文献支持PD158780是有效地 EGFR 家族抑制剂；对EGFR，ErbB2，ErbB3和ErbB4的 IC50 值分别为8 μM，49，52，52 nM。

价格： ￥937

品牌：medchemexpress(MCE)

货号：HY-18609

产品详情

PD158780

PD158780是有效地 EGFR 家族抑制剂；对EGFR，ErbB2，ErbB3和ErbB4的 IC₅₀ 值分别为8 μM，49，52，52 nM

美国medchemexpress（MCE)浙江省一级代理:杭州昊鑫生物科技股份有限公司
MCE中国是全球领先的科研化学品和生物活性化合物供应商，总部位于美国新泽西。我们的产品范围覆盖各种抑制剂、激动剂、API和化合物库。专业、高效的企业灵魂铸造了在行业的卓越地位。热情和充满活力的研发团队拥有着大量的化学和生物科学家。专注于生物活性化合物，拥有着多年的发展历程和丰富的行业经验。

生物活性	PD158780 is a potent EGFR family inhibitor with IC₅₀s of 8 pM, 49, 52, 52 nM for EGFR, ErbB2, ErbB3, and ErbB4, respectively.

体外研究 (In Vitro)	PD158780 inhibits EGF receptor autophosphorylation in A431 human epidermoid carcinoma with IC₅₀ value of 13 nM. PD158780 is highly specific for the EGF receptor in Swiss 3T3 fibroblasts, inhibiting EGF-dependent receptor autophosphorylation and thymidine incorporation at low nanomolar concentrations while requiring micromolar levels for platelet-derived growth factor- and basic fibroblast growth factordependent processes. PD158780 inhibits heregulin-stimulated phosphorylation in the SK-BR-3 and MDAMB-453 breast carcinomas with IC₅₀ values of 49 and 52 nM, respectively, suggesting that the compound is active against other members of the EGF receptor family^[1].

体外研究
(In Vitro)

PD158780 inhibits EGF receptor autophosphorylation in A431 human epidermoid carcinoma with IC₅₀ value of 13 nM. PD158780 is highly specific for the EGF receptor in Swiss 3T3 fibroblasts, inhibiting EGF-dependent receptor autophosphorylation and thymidine incorporation at low nanomolar concentrations while requiring micromolar levels for platelet-derived growth factor- and basic fibroblast growth factordependent processes. PD158780 inhibits heregulin-stimulated phosphorylation in the SK-BR-3 and MDAMB-453 breast carcinomas with IC₅₀ values of 49 and 52 nM, respectively, suggesting that the compound is active against other members of the EGF receptor family^[1].

体内研究 (In Vivo)	PD158780 is active against clone formation in several breast tumors having different expression patterns of the ErbB family. PD158780 shows good therapeutic effect against the A431 epidermoid carcinoma when administered either intraperitoneally or orally. PD158780 produces measurable, significant effects against a mouse fibroblast transfected with human EGFR. PD158780 produces a significant therapeutic effect against the estrogendependent MCF-7 breast carcinoma at equitoxic dose levels^[1].

体内研究
(In Vivo)

PD158780 is active against clone formation in several breast tumors having different expression patterns of the ErbB family. PD158780 shows good therapeutic effect against the A431 epidermoid carcinoma when administered either intraperitoneally or orally. PD158780 produces measurable, significant effects against a mouse fibroblast transfected with human EGFR. PD158780 produces a significant therapeutic effect against the estrogendependent MCF-7 breast carcinoma at equitoxic dose levels^[1].

分子量

330.18

性状

固体

Formula

C₁₄H₁₂BrN₅

CAS 号

171179-06-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

In Vitro:

DMSO : 16.67 mg/mL (50.49 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.0287 mL	15.1433 mL	30.2865 mL
5 mM	0.6057 mL	3.0287 mL	6.0573 mL
10 mM	0.3029 mL	1.5143 mL	3.0287 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℃, 2 years; -20℃, 1 year。-80℃ 储存时，请在 2 年内使用， -20℃ 储存时，请在 1 年内使用。

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: 1.67 mg/mL (5.06 mM); Clear solution; Need ultrasonic

此方案可获得 1.67 mg/mL (5.06 mM) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 16.7 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。
2.
请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: 1.67 mg/mL (5.06 mM); Suspended solution; Need ultrasonic

此方案可获得 1.67 mg/mL (5.06 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 16.7 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。

参考文献	[1]. Fry DW, et al. Biochemical and antiproliferative properties of 4-[ar(alk)ylamino]pyridopyrimidines, a new chemical class of potent and specific epidermal growth factor receptor tyrosine kinase inhibitor. Biochem Pharmacol. 1997 Oct 15;54(8):877-87. [Content Brief]