Riviciclib hydrochloride(Synonyms: P276-00)

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。

Riviciclib hydrochloride (Synonyms: P276-00) 纯度: 98.33%

Riviciclib hydrochloride (P276-00) 是有效的 CDK 抑制剂,抑制 CDK9-cyclinT1CDK4-cyclin D1CDK1-cyclinBIC50 值分别为 20 nM,63 nM,79 nM。Riviciclib hydrochloride (P276-00) 对 Cisplatin 耐药性细胞具有抗肿瘤活性。

Riviciclib hydrochloride(Synonyms: P276-00)

Riviciclib hydrochloride Chemical Structure

CAS No. : 920113-03-7

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10 mM * 1 mL in DMSO ¥1736 In-stock
2 mg ¥1200 In-stock
5 mg ¥1800 In-stock
10 mg ¥3000 In-stock
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50 mg ¥8600 In-stock
100 mg ¥15000 In-stock
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生物活性

Riviciclib hydrochloride (P276-00) is a potent cyclin-dependent kinase (CDK) inhibitor, which inhibits CDK9-cyclinT1, CDK4-cyclin D1, and CDK1-cyclinB with IC50s of 20 nM, 63 nM, and 79 nM, respectively[1][2]. Riviciclib hydrochloride (P276-00) shows antitumor activity on cisplatin-resistant cells[3].

IC50 & Target[1]

CDK9- Cyclin T1

0.020 μM (IC50)

cdk4-cyclin D1

0.063 μM (IC50)

CDK1-Cyclin B

0.079 μM (IC50)

cdk2-cyclin A

0.224 μM (IC50)

cdk2-cyclin E

2.500 μM (IC50)

cdk6-cyclin D3

0.396 μM (IC50)

CDK9-cyclin H

2.900 μM (IC50)

体外研究
(In Vitro)

Riviciclib hydrochloride (1.5-5 μM; 72 hours) shows no detectable cells in G1 and G2 in promyelocytic leukemia cells and arrest of cells in G1 in synchronized human non-small cell lung carcinoma (H-460) and human normal lung fibroblast (WI-38) cells[3].
Riviciclib hydrochloride (3-24 hours; 1.5 μM) reduces cyclin D1, Cdk4, and Rb levels in H-460 cells. Rb (retinoblastoma) phosphorylation at Ser780 decrease at 3 h[2].
Riviciclib hydrochloride shows activity in human cancer cell lines, such as colon carcinoma, osteosarcomal, cervical carcinoma, and bladder carcinoma cells[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[3]

Cell Line: Promyelocytic leukemia cells (HL-60 cells), non-small cell carcinoma (H-460) cells, human normal lung fibroblast (WI-38) cells
Concentration: 1.5, 5 μM
Incubation Time: 72 hours
Result: Showed apoptosis at the end of 24 h and no detectable cells were present in G1 and G2 in HL-60 cells. Caused an exclusive G1 arrest of synchronous population of cancerous cells H-460 cells and normal cells WI-38.

Western Blot Analysis[2]

Cell Line: H-460 cells; MCF-7 cells
Concentration: 1.5 μM
Incubation Time: 3, 6, 9, 12, 24 hours
Result: Reduced cyclin D1, Cdk4, and Rb levels in H-460 cells. Rb (retinoblastoma) phosphorylation at Ser780 decrease at 3 h. Decreased protein levels of cyclin D1 and Cdk4 levels staring at 6 and 9 h in MCF-7 cells, respectively, and accompanied by a decrease in phosphorylation of Rb at Ser780 from 6 h onward, followed by reduced Rb levels at 24 h.

体内研究
(In Vivo)

Riviciclib hydrochloride (administered i.p.; 35 kg/mg daily for 10 days, in human xenograft mode with severe combined immunodeficient mice) shows significant inhibition in the growth of human colon carcinoma HCT-116 xenograft[3].
Riviciclib hydrochloride (administered via i.p.; 50 mg/kg once daily; 30 mg/kg twice daily for 18 treatments, in human xenograft mode with severe combined immunodeficient mice) significantly inhibited growth[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Human xenograft mode with HCT-116 tumor model (severe combined immunodeficient mice)[3]
Dosage: 35 mg/kg
Administration: Administered i.p.; daily for 10 days
Result: Given 35 mg/kg showed significant inhibition in the growth.
Animal Model: Human xenograft model with H-460 tumor xenograft (severe combined immunodeficient mice)[3]
Dosage: 50 mg/kg; 30 mg/kg
Administration: Administered i.p.; 50 mg/kg once daily for 20 days; Administered i.p.; 30 mg/kg twice daily for 18 treatments
Result: Given 50 mg/kg and 30 mg/kg twice daily significantly inhibited growth.

Clinical Trial

分子量

438.30

Formula

C21H21Cl2NO5

CAS 号

920113-03-7

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: 

DMSO : 50 mg/mL (114.08 mM; Need ultrasonic)

H2O : 25 mg/mL (57.04 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2815 mL 11.4077 mL 22.8154 mL
5 mM 0.4563 mL 2.2815 mL 4.5631 mL
10 mM 0.2282 mL 1.1408 mL 2.2815 mL

*

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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.75 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.75 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.75 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.75 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.75 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.75 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Roskoski R Jr,Cyclin-dependent protein kinase inhibitors including palbociclib as anticancer drugs.Pharmacol Res. 2016 May;107:249-275.

    [2]. Joshi KS, et al. In vitro antitumor properties of a novel cyclin-dependent kinase inhibitor, P276-00. Mol Cancer Ther. 2007 Mar;6(3):918-25.

    [3]. Joshi KS,et al. P276-00, a novel cyclin-dependent inhibitor induces G1-G2 arrest, shows antitumor activity on cisplatin-resistant cells and significant in vivo efficacy in tumor models. Mol Cancer Ther. 2007 Mar;6(3):926-34.

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