XP-524|cas:2344825-52-9|西域试剂

XP-524,99.66%

产品编号：Bellancom-147008| CAS NO：2344825-52-9| 分子式：C₃₀H₂₈N₆O₃S| 分子量：552.65

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-147008		￥12300.00	杭州北京（现货）

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XP-524

产品介绍

XP-524 是一种有效的 BET 和 EP300 抑制剂。XP-524 在体内显示出强大的杀肿瘤活性。 XP-524 可防止 KRAS 诱导的体内肿瘤转化，并延长两种侵袭性 PDAC 转基因小鼠模型的存活时间。XP-524 还增强了自身肽的表达和将肿瘤细胞向细胞毒性 T 淋巴细胞的募集。XP-524 具有研究胰腺导管腺癌（PDAC）的潜力。

生物活性

XP-524 is a potent BET and EP300 inhibitor. XP-524 shows great tumoricidal activity in vivo. XP-524 prevents KRAS-induced, neoplastic transformation in vivo and extends survival in two transgenic mouse models of aggressive PDAC. XP-524 also enhances the presentation of self-peptide and tumor recruitment of cytotoxic T lymphocytes. XP-524 has the potential for the research of pancreatic ductal adenocarcinoma (PDAC).

体外研究

体内研究

XP-524 (5 mg/kg; i.p.; daily for 150 days) extends survival and inhibits KRAS signaling in uurinePDAC.
XP-524 (5 mg/kg; i.p.; daily for 250 days) Cooperates with PD-1 inhibition to further extends survivalin KPC Mice.

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

Animal Model:	15 weeks KPC mice
Dosage:	5 mg/kg
Administration:	I.p., daily for 150 days
Result:	Significantly delayed mortality in KPC mice, extending median survival from 43- to 108-d postenrollment and reduced ERK activation, with parallel reductions in cell prolif-eration and uniform increases in apoptosis.

Animal Model:	15 weeks KPC mice
Dosage:	5 mg/kg
Administration:	I.p.; daily (200-μg dose of anti–PD-1 every other day) for 250 days
Result:	Increased in cell-mediated cytotoxicity andreduction in T cell exhaustion, the combination of XP-524 andanti–PD-1 enhanced expression of the surrogate marker of cyto-toxicity perforin-1 in tumor-infiltrating CD8+T cell.

体内研究

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

Animal Model:	15 weeks KPC mice
Dosage:	5 mg/kg
Administration:	I.p., daily for 150 days
Result:	Significantly delayed mortality in KPC mice, extending median survival from 43- to 108-d postenrollment and reduced ERK activation, with parallel reductions in cell prolif-eration and uniform increases in apoptosis.

Animal Model:	15 weeks KPC mice
Dosage:	5 mg/kg
Administration:	I.p.; daily (200-μg dose of anti–PD-1 every other day) for 250 days
Result:	Increased in cell-mediated cytotoxicity andreduction in T cell exhaustion, the combination of XP-524 andanti–PD-1 enhanced expression of the surrogate marker of cyto-toxicity perforin-1 in tumor-infiltrating CD8+T cell.

性状

Solid

溶解性数据

In Vitro:

DMSO : 33.33 mg/mL (60.31 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8095 mL	9.0473 mL	18.0946 mL
5 mM	0.3619 mL	1.8095 mL	3.6189 mL
10 mM	0.1809 mL	0.9047 mL	1.8095 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 (4.52 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.52 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 (4.52 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (4.52 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 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