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中文名称: Nutlin-3a 促销
英文名称: Nutlin-3a
CAS No: 675576-98-4
分子式: C30H30Cl2N4O4
分子量: 581.49
安全技术说明书(PDF) MSDS(PDF) 点击下载技术规格说明书(PDF) 点击下载产品说明书(PDF)
N10191 Nutlin-3a ≥98% (psaitong)
包装规格：
5mg 10mg 50mg in glass bottle
溶解性：
溶于DMSO(≥100mg/mL)
产品描述：

基本信息

产品编号：N10191

产品名称：Nutlin-3a

CAS:

675576-98-4

 

储存条件

粉末

-20℃

三年

 

 

分子式：

C30H30Cl2N4O4

溶于液体

-80℃

六个月

分子量

581.49

-20℃

一个月

化学名： 

 

 

Solubility (25°C)

 

体外

DMSO

100mg/mL (171.97mM)

Ethanol

100mg/mL (171.97mM)

Water

Insoluble

体内（现配现用）

5% DMSO+40% PEG 300+5% Tween 80+50% ddH2O

10mg/mL

＜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

1.7197mL

8.5986mL

17.1972mL

5mM

0.3439mL

1.7197mL

3.4394mL

10mM

0.1720mL

0.8599mL

1.7197mL

50mM

0.0344mL

0.1720mL

0.3439mL

 

生物活性

产品描述

一种有效的MDM2抑制剂。

靶点/IC50

p53/MDM2 interaction
(Cell-free assay)

90nM

 

体外研究

Nutlin-3a is a therapeutic which inhibits MDM2, activates wild-type p53, and induces apoptosis-as a therapeutic compound for TP53 wild-type ovarian carcinomas. Three cell lines (HOC-7, OVCA429 and A2780) with wild-type TP53 are highly sensitive to Nutlin-3a (IC50=4 to 6μM). SKOV3 cells have an IC50 of 38μM to Nutlin-3a. The two remaining ovarian clear cell lines (TOV21G and OVAS), both with TP53 wild-type, are relatively more sensitive to growth inhibition with Nutlin-3a (IC50=14 and 25μm respectively) than the TP53 mutant cell lines. Nutlin-3a is the active enantiomer of Nutlin-3. Nutlin-3a is a highly selective MDM2 antagonist and p53 inducer. Seven days of incubation with 10μM Nutlin-3a leads to >90% inhibition of NIH/3T3 cells’growth but does not affect the proliferation of MEF in which both targets of the drug are eliminated. Nutlin-3a effectively arrestes cell-cycle progression in all cell lines, depleting the S-phase compartment to 0.2-2% and increasing the G1- and G2/M-phase compartments, indicating G1 and G2 arrest.The p53 targets p21 and MDM2 are elevated significantly 3h after Nutlin-3a addition and reach maximal levels at 8h. Nutlin-3a induces apoptosis in≈60% of SJSA-1 and MHM cells after 40h,which increase further after 60h (85% and 65%, respectively).

体内研究

Nutlin-3a is efficacious in all models with average tumor growth inhibition ≥98%. Nutlin-3a suppresses xenograft growth in a dose-dependent fashion with the highest dose (200mg/kg) showing a substantial tumor shrinkage (eight partial and one full regressions). The established SJSA-1 and MHM osteosarcoma xenografts with Nutlin-3a causes extensive tumor regression.

 

推荐实验方法(仅供参考)

细胞实验:

 

All 15 cell lines are plated at a density of 1×103 cells per well in 96-well plates. After 24h, media is exchanged and cells are treated with incremental concentrations of Nutlin 3a (1μM,5μM,10μM,25μM, 50μM, and 70μM). After 72h of incubation,WST-1 is added to each well,and a microplate reader is used at an absorbance of 450nm to measure the number of remaining viable cells. Experiments are repeated with smaller titrations of Nutlin 3a as needed to determine the exact IC50 of cell lines. The IC50 is defined. Cell lines are again plated in a manner identical to above and treated with Nutlin 3a at their respective IC50, and WST-1 is added with cell viability measurement at 24, 48, and 72h.

 

动物实验:

 

Mice

Nude mice bearing s.c. tumor xenografts (10 mice per group in the SJSA-1, LnCaP, and 22Rv1 study and 15 mice per group in the MHM study) are dosed orally twice daily with Nutlin 3a (50-200mg/kg) or vehicle (1% Klucel, 0.1% Tween 80) for 2 weeks (22Rv1 and LnCap) or 3 weeks (SJSA-1 and MHM). Tumor volume is measured with a caliper and calculated. For Western blot analysis, nude mice with established SJSA-1 tumors (200-400 mm3, three animals per group are treated with three doses of Nutlin 3a at 150mg/kg (at 0, 8, and 24h), and tumors are harvested 3h after the last dose. Tumor samples are flash-frozen and processed.
保存条件：
-20℃
UN码：
HazardClass：
危害声明：
安全说明：
搜索质检报告(COA)
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

  • =
    *
    *
    *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):
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