Riviciclib hydrochloride(Synonyms: P276-00)

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

Riviciclib hydrochloride (P276-00) 是有效的 CDK 抑制剂，抑制 CDK9-cyclinT1，CDK4-cyclin D1，CDK1-cyclinB 的 IC50 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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Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥1736 In-stock
2 mg ￥1200 In-stock
5 mg ￥1800 In-stock
10 mg ￥3000 In-stock
25 mg ￥5500 In-stock
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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