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抑制剂/激活剂

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凋亡与自噬

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Erlotinib 埃罗替尼; CP-358774; NSC 718781; OSI-774

Erlotinib是一种EGFR抑制剂，IC50 为 2 nM，对EGFR的敏感性比对人c-Src 或 v-Ab高1000多倍。Erlotinib可诱导自噬。

货号：
TK0315
规格：

25mg

100mg

500mg

1g
价格：
￥0.00

产品参数

CAS No.	183321-74-6
生物活性	Erlotinib (CP-358774) is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC50 of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer.
分子式	C22H23N3O4
分子量	393.44
储存条件	Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶解性数据	DMSO : 3.94 mg/mL (10.01 mM; ultrasonic and warming and heat to 40°C)
体内研究	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. 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
体外研究	Erlotinib (CP-358774) is also a potent inhibitor of the recombinant intracellular (kinase) domain of the EGFR, with an IC50 of 1 nM. The proliferation of DiFi cells is strongly inhibited by Erlotinib with an IC50 of 100 nM for an 8-day proliferation assay. 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.
纯度及产品资料	98%

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