Erlotinib

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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。

CAS NO:

183321-74-6

埃罗替尼
CP-358774
NSC 718781
OSI-774

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°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 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 mg

5 mg

10 mg

1 mM	2.5417 mL	12.7084 mL	25.4168 mL
5 mM	0.5083 mL	2.5417 mL	5.0834 mL
10 mM	0.2542 mL	1.2708 mL	2.5417 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。