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

Trilaciclib  (Synonyms: G1T28)

目录号: HY-101467 纯度: 98.66%
COA 产品使用指南

摩尔计算器

Trilaciclib (G1T28) 是一种口服有效的 CDK4/6 的抑制剂，对于 CDK4 和 CDK6 的 IC50 值分别为 1 nM 和 4 nM。Trilaciclib 能够有效抑制肿瘤细胞增殖，并减轻化疗产生的血液毒性。Trilaciclib 可减轻 5FU (HY-90006) 化疗引起的细胞凋亡和骨髓抑制。

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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
In-stock
5 mg ￥1150
In-stock
10 mg ￥1650
In-stock
50 mg ￥4000
In-stock
100 mg ￥5800
In-stock
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500 mg   询价  

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Customer Review

Other Forms of Trilaciclib:

Trilaciclib 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

查看 CDK 亚型特异性产品:

查看所有亚型
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Trilaciclib (G1T28) is an orally active CDK4/6 inhibitor with IC50 values of 1 nM and 4 nM for CDK4 and CDK6, respectively. . Trilaciclib can effectively inhibit tumor cell proliferation and reduce the hematological toxicity caused by chemotherapy. Trilaciclib attenuates apoptosis and myelosuppression induced by 5FU (HY-90006) chemotherapy[1].

IC50 & Target

IC50: 1 nM (CDK4), 4 nM (CDK6)[1]
体外研究
(In Vitro)

Trilaciclib (10-1000 nM; 24 h) 可逆地调节小鼠和犬骨髓造血干细胞和祖细胞的增殖[1]。
Trilaciclib (10-1000 nM; 24 h) 可将 CDK4/6 依赖性细胞的细胞周期阻滞在 G1 期，对HS68的EC50为 30 nM[1]。
Trilaciclib (300 nM；16 或 48 h) 可保护 CDK4/6 依赖性细胞（HS68、WM2664）免受化疗引起的损伤，并减弱化疗引起的细胞凋亡[1]。

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

Trilaciclib 相关抗体:

Cell Proliferation Assay[1]

Cell Line: HS68, WM2664 cells
Concentration: 300 nM
Incubation Time: 8h for measure γH2AX foci (DNA damage); 48 hours to measure caspase 3/7 activity (apoptosis).
Result: Produced a strong dose-dependent inhibition of HSPC proliferation within 12 hours.
Elicited a robust dose-dependent decrease in caspase 3/7 activation suggesting an attenuation of apoptosis.
Resulted a dose-dependent decrease in γH2AX foci in all DNA damaging chemotherapies tested (carboplatin, doxorubicin, etoposide, camptothecin).

Western Blot Analysis[1]

Cell Line: HS68, WM2664 cells
Concentration: 10, 30, 100, 300, 1000 nM
Incubation Time: 16 h
Result: Blocked RB phosphorylation in the RB dependent cell lines by 16 hours post exposure, while the CDK4/6-independent cell line (A2058) exhibits no RB or pRB expression. Suggesting an attenuation of chemotherapy-induced DNA damag

Cell Cycle Analysis[1]

Cell Line: HS68, WM2664 cells
Concentration: 300 nM
Incubation Time: 24 h
Result: Inhibited only CDK4/6-dependent cells, with EC50 of 30 nM for HS68 cell.
Singnificantly decreased the S phase cell numbers, increased the G1 phase cell numbers.
体内研究
(In Vivo)

Trilaciclib (50-150 mg/kg；口服；单剂量) 可保护小鼠骨髓细胞免受化疗诱导的细胞凋亡，并以剂量依赖性减轻体内化疗诱导的骨髓抑制。Trilaciclib 在 150 mg/kg 剂量下，可以减少 5FU (HY-90006) (150 mg/kg; ip) 化疗引起的 HSPC 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.

Animal Model: FVB/n female C57Bl6 mice[1]
Dosage: 50, 100, 150 mg/kg
Administration: Po; single dose; treated followed 11 or 23 hours later by a single injection of EdU (HY-118411) (100 μg; ip); mouse were euthanized 1 hour after EdU injection.
Result: Showed a dose-dependent decrease in caspase 3/7 activation.
Attenuated chemotherapy-induced myelosuppression in mice.
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

只
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%

COA (265 KB) HNMR (300 KB) RP-HPLC (249 KB) MS (182 KB)

产品使用指南 (1538 KB)
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.

Keywords:

Trilaciclib1374743-00-6G1T28CDKCyclin dependent kinaseInhibitorinhibitorinhibit

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目录号：
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