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

Dalpiciclib hydrochloride  (Synonyms: SHR-6390 hydrochloride)

目录号: HY-114338A 纯度: 98.22%
COA 产品使用指南

Dalpiciclib (SHR-6390) hydrochloride 是一种具有口服活性和高选择性的 CDK4/6 抑制剂,IC50 值分别为 12.4 nM 和 9.9 nM。Dalpiciclib hydrochloride 对乳腺癌和食道鳞状细胞癌显示出抗肿瘤活性。

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Dalpiciclib hydrochloride Chemical Structure

Dalpiciclib hydrochloride Chemical Structure

CAS No. : 2891598-76-6

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5 mg ¥4600
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Customer Review

Other Forms of Dalpiciclib hydrochloride:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Dalpiciclib (SHR-6390) hydrochloride is an orally active and highly selective inhibitor of CDK4 and 6 with IC50 values of 12.4 nM and 9.9 nM, respectively[1][2]. Dalpiciclib hydrochloride shows antitumor activity against breast cancer and esophageal squamous cell carcinoma[1][2][3][4].

IC50 & Target

CDK6

9.9 nM (IC50)

CDK4

12.4 nM (IC50)

体外研究
(In Vitro)

Dalpiciclib hydrochloride (0-4 μM, 72 h) inhibits cell proliferation in a dose-dependent manner[3].
Dalpiciclib hydrochloride (0-10 μM, 6 d) inhibits the proliferation of retinoblastoma-positive tumor cell lines[4].

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

Cell Proliferation Assay[3]

Cell Line: Eca 109, Eca 9706 and KYSE-510 ESCC cell lines
Concentration: 0-4 μM
Incubation Time: 72  hours
Result: Inhibited cell proliferation in a dose-dependent manner, with Eca 109 being the relative sensitive one and Eca 9706 being the relative resistant one.

Cell Viability Assay[4]

Cell Line: MCF7, MCF7/TR, BT-474/T cell lines
Concentration: 0-10 μM
Incubation Time: 6  days
Result: Inhibited MCF7/TR cells, parental MCF7 cells and BT-474/T resistant cells with the IC50 values of 229.5, 115.4 and 210.7 nM, respectively.
体内研究
(In Vivo)

Dalpiciclib hydrochloride (oral gavage; 150 mg/kg; once weekly; 3 weeks) shows antitumor activity against ESCC xenografts[3].
Dalpiciclib hydrochloride combined with Paclitaxel (PTX) or Cisplatin (CDDP) offer synergistic inhibitory effects in ESCC xenografts[3].
Dalpiciclib hydrochloride (oral gavage; 37.5 mg/kg, 75 mg/kg, 150 mg/kg; once daily; 30 days) shows antitumor activity in human xenograft models [4].

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

Animal Model: NOD/SCID mice (ESCC PDXs models)[3]
Dosage: 150 mg/kg
Administration: Oral gavage; 150 mg/kg; once weekly; 3 weeks
Result: Suppressed the growth of tumor.
Animal Model: 5-week-old female Balb/cA-nude mice subcutaneously inoculated MCF7/ARO, COLO 205 and U87MG[4]
Dosage: 37.5 mg/kg, 75 mg/kg, 150 mg/kg
Administration: Oral gavage; 37.5 mg/kg, 75 mg/kg, 150 mg/kg; once daily; 30 days
Result: Caused regression of all tumor xenografts at the highest dose tested.
Clinical Trial
分子量

483.01

Formula

C25H31ClN6O2

CAS 号
性状

固体

颜色

White to off-white

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
细胞实验: 

DMSO 中的溶解度 : 5 mg/mL (10.35 mM; 超声助溶 (<60°C); 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 2.0704 mL 10.3518 mL 20.7035 mL
5 mM 0.4141 mL 2.0704 mL 4.1407 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。

  • 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
参考文献

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 1 mM 2.0704 mL 10.3518 mL 20.7035 mL 51.7588 mL
5 mM 0.4141 mL 2.0704 mL 4.1407 mL 10.3518 mL
10 mM 0.2070 mL 1.0352 mL 2.0704 mL 5.1759 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:
Dalpiciclib hydrochloride
目录号:
HY-114338A
需求量: