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

Trilaciclib hydrochloride  (Synonyms: G1T28 hydrochloride)

目录号: HY-101467A 纯度: 99.74%
COA 产品使用指南

Trilaciclib (G1T28) hydrochloride 是一种口服有效的 CDK4/6 的抑制剂,对于 CDK4CDK6IC50 值分别为 1 nM 和 4 nM。Trilaciclib hydrochloride 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 hydrochloride 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 hydrochloride Chemical Structure

Trilaciclib hydrochloride Chemical Structure

CAS No. : 1977495-97-8

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1 mg ¥390
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Customer Review

Other Forms of Trilaciclib hydrochloride:

MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

IC50 & Target[1]

Cdk4/cyclin D1

1 nM (IC50)

cdk6/cyclin D3

4 nM (IC50)

体外研究
(In Vitro)

Trilaciclib hydrochloride (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 hydrochloride (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 hydrochloride (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.

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: 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).

Cell Cycle Analysis[1]

Cell Line: HS68, WM2664 cells
Concentration: 10, 30, 100, 300, 1000 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.

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
体内研究
(In Vivo)

Trilaciclib hydrochloride (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 hydrochloride 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

519.47

Formula

C24H32Cl2N8O

CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

H2O 中的溶解度 : 25.64 mg/mL (49.36 mM; 超声助溶; 酸性条件溶解 (HCL 调节,pH≈2))

DMSO 中的溶解度 : 1.1 mg/mL (2.12 mM; 超声助溶; 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 1.9250 mL 9.6252 mL 19.2504 mL
5 mM 0.3850 mL 1.9250 mL 3.8501 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 (sealed storage, away from moisture)。-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。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 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
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体积
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分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

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体积 (start)

V1

=
浓度 (final)

C2

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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
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: 99.74%

参考文献

Trilaciclib hydrochloride 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 (sealed storage, away from moisture)。-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 / H2O 1 mM 1.9250 mL 9.6252 mL 19.2504 mL 48.1260 mL
H2O 5 mM 0.3850 mL 1.9250 mL 3.8501 mL 9.6252 mL
10 mM 0.1925 mL 0.9625 mL 1.9250 mL 4.8126 mL
15 mM 0.1283 mL 0.6417 mL 1.2834 mL 3.2084 mL
20 mM 0.0963 mL 0.4813 mL 0.9625 mL 2.4063 mL
25 mM 0.0770 mL 0.3850 mL 0.7700 mL 1.9250 mL
30 mM 0.0642 mL 0.3208 mL 0.6417 mL 1.6042 mL
40 mM 0.0481 mL 0.2406 mL 0.4813 mL 1.2031 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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 hydrochloride
目录号:
HY-101467A
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