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TSU-68 (SU6668,Orantinib) Sale

(Synonyms: SU6668; TSU-68) 目录号 : GC16732

An inhibitor of select receptor tyrosine kinases

TSU-68 (SU6668,Orantinib) Chemical Structure

Cas No.:252916-29-3

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥378.00
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5mg
¥378.00
现货
10mg
¥693.00
现货
50mg
¥2,160.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

Ki: Flk-1trans-phosphorylation (2.1 mM), FGFR1 trans-phosphorylation (1.2 mM), and PDGFR autophosphorylation (0.008 mM).

Vascular endothelial growth factor, fibroblast growth factor (FGF), and platelet-derived growth factor (PDGF) and their cognate receptor tyrosine kinases are strongly implicated in angiogenesis associated with solid tumors. TSU-68 is a novel inhibitor of these receptors.

In vitro: Biochemical kinetic studies using isolated Flk-1, FGF receptor 1, and PDGF receptor β kinases revealed that TSU-68 has competitive inhibitory properties with respect to ATP. In cellular systems, TSU-68 inhibited receptor tyrosine phosphorylation and mitogenesis after stimulation of cells by appropriate ligands [1].

In vivo: Oral or i.p. administration of TSU-68 in athymic mice resulted in significant growth inhibition of a diverse panel of human tumor xenografts of glioma, melanoma, lung, colon, ovarian, and epidermoid origin [1].

Clinical trial: Phase I clinical study indicated that TSU-68 can be safely combined with standard doses of carboplatin-paclitaxel, with the combination manifesting promising antitumor activity [2].

References:
[1] Laird AD, Vajkoczy P, Shawver LK et al.  SU6668 is a potent antiangiogenic and antitumor agent that induces regression of established tumors. Cancer Res. 2000 Aug 1;60(15):4152-60.
[2] Okamoto I, Yoshioka H, Takeda K et al.  Phase I clinical study of the angiogenesis inhibitor TSU-68 combined with carboplatin and paclitaxel in chemotherapy-naive patients with advanced non-small cell lung cancer. J Thorac Oncol. 2012 Feb;7(2):427-33.

Chemical Properties

Cas No. 252916-29-3 SDF
别名 SU6668; TSU-68
化学名 3-[2,4-dimethyl-5-[(Z)-(2-oxo-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid
Canonical SMILES CC1=C(NC(=C1CCC(=O)O)C)C=C2C3=CC=CC=C3NC2=O
分子式 C18H18N2O3 分子量 310.35
溶解度 ≥ 15.5mg/mL in DMSO 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 3.2222 mL 16.1108 mL 32.2217 mL
5 mM 0.6444 mL 3.2222 mL 6.4443 mL
10 mM 0.3222 mL 1.6111 mL 3.2222 mL
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