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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 Chemical Structure
规格 |
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是否有货 |
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100 mg |
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询价 |
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250 mg |
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询价 |
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500 mg |
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询价 |
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* 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].
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IC50 & Target |
CDK4
12.4 nM (IC50)
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CDK6
9.9 nM (IC50)
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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. |
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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. |
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分子量 |
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Formula |
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运输条件 |
Room temperature in continental US; may vary elsewhere.
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储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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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 |
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参考文献 |
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[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.
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