ONC212 - CAS:1807861-48-8 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	ONC212
英文名称:	ONC212
别名:	2,4,6,7,8,9-Hexahydro-7-(phenylmethyl)-4-[[4-(trifluoromethyl)phenyl]methyl]imidazo[1,2-a]pyrido[3,4-e]pyrimidin-5(1H)-one
CAS No:	1807861-48-8	分子式:	C₂₄H₂₃F₃N₄O	分子量:	440.46
CAS No:	1807861-48-8
分子式:	C₂₄H₂₃F₃N₄O
分子量:	440.46

安全技术说明书(PDF) MSDS(PDF) 点击下载产品说明书(PDF)

O10207 ONC212 ≥98% (psaitong)

相关产品

包装规格：

5mg in glass bottle

溶解性：

溶于DMSO（50 mg/mL 超声）

产品描述：

基本信息

产品编号：O10207
产品名称：ONC212
CAS:	1807861-48-8	储存条件	粉末	-20℃	四年

分子式：	C24H23F3N4O		溶于液体	-80℃	六个月
分子量	440.46			-20℃	一个月
化学名：
Solubility (25°C)	体外	DMSO	88mg/mL (199.79mM)
		Ethanol	88mg/mL (199.79mM)
		Water	Insoluble
	体内（现配现用）
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
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。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	2.2704mL	11.3518mL	22.7035mL
5mM	0.4541mL	2.2704mL	4.5407mL
10mM	0.2270mL	1.1352mL	2.2704mL
50mM	0.0454mL	0.2270mL	0.4541mL

生物活性

产品描述	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。
靶点/IC₅₀	GPR132
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 0.4μM, while the corresponding ONC201 GI50 values are in the range of 4 to 9μM 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 20µM dose.However, at a 5µM 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.
体内研究	Biweekly oral administration of 50mg/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 50mg/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 250mg/kg. 300mg/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, T1/2 of 4.3 hours, and Cmax of 1.4µg/mL

推荐实验方法(仅供参考)

细胞实验:

All pancreatic cancer cell lines are treated with ONC201 or ONC212 at the indicated doses and time-points. Post-treatment,both floating and adherent cells are collected, fixed in 70% ethanol and stained with propidium iodide in the presence of ribonuclease A. Flow cytometric data is collected using a flow cytometer.The sub-G1 fraction (apoptotic) is quantified, and analysis is performed to quantify the distribution of cells in G1, S and G2-M phases of the cell cycle utilizing.

动物实验:

Six- to seven-week-old female athymic nu/nu mice are used in this study. A total of 3 to 5×106 luciferase-expressing cells are suspended in 50μL of PBS mixed with 50μL of Matrigel and subcutaneously injected into the rear flanks of the mice. When tumor volume reaches an average of 100 to 150 cm3, mice are randomly assigned to the indicated control or treatment groups.ONC201 and ONC212 are delivered in a solution of 10% DMSO, 20% Kolliphor®EL and 70% PBS by oral gavage. The length (L) and width (W) of the tumors are measured 1 to 2 times a week using a digital caliper, and the volume of the tumor is calculated. Mice are also weighed once a week to monitor signs of drug toxicity.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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参考文献 & 客户发表文献

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

质量 =

浓度 *

体积 *

分子量

*选择对应的单位 *空出希望得到的变量，填写另外两个变量

用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入输出 )

* = *

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

摩尔浓度计算公式

稀释公式

连续稀释计算器方程

连续稀释

计算结果