Pazopanib Hydrochloride
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.
Pazopanib HCl(帕唑帕尼盐酸)是一种受体酪氨酸激酶抑制剂,靶向多种激酶,包括VEGFR1、VEGFR2、VEGFR3、PDGFR、FGFR、c-Kit和C-FMS,IC50分别为10 nM、30 nM、47 nM、84 nM、74 nM、140 nM和146 nM[1-3]。帕唑帕尼通过抑制这些受体来抑制肿瘤的生长和血管生成。临床前研究表明它对几种人肿瘤异种移植物的抗肿瘤活性,包括肾癌、前列腺癌、结肠癌、肺癌、黑色素瘤、头颈癌和乳腺癌[4]。它在动物模型中具有理想的药代动力学特征和口服生物利用度[4]。
帕唑帕尼已被全球多个监管部门批准用于晚期/转移性肾细胞癌和晚期软组织肉瘤的治疗,包括美国FDA、EMA、MHRA和TGA。在软组织肉瘤的临床试验中,接受安慰剂的患者的中位无进展生存期(PFS)为1.6个月,与之相比,帕唑帕尼将患者的PFS提高为4.6个月[5]。在肾细胞癌试验中,帕唑帕尼将中位PFS从4.2个月(安慰剂)增加到9.2个月[5]。帕唑帕尼最常见的副作用是腹泻、高血压、毛色变化、恶心、疲劳、食欲不振以及呕吐[6]。
参考文献:
1. Verweij J, Sleijfer S. Pazopanib, a new therapy for metastatic soft tissue sarcoma. Expert Opin Pharmacother 2013; 14: 929-935.
2. Pick AM, Nystrom KK. Pazopanib for the treatment of metastatic renal cell carcinoma. Clin Ther 2012; 34: 511-520.
3. Bukowski RM, Yasothan U, Kirkpatrick P. Pazopanib. Nat Rev Drug Discov 2010; 9: 17-18.
4. Sonpavde G, Hutson TE. Pazopanib: a novel multitargeted tyrosine kinase inhibitor. Curr Oncol Rep 2007; 9: 115-119.5.http://www.cancer.gov/cancertopics/druginfo/fda-pazopanibhydrochloride6.http://www.gsksource.com/gskprm/en/US/adirect/gskprmcmd=ProductDetailPage&product_id=1336067580985&featureKey=603422
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 473.98 |
Cas No. | 635702-64-6 |
Formula | C21H24ClN7O2S |
Synonyms | GW786034;Votrient;Armala;GW 786034;GW-786034 |
Solubility | ≥11.1 mg/mL in H2O; ≥11.85 mg/mL in DMSO; ≥2.88 mg/mL in EtOH |
Chemical Name | 5-[[4-[(2,3-dimethylindazol-6-yl)-methylamino]pyrimidin-2-yl]amino]-2-methylbenzenesulfonamide;hydrochloride |
SDF | Download SDF |
Canonical SMILES | CC1=C(C=C(C=C1)NC2=NC=CC(=N2)N(C)C3=CC4=NN(C(=C4C=C3)C)C)S(=O)(=O)N.Cl |
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。 |
Description | Pazopanib(GW786034)是一种新型的多靶点抑制剂,对VEGFR1、VEGFR2、VEGFR3、PDGFR、FGFR、c-Kit和C-FMS的IC50分别为10 nM、30 nM、47 nM、84 nM、74 nM、140 nM和146 nM。 | |||||
靶点 | VEGFR1 | VEGFR2 | VEGFR3 | PDGFR | FGFR | |
IC50 | 10 nM | 30 nM | 47 nM | 84 nM | 74 nM |
质量控制和MSDS
- 批次: