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Telatinib

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Chemical Structure| 332012-40-5 同义名 : Bay 57-9352
CAS号 : 332012-40-5
货号 : A485916
分子式 : C20H16ClN5O3
纯度 : 99%+
分子量 : 409.826
MDL号 : MFCD18251453
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 45 mg/mL(109.8 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • VEGFR3

    VEGFR3, IC50:4 nM

  • VEGFR2

    VEGFR2, IC50:6 nM

  • PDGFRα

    PDGFRα, IC50:15 nM

  • c-Kit

    c-Kit, IC50:1 nM
描述 Telatinib is a potent inhibitor of VEGFR2/3, c-Kit and PDGFRα with IC50 of 6 nM/4 nM, 1 nM and 15 nM, respectively.
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00952497 Gastric Cancer Phase 2 Completed - United States, California ... 展开 >> UCSF Helen Diller Family Comprehensive Cancer Center San Francisco, California, United States, 94115 United States, Georgia Central Georgia Cancer Care, P.C. Macon, Georgia, United States, 31201 United States, Pennsylvania University of Pennsylvania, Abramson Cancer Center Philadelphia, Pennsylvania, United States, 19104 United States, Tennessee The West Clinic Memphis, Tennessee, United States, 38120 United States, Texas The University of Texas MD Anderson Cancer Center Houston, Texas, United States, 77030 Spain Hospital Vall d' Hebron Barcelona, Spain, 08035 Hospital Universitari Germans Trias i Pujol Barcelona, Spain, 08916 Hospital Universitario Ramon y Cajal Madrid, Spain, 28034 Hospital Clinico San Carlos Madrid, Spain, 28040 Hospital Universitario 12 de Octubre Madrid, Spain, 28041 Hospital Universitario Marques de Valdecilla Santander, Spain, 39008 收起 <<
NCT03175497 Solid Tumor, Adult Phase 1 Recruiting June 1, 2018 China ... 展开 >> Fudan University, Zhongshan Hospital Recruiting Shanghai, China Contact: Taishu Liu 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.44mL

0.49mL

0.24mL

12.20mL

2.44mL

1.22mL

24.40mL

4.88mL

2.44mL
参考文献

[1]Steeghs N, Gelderblom H, et al. Hypertension and rarefaction during treatment with telatinib, a small molecule angiogenesis inhibitor. Clin Cancer Res. 2008 Jun 1;14(11):3470-6.

[2]Strumberg D, Schultheis B, et al. Phase I dose escalation study of telatinib (BAY 57-9352) in patients with advanced solid tumours. Br J Cancer. 2008 Nov 18;99(10):1579-85.