1. Cell Cycle/DNA Damage
  2. CDK
  3. Trilaciclib

Trilaciclib  (Synonyms: G1T28)

目录号: HY-101467 纯度: 98.66%
COA 产品使用指南

Trilaciclib 是 CDK4/6 的抑制剂,对于 CDK4CDK6IC50 值分别为 1 nM 和 4 nM。

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Trilaciclib Chemical Structure

Trilaciclib Chemical Structure

CAS No. : 1374743-00-6

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规格 价格 是否有货 数量
1 mg ¥390
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5 mg ¥1150
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10 mg ¥1650
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50 mg ¥4000
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100 mg ¥5800
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200 mg   询价  
500 mg   询价  

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Other Forms of Trilaciclib:

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Trilaciclib is a CDK4/6 inhibitor with IC50s of 1 nM and 4 nM for CDK4 and CDK6, respectively.

IC50 & Target

IC50: 1 nM (CDK4), 4 nM (CDK6)[1]

体外研究
(In Vitro)

与 Trilaciclib (G1T28) 孵育 24 小时可诱导强烈的 G1 细胞周期停滞 (时间=0)。Trilaciclib 清除后 16 小时,细胞已重新进入细胞周期并表现出与未处理的对照细胞相似的细胞周期动力学。这些结果表明 Trilaciclib 引起短暂的、可逆的 G1 停滞。CDK4/6 敏感细胞中 Trilaciclib 介导的瞬时 G1 细胞周期停滞降低了多种与骨髓抑制相关的常用细胞毒性化疗药物的体外毒性[1]

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

体内研究
(In Vivo)

Trilaciclib (G1T28) 处理可在 12 小时内对 HSPC 的增殖产生强烈的剂量依赖性抑制,EdU 掺入在给药后 24 小时内以剂量依赖性方式恢复到接近基线水平。这些数据表明,单次口服剂量的 Trilaciclib 可以体内以剂量依赖性方式在 HSPC 中产生可逆的细胞周期停滞。在依托泊苷处理前 30 分钟给予 100 mg/kg Trilaciclib 的小鼠仅表现出背景水平的 caspase-3/7 活性。这些数据表明 Trilaciclib 可以在体内保护骨髓免受化疗诱导的细胞凋亡。数据表明,在 5-FU 之前使用 Trilaciclib 处理可能会减少 HSPC 中化疗引起的 5-FU 损伤,从而加速化疗后血细胞计数的恢复[1]

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

Clinical Trial
分子量

446.55

Formula

C24H30N8O

CAS 号
性状

固体

颜色

White to yellow

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 中的溶解度 : 6.82 mg/mL (15.27 mM; ultrasonic and adjust pH to 6 with HCl; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2394 mL 11.1970 mL 22.3939 mL
5 mM 0.4479 mL 2.2394 mL 4.4788 mL
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.20%

参考文献
Kinase Assay
[1]

HS68, WM2664, and A2058 cells are treated with 300 nM Trilaciclib (G1T28) or DMSO (0.1%), for 4, 8, 16, or 24 hours. Whole cell extracts are prepared using 1× radioimmunoprecipitation assay buffer containing 1× HALT protease and phosphatase inhibitors. Total protein concentration is determined by using the kit, according to the manufacturer's instructions. For Western blot analysis, protein is processed as described previously. Antibodies to total RB andβ-tubulin run as a loading control are assessed[1].

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

Cell Assay
[1]

HS68 cells are treated for 24 hours with Trilaciclib (G1T28) at 10, 30, 100, 300, 1,000, or 3,000 nM final concentration. Cells are harvested and fixed in ice-cold methanol. Fixed cells are stained with 20 μg propidium iodide, 50 μg RNAse A in PBS-CMF (calcium magnesium free)+1% BSA, Fraction V. Samples are processed on Cyan ADP Analyzer, and cell-cycle analysis is completed using software[1].

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

Animal Administration
[1]

Mice[1]
Female athymic nude mice are implanted with H69 cells and monitored until treatment initiation. Once tumors reach an acceptable size (150 mm3), mice are dosed in various combinations of Trilaciclib (100 mg/kg) and topotecan for 5 days per week for 4 weeks. Tumors are measured for up to 60 days after treatment. All mice that reach excessive tumor burden before 60 days are humanely euthanized. Topotecan and Trilaciclib levels in blood plasma from the mice treated with Trilaciclib hydrochloride and/or topotecan are processed and analyzed using established methods
.

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

参考文献

Trilaciclib 相关分类

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2394 mL 11.1970 mL 22.3939 mL 55.9848 mL
5 mM 0.4479 mL 2.2394 mL 4.4788 mL 11.1970 mL
10 mM 0.2239 mL 1.1197 mL 2.2394 mL 5.5985 mL
15 mM 0.1493 mL 0.7465 mL 1.4929 mL 3.7323 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Trilaciclib
目录号:
HY-101467
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