AGX51|cas:330834-54-3|西域试剂

AGX51,99.09%

产品编号：Bellancom-129241| CAS NO：330834-54-3| 分子式：C₂₇H₂₉NO₄| 分子量：431.52

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-129241	￥3500.00	杭州北京（现货）
Bellancom-129241	￥5500.00	杭州北京（现货）
Bellancom-129241	￥9900.00	杭州北京（现货）
Bellancom-129241	￥16500.00	杭州北京（现货）
Bellancom-129241	￥22500.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

AGX51

产品介绍

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 the Id1-E47 interaction, leading to ubiquitin-mediated degradation of Ids, cell growth arrest, and reduces viability. AGX51 inhibits the TNBC cell lines with IC₅₀s of nearly 25 μM. AGX51 can be used for the research of cancer.

体外研究

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

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

Western Blot Analysis

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

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

Cell Line:	4T1 cells, HMLE RAS 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, HMLE RAS 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

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

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

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.
AGX51 (15 mg/kg; i.p. twice a day for 3 weeks) exibits anti-tumor activity with autochronous cancer.

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

Animal Model:	Balb/c mice with luciferase-labeled 4T1 cells
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
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.

体内研究

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

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

Animal Model:	Balb/c mice with luciferase-labeled 4T1 cells
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
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.

体内研究

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

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

Animal Model:	Balb/c mice with luciferase-labeled 4T1 cells
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
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.

性状

Oil

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 mg	5 mg	10 mg

1 mM	2.3174 mL	11.5869 mL	23.1739 mL
5 mM	0.4635 mL	2.3174 mL	4.6348 mL
10 mM	0.2317 mL	1.1587 mL	2.3174 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°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: ≥ 2.08 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-CD in 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 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: ≥ 2.08 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。