ONC212|cas:1807861-48-8|西域试剂

ONC212,99.32%

产品编号：Bellancom-111343| CAS NO：1807861-48-8| 分子式：C₂₄H₂₃F₃N₄O| 分子量：440.46

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-111343	￥1100.00	杭州北京（现货）
Bellancom-111343	￥1800.00	杭州北京（现货）
Bellancom-111343	￥3060.00	杭州北京（现货）
Bellancom-111343	￥4900.00	杭州北京（现货）
Bellancom-111343	￥7400.00	杭州北京（现货）

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ONC212

产品介绍

ONC212 是一种氟化的 ONC201 类似物，是一种有前景的抗癌剂，也是 GPR132 的选择性激动剂。ONC212 还诱导凋亡 (apoptosis)。

生物活性

ONC212, a fluorinated-ONC201 analogue, is a promising anti-cancer agent and also a selective agonist of GPR132. ONC212 also induces apoptosis.

体外研究

Cell proliferation assay reveals that at least a ten-fold lower concentration of ONC212 is needed to achieve 50% growth inhibition in comparison to ONC201. ONC212 shows GI₅₀ values in the range of 0.1 to 0.4 μM, while the corresponding ONC201 GI₅₀ values are in the range of 4 to 9 μM for the seven pancreatic cancer cell lines tested. Long-term cell proliferation assay shows that both ONC201 and ONC212 are comparable in inhibiting colony formation at a 20 µM dose. However, at a 5 µM dose, ONC212 is about 50-times more potent than ONC201 in preventing colony formation in four out of the seven pancreatic cancer cell lines tested. Induction of apoptosis by ONC212 is an earlier event than ONC201. Treatment with ONC201 and ONC212 reduces the expression of anti-apoptotic markers such as XIAP and MCL-1. Western blot analysis shows that in the HPAF-II cell line, ATF4 and phosphorylated EIF2α are upregulated as early as 6 to 12 hours post ONC201 or ONC212 treatment.

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

体内研究

Biweekly oral administration of 50 mg/kg ONC212 markedly inhibits Acute myeloid leukemia (AML) expansion and prolongs overall survival (p=0.0003). Median survival increases from 43 d in controls to 49 d in the ONC212-treated group (+14%). ONC212 treatment exhibits significantly greater growth inhibition in comparison to ONC201. A dose of 50 mg/kg of ONC212 administered three-times a week is sufficient to lead to significant growth inhibition of tumors compare to the control group for these two models. Results demonstrate that ONC212 treated tumors show reduced proliferation in the HPAF-II model. In vivo toxicity assessment experiments show that ONC212 is well tolerated up to 250 mg/kg. 300 mg/kg of ONC212 causes splenic damage and elevates liver enzymes. ONC212 has a slightly shorter half-life than ONC201, with a clearance from the blood at 12 hours, T_1/2 of 4.3 hours, and C_max of 1.4 µg/mL.

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (113.52 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2704 mL	11.3518 mL	22.7035 mL
5 mM	0.4541 mL	2.2704 mL	4.5407 mL
10 mM	0.2270 mL	1.1352 mL	2.2704 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: ≥ 2.5 mg/mL (5.68 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.68 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (5.68 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.68 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (5.68 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.68 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。