CCG-222740,99.85%

产品编号:Bellancom-121750| CAS NO:1922098-69-8| 分子式:C23H19ClF2N2O3| 分子量:444.86

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 包装 价格 库存与货期 购买量 操作
Bellancom-121750
3100.00 杭州 北京(现货)
Bellancom-121750
4900.00 杭州 北京(现货)
Bellancom-121750
8700.00 杭州 北京(现货)
Bellancom-121750
14000.00 杭州 北京(现货)
Bellancom-121750
19000.00 杭州 北京(现货)

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CCG-222740

产品介绍 CCG-222740 是一种口服有效的,选择性 Rho/MRTF 途径抑制剂。CCG-222740 也是有效的 α-平滑肌肌动蛋白蛋白表达抑制剂。CCG-222740 有效减少皮肤纤维化并阻止黑色素瘤转移。
生物活性

CCG-222740 is an orally active and selective Rho/myocardin-related transcription factor (MRTF) pathway inhibitor. CCG-222740 is also a potent inhibitor of alpha-smooth muscle actin protein expression. CCG-222740 effectively reduces fibrosis in skin and blocks melanoma metastasis.

体外研究

CCG-222740 (10, 20 μM; for 72 hours) increases the protein levels of p27 and decreases cyclin D1. CCG-222740 decreases cell viability of CAFs, with an IC50 of ~10 μM.
CCG-222740 (10, 25 μM) is potent at decreasing αSMA protein expression in human conjunctival fibroblasts.
CCG-222740 has an IC50 of 5 μM in a fibroblast-mediated collagen contraction assay, and it is less cytotoxic.

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

Cell Cycle Analysis

Cell Line: Cancer associated fibroblasts (CAFs)
Concentration: 10, 20 μM
Incubation Time: 72 hours
Result: Increased the protein levels of p27 and decreased cyclin D1.
体内研究
(In Vivo)

CCG-222740 (oral gavage; 100 mg/kg/day for 7 days) significantly reduces α-SMA levels in the pancreas of caerulein-stimulated KC mice.

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

Animal Model: KC mice (LSL-KrasG12D/+; Pdx-1-Cre) of age at 9 weeks
Dosage: 100 mg/kg
Administration: Oral gavage; daily; for 7 days
Result: Reduced α-SMA levels in the pancreas of caerulein-stimulated KC mice.
体内研究

CCG-222740 (oral gavage; 100 mg/kg/day for 7 days) significantly reduces α-SMA levels in the pancreas of caerulein-stimulated KC mice.

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

Animal Model: KC mice (LSL-KrasG12D/+; Pdx-1-Cre) of age at 9 weeks
Dosage: 100 mg/kg
Administration: Oral gavage; daily; for 7 days
Result: Reduced α-SMA levels in the pancreas of caerulein-stimulated KC mice.
体内研究

CCG-222740 (oral gavage; 100 mg/kg/day for 7 days) significantly reduces α-SMA levels in the pancreas of caerulein-stimulated KC mice.

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

Animal Model: KC mice (LSL-KrasG12D/+; Pdx-1-Cre) of age at 9 weeks
Dosage: 100 mg/kg
Administration: Oral gavage; daily; for 7 days
Result: Reduced α-SMA levels in the pancreas of caerulein-stimulated KC mice.
性状Solid
溶解性数据
In Vitro: 

DMSO : 125 mg/mL (280.99 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2479 mL 11.2395 mL 22.4790 mL
5 mM 0.4496 mL 2.2479 mL 4.4958 mL
10 mM 0.2248 mL 1.1239 mL 2.2479 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: ≥ 2.25 mg/mL (5.06 mM); Clear solution

    此方案可获得 ≥ 2.25 mg/mL (5.06 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 22.5 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: 2.25 mg/mL (5.06 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.25 mg/mL (5.06 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 22.5 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
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.25 mg/mL (5.06 mM); Clear solution

    此方案可获得 ≥ 2.25 mg/mL (5.06 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 22.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*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

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