CAS NO: | 183321-74-6 |
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 |
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 |
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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 |
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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
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