Delanzomib(Synonyms: CEP-18770)

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Delanzomib (Synonyms: CEP-18770) 纯度: ≥98.0%

Delanzomib (CEP-18770) 是一种强效的具有口服活性的蛋白酶体的胰凝乳蛋白酶样活性 (chymotrypsin-like activity of the proteasome) 抑制剂，IC50 为 3.8 nM。Delanzomib 抑制 NF-κB 活性，诱导癌细胞凋亡 (apoptotic)，并具有很强的抗血管生成和抗癌活性。

Delanzomib(Synonyms: CEP-18770)

Delanzomib Chemical Structure

CAS No. : 847499-27-8

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1278 In-stock
5 mg ￥1162 In-stock
50 mg ￥7348 In-stock
100 mg ￥8928 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Delanzomib 相关产品

•相关化合物库:

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生物活性

Delanzomib (CEP-18770) is a potent and orally active chymotrypsin-like activity of the proteasome inhibitor with an IC50 of 3.8 nM. Delanzomib inhibits NF-κB activity, induces cancer cell apoptotic, and has strong antiangiogenic and anti-cancer activities[1].

IC50 & Target

IC50: 3.8 nM (Chymotrypsin-like activity of the proteasome)[1]
体外研究
(In Vitro)

Delanzomib (CEP-18770; 20 nM; 12-24 hours) treatment results in a progressive appearance of cleaved caspases-3, -7, and -9 between 12 and 24 hours’exposure in the human MM cell lines, RPMI-8226, and U266[1].
Delanzomib (CEP-18770; 5-40 nM; 4-24 hours) treatment induces an accumulation of ubiquitinated proteins over 4 to 8 hours[1].
Delanzomib (CEP-18770) inhibits endothelial cell survival, vasculogenesis, and osteoclastogenesis in vitro; and displays a favorable cytotoxicity profile toward normal cells[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.

Apoptosis Analysis[1]

Cell Line: RPMI-8226, U266, and K562 cells
Concentration: 20 nM
Incubation Time: 12 hours, 24 hours
Result: Resulted in a progressive appearance of cleaved caspases-3, -7, and -9 between 12 and 24 hours’exposure in the human MM cell lines.

Western Blot Analysis[1]

Cell Line: RPMI-8226, U266, and K562 cells
Concentration: 5 nM, 10 nM, 20 nM, 40 nM
Incubation Time: 4 hours, 8 hours, 12 hours, 24 hours
Result: Induced an accumulation of ubiquitinated proteins over 4 to 8 hours.

体内研究
(In Vivo)

Delanzomib (CEP-18770; 7.8-13 mg/kg; oral administration; twice a week; for 4 weeks) treatment results in a more sustained pharmacodynamic inhibition of proteasome activity in tumors relative to normal tissues, complete tumor regression of multiple myeloma (MM) xenografts and improves overall median survival in a systemic model of human MM[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 Model: SCID mice injected with RPMI 8226 cells[1]
Dosage: 7.8 mg/kg, 10 mg/kg, 13 mg/kg
Administration: Oral administration; twice a week; for 4 weeks
Result: Resulted in a more sustained pharmacodynamic inhibition of proteasome activity in tumors relative to normal tissues.

Clinical Trial

分子量

413.28

Formula

C21H28BN3O5
CAS 号

847499-27-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (241.97 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4197 mL 12.0983 mL 24.1967 mL
5 mM 0.4839 mL 2.4197 mL 4.8393 mL
10 mM 0.2420 mL 1.2098 mL 2.4197 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。-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: ≥ 2.17 mg/mL (5.25 mM); Clear solution

    此方案可获得 ≥ 2.17 mg/mL (5.25 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 21.7 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: 2.17 mg/mL (5.25 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.17 mg/mL (5.25 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 21.7 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: ≥ 2.17 mg/mL (5.25 mM); Clear solution

    此方案可获得 ≥ 2.17 mg/mL (5.25 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 21.7 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]. Piva R, et al. CEP-18770: A novel, orally active proteasome inhibitor with a tumor-selective pharmacologic profile competitive with bortezomib. Blood. 2008 Mar 1;111(5):2765-75.

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