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Erlotinib
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。
Erlotinib图片
CAS NO:183321-74-6
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
100mg电议
500mg电议
1 g电议
5 g电议

产品名称
埃罗替尼
CP-358774
NSC 718781
OSI-774
产品介绍
Erlotinib (CP-358774) 是一种直接作用的EGFR酪氨酸激酶抑制剂,对人 EGFR 的IC50为 2 nM。Erlotinib 可降低完整肿瘤细胞的 EGFR 自磷酸化,IC50为 20 nM。Erlotinib 用于非小细胞肺癌的研究。
生物活性

Erlotinib (CP-358774) is a directly actingEGFRtyrosine kinase inhibitor, with anIC50of 2 nM for humanEGFR. Erlotinib reducesEGFRautophosphorylation in intact tumor cells with an IC50of 20 nM. Erlotinib is used for the treatment of non-small cell lungcancer[1].

IC50& Target

EGFR

2 nM (IC50, Cell Free Assay)

体外研究
(In Vitro)

Erlotinib (CP-358774) is also a potent inhibitor of the recombinant intracellular (kinase) domain of the EGFR, with an IC50of 1 nM. The proliferation of DiFi cells is strongly inhibited by Erlotinib with an IC50of 100 nM for an 8-day proliferation assay[1]. The combination of B-DIM and Erlotinib (2 μM) results in a significant inhibition of colony formation in BxPC-3 cells when compared with either agent alone. The combination of B-DIM and Erlotinib (2 μM) results in a significant induction of apoptosis only in BxPC-3 cells when compare with the apoptotic effect of either agent alone[2].

体内研究
(In Vivo)

Under the experimental conditions, the combination of B-DIM and Erlotinib (50 mg/kg, i.p.) treatment shows significant decrease (P<0.01) in tumor weight compared with untreated control[2]. Erlotinib (20 mg/kg, p.o.) significantly attenuates Cisplatin (CP)-induced body weight (BW) loss when compared to the CP+vehicle (V) rats (P<0.05). Erlotinib treatment significantly improves renal function in CP-N(normal control group, NC) rats. The CP+Erlotinib (E) rats show significant reduction of the levels of Serum creatinine (s-Cr) (P<0.05), blood urea nitrogen (BUN) (P<0.05), urinary N-acetyl-β-D-glucosaminidase (NAG) index (P<0.05), and significant increase of urine volume (UV) (P<0.05) and Cr clearance (Ccr) (P<0.05) compare to the CP+V rats[3]

Clinical Trial
分子量

393.44

性状

Solid

Formula

C22H23N3O4

CAS 号

183321-74-6

中文名称

埃罗替尼;伊诺替尼;厄洛替尼

运输条件

Room temperature in continental US; may vary elsewhere.

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

DMSO : 3.94 mg/mL(10.01 mM;ultrasonic and warming and heat to 40℃)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.5417 mL12.7084 mL25.4168 mL
5 mM0.5083 mL2.5417 mL5.0834 mL
10 mM0.2542 mL1.2708 mL2.5417 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: 0.5%CMC-Na/saline water

    Solubility: 10 mg/mL (25.42 mM); Suspended solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 50%PEG300   50% saline

    Solubility: 10 mg/mL (25.42 mM); Suspended solution; Need ultrasonic

*以上所有助溶剂都可在本网站选购。