Dalpiciclib hydrochloride

(Synonyms: SHR-6390 hydrochloride)
目录号: PL02203 纯度: ≥99%
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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中文名称
Dalpiciclib hydrochloride
英文名称
Dalpiciclib hydrochloride
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
详情描述
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。
产品详情
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。
生物活性
Dalpiciclib (SHR-6390) hydrochloride is an orally active and highly selective inhibitor of CDK4 and 6 with IC 50 values of 12.4?nM and 9.9?nM, respectively. Dalpiciclib hydrochloride shows antitumor activity against breast cancer and esophageal squamous cell carcinoma.
性状
Solid
IC50 & Target[1][2]
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.
Dalpiciclib hydrochloride (0-10 μM, 6 d) inhibits the proliferation of retinoblastoma-positive tumor cell lines. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Proliferation Assay-tbl">
体内研究(In Vivo)
Dalpiciclib hydrochloride (oral gavage; 150 mg/kg; once weekly; 3 weeks) shows antitumor activity against ESCC xenografts.
Dalpiciclib hydrochloride combined with Paclitaxel (PTX) or Cisplatin (CDDP) offer synergistic inhibitory effects in ESCC xenografts.
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 . has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
ClinicalTrial
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.
溶解度数据
In Vitro: DMSO : 5 mg/mL (10.35 mM; ultrasonic and warming and heat to 60°C)配制储备液
搜索质检报告(COA)
[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.

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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The dilution calculator equation
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