Riviciclib hydrochloride P276-00|cas:920113-03-7|西域试剂

Riviciclib hydrochloride P276-00,99.01%

产品编号：Bellancom-16559| CAS NO：920113-03-7| 分子式：C₂₁H₂₁Cl₂NO₅| 分子量：438.30

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-16559	￥1200.00	杭州北京（现货）
Bellancom-16559	￥1800.00	杭州北京（现货）
Bellancom-16559	￥3000.00	杭州北京（现货）
Bellancom-16559	￥5500.00	杭州北京（现货）
Bellancom-16559	￥8600.00	杭州北京（现货）

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Riviciclib hydrochloride P276-00

产品介绍

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。

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. Riviciclib hydrochloride (P276-00) shows antitumor activity on cisplatin-resistant cells.

体外研究

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.
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.
Riviciclib hydrochloride shows activity in human cancer cell lines, such as colon carcinoma, osteosarcomal, cervical carcinoma, and bladder carcinoma cells.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis

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

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.
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.

西域 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)
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)
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.

体内研究

西域 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)
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)
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.

体内研究

西域 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)
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)
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.

性状

Solid

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。