Conteltinib - CAS:1384860-29-0

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Conteltinib (Synonyms:CT-707)

目录号 : KM5079 CAS No. : 1384860-29-0 纯度 : 98%

Data Sheet 产品使用指南

Conteltinib (CT-707) 是一种多激酶抑制剂，可靶向作用于 FAK，ALK 和 Pyk2。Conteltinib (CT-707) 对 FAK 具有显着的抑制作用，IC₅₀ 为 1.6 nM。

规格	价格	是否有货
5mg		In-stock
10mg		In-stock
50mg		In-stock
100mg	询价	In-stock
200mg	询价	In-stock

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生物活性

Conteltinib (CT-707) is a multi-kinase inhibitor targeting FAK, ALK, and Pyk2. Conteltinib exerts significant inhibitory effect on FAK with an IC₅₀ of 1.6 nM.

IC₅₀&Target

IC50: 1.6 nM (FAK)

体外研究

Conteltinib (CT-707) synergizes with XL184 to suppress hepatocellular carcinoma by blocking XL184-induced FAK activation.
The combination of XL184 (5 μM) and Conteltinib (3 μM) significantly reduces the survival fraction, compared with each agent alone.
The combination of XL184 (5 μM) and Conteltinib (3 μM) results in enhanced caspase-dependent apoptosis in human hepatocellular carcinoma cell lines.
The FAK phosphorylation induced by XL184 (5 μM) might be involved in the synergistic antitumor effect of Conteltinib (3 μM) and XL184.

Cell Viability Assay

Cell Line:	The human hepatocellular carcinoma cell lines HepG2 and Bel-7402
Concentration:	1.0, 1.5, 2.0, 2.5, and 3.0 μM for HepG2 cells; 0.2, 0.4, 0.8, 1.5, and 3.0 μM for Bel-7402 cells
Incubation Time:	72 hours
Result:	When cells were exposed to XL184 (5 μM), Conteltinib (3 μM), or their combination, the survival rates were 57.3%, 39.3%, and 11.2%, respectively, in HepG2; those in Bel-7402 were 57.8%, 61.6%, and 34.2%, respectively.

Apoptosis Analysis

Cell Line:	HepG2 and Bel-7402 cells
Concentration:	3 μM
Incubation Time:	48 hours
Result:	The apoptosis rates of control, XL184, Conteltinib, and combination groups in HepG2 were 5.0%, 10.5%, 18.4%, and 41.1%, respectively, and those in Bel-7402 were 4.4%, 16.3%, 8.7%, and 36.4%, respectively.

Western Blot Analysis

Cell Line:	HepG2 and Bel-7402
Concentration:	3 μM
Incubation Time:	24 hours
Result:	Could markedly decrease FAK phosphorylation induced by XL184, which might partially account for the synergetic effect.

体内研究

The combination of XL184 (20 mg/kg once daily for first 3 days; i.g. 10 mg/kg once a day for 4th day; no administration from 5th to 10th days; i.g. 10 mg/kg once a day from the 10th to 14th days )and CT-707 (i.g. 50 mg/kg twice a day for first 3 days, 7th, 8th, 11th, 12th, and 14th days; once a day for 4th, 6th, 9th, 10th, and 13th days; no administration for the 5th day) shows the synergistic antitumor effect in HepG2 xenograft nude mice.

Animal Model:	Nude mice transplanted with HepG2 xenografts
Dosage:	50 mg/kg
Administration:	Intragastrically (i.g.) twice a day for first 3 days, 7th, 8th, 11th, 12th, and 14th days; once a day for 4th, 6th, 9th, 10th, and 13th days; no administration for the 5th day.
Result:	Caused a moderate decrease in the relative tumor volume (RTV). The inhibition rate of combination group reached 77.4%, whereas the mono-treatment of XL184 or CT-707 alone caused 30.7% and 19.4% inhibition in the tumor weight, respectively.

分子式

C₃₂H₄₅N₉O₃S

分子量

635.82

CAS号

1384860-29-0

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

溶解性数据

In Vitro:

DMSO : 31.25 mg/mL (49.15 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5728 mL	7.8639 mL	15.7277 mL
5 mM	0.3146 mL	1.5728 mL	3.1455 mL
10 mM	0.1573 mL	0.7864 mL	1.5728 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 (3.27 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.27 mM，饱和度未知) 的澄清溶液。
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。
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (3.27 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.27 mM，饱和度未知) 的澄清溶液。
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。
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.27 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.27 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
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玉米油中，混合均匀。

临床试验

纯度： 98%

Data Sheet

产品使用指南

暂无相关参考文献

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

浓度

体积

分子量*

重置计算

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

重置计算

动物实验计算换算器

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系客服为您提供正确的澄清溶液配方）

% DMSO

% Tween 80

% ddH₂O

% DMSO

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

Other Forms of Rapamycin:

KKL 顾客使用本产品发表的 0 篇科研文献

The molarity calculator equation

The dilution calculator equation

动物实验计算换算器