(Z)-Orantinib (Z-SU6668; (Z)-TSU-68)|cas:210644-62-5|西域试剂

(Z)-Orantinib (Z-SU6668; (Z)-TSU-68),99.02%

产品编号：Bellancom-10517A| CAS NO：210644-62-5| 分子式：C₁₈H₁₈N₂O₃| 分子量：310.35

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-10517A	￥600.00	杭州北京（现货）
Bellancom-10517A	￥1800.00	杭州北京（现货）
Bellancom-10517A	￥2700.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

(Z)-Orantinib (Z-SU6668; (Z)-TSU-68)

产品介绍

(Z)-Orantinib ((Z)-SU6668) 是一种有效，选择性，具有口服活性和 ATP 竞争性的 Flk‐1/KDR，PDGFRβ 和 FGFR1 抑制剂，IC₅₀ 值分别为 2.1，0.008 和 1.2 µM。(Z)-Orantinib 是有效的抗血管生成和抗肿瘤剂，可诱导已建立的肿瘤消退。

生物活性

(Z)-Orantinib ((Z)-SU6668) is a potent, selective, orally active and ATP competitive inhibitor of Flk‐1/KDR, PDGFRβ, and FGFR1, with IC₅₀s of 2.1, 0.008, and 1.2 µM, respectively. (Z)-Orantinib is a potent antiangiogenic and antitumor agent that induces regression of established tumors.

体外研究

SU6668 (5-15 min) inhibits Flk-1 trans-phosphorylation (K_i=2.1 μM), FGFR1 trans-phosphorylation (K_i=1.2 μM), and PDGFR autophosphorylation (K_i=0.008 μM).
SU6668 (0.03-10 μM; 60 min) inhibits the VEGF-stimulated increase of KDR tyrosine phosphorylation in HUVECs.
SU6668 inhibits mitogenesis of HUVECs induced by both VEGF and FGF in a dose-dependent manner with IC₅₀s of 0.34 and 9.6 μM, respectively.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

SU6668 (4-200 mg/kg/day; p.o. for 21 d) induces dose-dependent inhibition of A431 tumor growth in athymic mice.
SU6668 (75 mg/kg/day; i.p. for 22 d) significantly suppresses tumor angiogenesis and vascularization in mice.
SU6668 (200 mg/kg/day; p.o. for 11-27 d) induces striking regression of large established A431 xenografts in athymic mice.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female athymic mice (BALB/c, nu/nu) were implanted A431 tumor cells
Dosage:	4, 40, 75, 200 mg/kg
Administration:	P.o. daily for 21 days
Result:	Induced 97% growth inhibition against A431 tumor at the dose of 97%. No mortality was observed in any treatment group.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female athymic mice (BALB/c, nu/nu) were implanted A431 tumor cells
Dosage:	4, 40, 75, 200 mg/kg
Administration:	P.o. daily for 21 days
Result:	Induced 97% growth inhibition against A431 tumor at the dose of 97%. No mortality was observed in any treatment group.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (161.11 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	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

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 2.08 mg/mL (6.70 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (6.70 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.08 mg/mL (6.70 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (6.70 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

*以上所有助溶剂都可在西域网站选购。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

. Laird AD, 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. [Content Brief]

. Laird ad, et, al. SU6668 inhibits Flk-1/KDR and PDGFRbeta in vivo, resulting in rapid apoptosis of tumor vasculature and tumor regression in mice. FASEB J. 2002 May;16(7):681-90. [Content Brief]

化学品安全说明书(MSDS)

下载MSDS

质检证书(COA)

产品编号(Item Number)

批号(Lot Number)

(Z)-Orantinib (Z-SU6668; (Z)-TSU-68),99.02%

(Z)-Orantinib (Z-SU6668; (Z)-TSU-68)

化学品安全说明书(MSDS)

质检证书(COA)

在线咨询