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AGX51
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
AGX51图片
CAS NO:330834-54-3

AGX51 是首创的 pan-Id(inhibitors of DNA-binding/differentiation proteins) 拮抗剂和降解剂。AGX51 抑制Id1-E47相互作用，导致泛素介导的 Ids 降解，细胞生长停滞和活力降低。AGX51 能抑制 TNBC，其IC50值约为 25 nM。AGX51 可用于癌症的研究。
生物活性

AGX51 is a first-in-class pan-Id(inhibitors of DNA-binding/differentiation proteins) antagonist and degrader. AGX51 inhibits theId1-E47interaction, leading to ubiquitin-mediated degradation of Ids, cell growth arrest, and reduces viability. AGX51 inhibits the TNBC cell lines withIC50s of nearly 25 μM. AGX51 can be used for the research ofcancer[1].

IC50& Target

IC50: 26.66 μM (4T1), 8.7 μM (HMLE RAS Twist), 22.28 μM (MDA-MB-157), 30.91 μM (MDA-MB-436), 36.55 μM (SK-BR-3), 60 μM (MCF-7), 10.89 μM (PDX-BR7), 11.97 μM (PDX-IBT) , 18.56 μM (PDX-BR11)[1]

体外研究
(In Vitro)

AGX51 (0-80 μM; 24 h) decreases ID1 protein levels in 4T1 cells[1].
AGX51 (40 μM; 0-72 h) decreases ID1 levels protein with a 40 μM concentratio in 4T1 cells[1].
AGX51 (40 μM; 24 h) influences 4T1 cells , ER+, HER2+, TNBC and three breast cancer PDX cell ines[1].
AGX51 (0-80 μM; 24-48 h) influences cell cycle of 4T1 cells[1].
AGX51 (40 μM; 4-24 h) influences phospho-histone H3 levels in 4T1 cells[1].
AGX51 (40 μM; 24 h) influences ROS levels in 4T1 cells[1].

Western Blot Analysis[1]

Cell Line:4T1 cells
Concentration:0, 5, 10, 20, 40 and 80 μM
Incubation Time:24 hours
Result:Decreased ID1 protein levels starting at a concentration of 40 μM in 4T1 cells.

Western Blot Analysis[1]

Cell Line:4T1 cells
Concentration:40 μM
Incubation Time:0, 2, 4, 8 , 12, 24, 48 and 72 hours
Result:Decreased ID1 protein levels starting at 4 h, while until 24 h ID1 protein completely loss.

Cell Viability Assay[1]

Cell Line:4T1 cells, HMLERAS Twist, MDA-MB-157, MDA-MB-436, MDA-MB-231, MDA-MB-453, BT-474, MDA-MB-361, SK-BR-3, MCF-7, T47-D, PDX-BR7, PDX-IBT and PDX-BR11
Concentration:40 μM
Incubation Time:24 hours
Result:Inhibited 4T1, HMLERAS Twist, MDA-MB-157, MDA-MB-436, SK-BR-3, MCF-7, PDX-BR7, PDX-IBT and PDX-BR11 cell lines with IC50s of 26.66, 8.7, 22.28, 30.91, 36.55, 60, 10.89, 11.97 and 18.56 μM, respectively.

Cell Cycle Analysis[1]

Cell Line:4T1 cells
Concentration:40 μM
Incubation Time:24 and 48 hours
Result:Affected cell cycle of 4T1 cells with a G0/G1 phase accumulation.

Cell Viability Assay[1]

Cell Line:4T1 cells
Concentration:40 μM
Incubation Time:4 and 24 hours
Result:Reduced phospho-histone H3 levels in 4T1 cells.

Cell Viability Assay[1]

Cell Line:4T1 cells
Concentration:40 μM
Incubation Time:24 hours
Result:Increased ROS level of 4T1 cells and indicated ROS production is a main mechanism of cell killing.
体内研究
(In Vivo)

AGX51 (50 mg/kg; i.p. twice a day for 4 weeks) inhibits lung metastasis[1].
AGX51 (15 mg/kg; i.p. twice a day for 3 weeks) exibits anti-tumor activity with autochronous cancer[1].

Animal Model:Balb/c mice with luciferase-labeled 4T1 cells[1]
Dosage:50 mg/kg
Administration:Intraperitoneal injection; 60 mg/kg twice a day; for 4 weeks
Result:Inhibited lung metastasis development.
Animal Model:A/J mice with AOM colon tumor model[1]
Dosage:15 mg/kg
Administration:Intraperitoneal injection; 15 mg/kg twice a day; for 3 weeks
Result:Dreased the colon tumors and exhibited anti-tumor activity in AOM colon tumor mice.
分子量

431.52

性状

Oil

Formula

C27H29NO4

CAS 号

330834-54-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Pure form-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL(231.74 mM;Need ultrasonic)

Ethanol : 100 mg/mL(231.74 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.3174 mL11.5869 mL23.1739 mL
5 mM0.4635 mL2.3174 mL4.6348 mL
10 mM0.2317 mL1.1587 mL2.3174 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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 (4.82 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.82 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-CDin saline)

    Solubility: 2.08 mg/mL (4.82 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (4.82 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 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 (4.82 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.82 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本网站选购。
 
 
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