标签归档：belotecan

Belotecan-d7 hydrochloride(Synonyms: 盐酸贝洛替康 d7 (盐酸盐))

发表于由

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。

Belotecan-d7 hydrochloride (Synonyms: 盐酸贝洛替康 d7 (盐酸盐))

Belotecan-d7 hydrochloride 是 Belotecan hydrochloride 的氘代物。Belotecan hydrochloride (CKD-602 hydrochloride) 是拓扑异构酶 I (Topoisomerase I) 抑制剂，是一种合成的喜树碱衍生物。

Belotecan-d7 hydrochloride(Synonyms: 盐酸贝洛替康 d7 (盐酸盐))

Belotecan-d7 hydrochloride Chemical Structure

CAS No. : 1346598-22-8

规格 是否有货
1 mg Check price and availability
10 mg Check price and availability

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生物活性

Belotecan-d7 hydrochloride is the deuterium labeled Belotecan hydrochloride. Belotecan hydrochloride (CKD-602 hydrochloride), a Topoisomerase I inhibitor, is a synthetic camptothecin derivative[1][2].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

477.00

Formula

C25H21D7ClN3O4
CAS 号

1346598-22-8
中文名称

盐酸贝洛替康 d7 (盐酸盐)
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Kim YK, et al. Anticancer effects of CKD-602 (Camtobell?) via G2/M phase arrest in oral squamous cell carcinoma cell lines. Oncol Lett. 2015 Jan;9(1):136-142.

    [3]. Kim YY, et al. CKD-602, a camptothecin derivative, inhibits proliferation and induces apoptosis in glioma cell lines. Oncol Rep. 2009 Jun;21(6):1413-9.

    [4]. Kim CY, et al. Antitumor activity of CKD-602, a camptothecin derivative, in a mouse glioma model. J Clin Neurosci. 2012 Feb;19(2):301-5.

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Belotecan hydrochloride(Synonyms: CKD-602)

发表于由

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。

Belotecan hydrochloride (Synonyms: CKD-602) 纯度: 98.82%

Belotecan hydrochloride (CKD-602 hydrochloride) 是拓扑异构酶 I (Topoisomerase I) 抑制剂，是一种合成的喜树碱衍生物。

Belotecan hydrochloride(Synonyms: CKD-602)

Belotecan hydrochloride Chemical Structure

CAS No. : 213819-48-8

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1320 In-stock
5 mg ￥1200 In-stock
10 mg ￥1800 In-stock
25 mg ￥3800 In-stock
50 mg ￥6800 In-stock
100 mg ￥12000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Belotecan hydrochloride 相关产品

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生物活性

Belotecan hydrochloride (CKD-602 hydrochloride), a Topoisomerase I inhibitor, is a synthetic camptothecin derivative.

IC50 & Target[1]

Top1

 

体外研究
(In Vitro)

Belotecan exerts a significant cytotoxic effect on YD-8, YD-9 and YD-38 cells in a time- and dose-dependent manner with IC50 values of 2.4, 0.18 and 0.05 μg/mL at 72 h following treatment. Belotecan induces apoptosis in these cell lines. Belotecan induces G2/M phase arrest in oral squamous cell cancer cells[1]. Belotecan shows a significant anticancer effect on glioma cells, with IC50 values of 9.07 nM for LN229, 14.57 nM for U251 MG, 29.13 nM for U343 MG, and 84.66 nM for U87 MG[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.
体内研究
(In Vivo)

Belotecan has a significant effect on intracerebral glioma growth, with animals having significantly smaller tumors than those in the control group[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.
Clinical Trial

分子量

469.96

Formula

C25H28ClN3O4
CAS 号

213819-48-8
中文名称

盐酸贝洛替康
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 (106.39 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1278 mL 10.6392 mL 21.2784 mL
5 mM 0.4256 mL 2.1278 mL 4.2557 mL
10 mM 0.2128 mL 1.0639 mL 2.1278 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 (4.43 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.43 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 (4.43 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.43 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 (4.43 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.43 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]. Kim YK, et al. Anticancer effects of CKD-602 (Camtobell?) via G2/M phase arrest in oral squamous cell carcinoma cell lines. Oncol Lett. 2015 Jan;9(1):136-142.

    [2]. Kim YY, et al. CKD-602, a camptothecin derivative, inhibits proliferation and induces apoptosis in glioma cell lines. Oncol Rep. 2009 Jun;21(6):1413-9.

    [3]. Kim CY, et al. Antitumor activity of CKD-602, a camptothecin derivative, in a mouse glioma model. J Clin Neurosci. 2012 Feb;19(2):301-5.
Cell Assay
[1]

The cells are treated with different concentrations (0.01, 0.1, 0.5, 1, 5 and 10 μg/mL) of belotecan for 24, 48 and 72 h. Control samples of each cell line are treated with medium only. Cell viability is measured using the MTS assay[1].

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 Administration
[1]

Mice: Nude mice with established U87MG glioma are treated with a dose of belotecan of 0 mg/kg (control group, injection with saline), 40 mg/kg (group A) or 60 mg/kg (group B). Thereafter, the dose is repeated once every 4 days for a total of four doses. Tumor volume is measured histologically and apoptosis is detected[1].

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.
参考文献

  • [1]. Kim YK, et al. Anticancer effects of CKD-602 (Camtobell?) via G2/M phase arrest in oral squamous cell carcinoma cell lines. Oncol Lett. 2015 Jan;9(1):136-142.

    [2]. Kim YY, et al. CKD-602, a camptothecin derivative, inhibits proliferation and induces apoptosis in glioma cell lines. Oncol Rep. 2009 Jun;21(6):1413-9.

    [3]. Kim CY, et al. Antitumor activity of CKD-602, a camptothecin derivative, in a mouse glioma model. J Clin Neurosci. 2012 Feb;19(2):301-5.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务