical Name | N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide;(2S)-2-hydroxybutanedioic acid |
SDF | Download SDF |
Canonical SMILES | CCN(CC)CCNC(=O)C1=C(NC(=C1C)C=C2C3=C(C=CC(=C3)F)NC2=O)C.C(C(C(=O)O)O)C(=O)O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1]: | |
细胞系 |
NIH-3T3细胞,HUVECs |
溶解方法 |
该化合物在DMSO中的溶解度大于10 mM.。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。 |
应用 |
在血清饥饿的表达VEGFR2或PDGFRβ的NIH-3T3细胞中,Sunitinib抑制VEGF依赖性VEGFR2磷酸化和PDGF依赖性PDGFRβ磷酸化。Sunitinib抑制VEGF诱导的血清饥饿HUVEC的增殖,IC50为40 nM,抑制PDGFβ或PDGFRα过表达的NIH-3T3细胞中PDGF诱导的增殖,IC50分别为39 nM和69 nM。 |
动物实验 [1]: | |
动物模型 |
携带HT-29、A431、Colo205、H-460、SF763T、C6、A375或MDA-MB-435细胞的肿瘤异种移植小鼠模型 |
给药剂量 |
口服给药,20-80 mg/kg/day,每日一次 |
应用 |
Sunitinib (20-80 mg/kg/day)对各种肿瘤异种移植模型表现出广泛和有效的剂量依赖性抗肿瘤活性,包括HT-29、A431、Colo205、H-460、SF763T、C6、A375或MDA-MB-435。Sunitinib (80 mg/kg/day) 处理21天导致8只小鼠中的6只完全的肿瘤消退,在治疗结束后的110天观察期间没有肿瘤再生长现象。Sunitinib显著降低肿瘤MVD,在SF763T胶质瘤肿瘤中减少约40%。SU11248完全抑制了表达荧光素酶的PC-3M异种移植物额外的肿瘤生长,尽管肿瘤大小没有减少。 |
注意事项 |
由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。 |
References: [1]. Mendel D B, Laird A D, Xin X, et al. In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors[J]. Clinical Cancer Research, 2003, 9(1): 327-337. |
描述 | Sunitinib malate是VEGFR2和PDGFRβ的RTK多靶点抑制剂,IC50值为80 nM 和2 nM。 | |||||
靶点 | VEGFR2 (Flk-1) | PDGFRβ | ||||
IC50 | 80 nM | 2 nM |
质量控制和MSDS
- 批次: