|5-((5-氟-2-氧代吲哚-3-亚基)甲基)-N-(2-羟基-3-吗啉代丙基)-2,4-二甲基-1H-吡咯-3-甲酰胺|CsnPharm

CAS No.: 627908-92-3

SU14813 Catalog No. CSN12692

Synonyms: SU-014813

SU14813 is an oral, multitargeted tyrosine kinase inhibitor (TKI) targeting vascular endothelial growth factor receptors (VEGFR), platelet-derived growth factor receptors (PDGFR), Kit, and fms-like tyrosine kinase 3 (FLT-3).

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技术信息

生物活性

描述SU14813 is a multi-targeted receptor tyrosine kinases inhibitor with IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT. SU14813 inhibits the growth of U-118MG with an IC50 of 50 to 100 nM. SU14813 inhibited VEGFR (vascular endothelial growth factor receptor)-2, PDGFR (platelet-derived growth factor receptor)-beta, and FLT3 (fms-like tyrosine kinase 3) phosphorylation in xenograft tumors in a dose- and time-dependent fashion. SU14813 inhibited target RTK (Receptor tyrosine kinases) activity in vivo in association with reduction in angiogenesis, target RTK-mediated proliferation, and survival of tumor cells, leading to broad and potent antitumor efficacy. Treatment in combination with docetaxel significantly enhances both the inhibition of primary tumor growth and the survival of the tumor-bearing mice compared with administration of either agent alone^[3]. SU14813 has manageable safety and tolerability and allows once-daily continuous oral dosing. SU14813 shows dose-proportional pharmacokinetics, with target plasma concentrations achieved at doses ≥ 100 mg/day^[4].
参考文献

[1] Hu-Lowe D, Brega N, et al. The discovery and development of SU14813, a next-generation multitargeted tyrosine kinase inhibitor for the treatment of human malignancies. Mol Cancer Ther. 2011 Nov;10(11):2015.
[2] Patyna S, Laird AD, et al. SU14813: a novel multiple receptor tyrosine kinase inhibitor with potent antiangiogenic and antitumor activity. Mol Cancer Ther. 2006 Jul;5(7):1774-82.
[3] Patyna S, Laird AD, Mendel DB, O'farrell AM, Liang C, Guan H, Vojkovsky T, Vasile S, Wang X, Chen J, Grazzini M, Yang CY, Haznedar JO, Sukbuntherng J, Zhong WZ, Cherrington JM, Hu-Lowe D. SU14813: a novel multiple receptor tyrosine kinase inhibitor with potent antiangiogenic and antitumor activity. Mol Cancer Ther. 2006 Jul;5(7):1774-82
[4] Fiedler W, Giaccone G, Lasch P, van der Horst I, Brega N, Courtney R, Abbattista A, Shalinsky DR, Bokemeyer C, Boven E. Phase I trial of SU14813 in patients with advanced solid malignancies. Ann Oncol. 2011 Jan;22(1):195-201

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2600 mL
- 11.2999 mL
- 22.5997 mL
- 5 mM
- 0.4520 mL
- 2.2600 mL
- 4.5199 mL
- 10 mM
- 0.2260 mL
- 1.1300 mL
- 2.2600 mL

技术信息

CAS号

627908-92-3

储存条件

粉末: Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H27FN4O4

运输

蓝冰

分子量

442.48

别名

SU-014813

溶解度

DMSO	88.0 mg/mL (198.9 mM)
Water	Insoluble
Ethanol	Insoluble

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