标签归档：dalpiciclib

Dalpiciclib hydrochloride(Synonyms: SHR-6390 hydrochloride)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Dalpiciclib hydrochloride (Synonyms: SHR-6390 hydrochloride)

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。

Dalpiciclib hydrochloride(Synonyms: SHR-6390 hydrochloride)

Dalpiciclib hydrochloride Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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

CDK4

12.4 nM (IC50)

CDK6

9.9 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].

Shanghai Jinpan Biotech Co Ltd 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].

Shanghai Jinpan Biotech Co Ltd 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.

分子量

483.01

Formula

C25H31ClN6O2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
溶解性数据
In Vitro: 

DMSO : 5 mg/mL (10.35 mM; ultrasonic and warming and heat to 60°C)

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
10 mM 0.2070 mL 1.0352 mL 2.0704 mL

参考文献

  • [1]. Jose Manuel Perez-Garcia, et al. Perez-Garcia JM, Cortes J, Llombart-Cussac A. CDK4/6 inhibitors in breast cancer: spotting the difference. Nat Med. 2021 Nov;27(11):1868-1869.

    [2]. Pin Zhang, et al. A phase 1 study of dalpiciclib, a cyclin-dependent kinase 4/6 inhibitor in Chinese patients with advanced breast cancer. Biomark Res. 2021 Apr 12;9(1):24.

    [3]. Jiayuan Wang, et al. CDK4/6 inhibitor-SHR6390 exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated Rb and inducing G1 cell cycle arrest. J Transl Med. 2017 Jun 2;15(1):127.

    [4]. Fei Long, et al. Preclinical characterization of SHR6390, a novel CDK 4/6 inhibitor, in vitro and in human tumor xenograft models. Cancer Sci. 2019 Apr;110(4):1420-1430.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Dalpiciclib(Synonyms: SHR-6390)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Dalpiciclib (Synonyms: SHR-6390)

Dalpiciclib (SHR-6390) 是一种高选择性、口服生物利用度的 CDK4/6 抑制剂，对 CDK4 (IC50=12.4 nM) 和CDK6 (IC50=9.9 nM) 的数值相当。SHR6390通过抑制磷酸化 Rb 蛋白和诱导 G1 细胞周期阻滞在食管鳞状细胞癌中发挥有效的抗肿瘤活性。

Dalpiciclib(Synonyms: SHR-6390)

Dalpiciclib Chemical Structure

CAS No. : 1637781-04-4

规格 价格 是否有货
5 mg ￥5500 询问价格 & 货期
10 mg ￥8500 询问价格 & 货期
25 mg ￥16500 询问价格 & 货期

* Please select Quantity before adding items.

生物活性

Dalpiciclib (SHR-6390) is a highly selective, orally bioavailable CDK4/6 inhibitor with comparable potencies against CDK4 (IC50=12.4 nM) and CDK6 (IC50=9.9 nM). Dalpiciclib exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated tumor-suppressor retinoblastoma protein (Rb) and inducing G1 cell cycle arrest[1][2].

IC50 & Target[1]

CDK4

12.4 nM (IC50)

CDK6

9.9 nM (IC50)

体外研究
(In Vitro)

Dalpiciclib (SHR-6390) (0-4 μM) inhibits cell proliferation in a dose-dependent manner[2].
Dalpiciclib (24 hours) significantly blocks phosphorylation of Rb at serine 780 in relative sensitive Eca 109 and KYSE-510 cell lines, but not in relative resistant Eca 9706 cell line. Dalpiciclib induces cell cycle arrest at G1 phase in Eca 109 and KYSE-510 cell lines[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[2]

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.

体内研究
(In Vivo)

Dalpiciclib (SHR-6390) (150 mg/kg; oral gavage; weekly for 3 weeks) shows antitumor activity against ESCC xenografts[2].
Dalpiciclib combines with Paclitaxel (PTX) or Cisplatin (CDDP) offered synergistic inhibitory effects in ESCC xenografts[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NOD/SCID mice (ESCC PDXs models) [2]
Dosage: 150 mg/kg
Administration: Oral gavage; weekly for 3 weeks
Result: The growth of tumor was significantly suppressed in SHR6390 treatment group with various suppressions.

分子量

446.54

Formula

C25H30N6O2
CAS 号

1637781-04-4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Zhang P, et al. A phase 1 study of dalpiciclib, a cyclin-dependent kinase 4/6 inhibitor in Chinese patients with advanced breast cancer. Biomark Res. 2021;9(1):24. Published 2021 Apr 12.

    [2]. Wang J, et al. CDK4/6 inhibitor-SHR6390 exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated Rb and inducing G1 cell cycle arrest. J Transl Med. 2017;15(1):127. Published 2017 Jun 2.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务