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EGFR-IN-82

Catalog No. T78788 CAS 2568086-81-5

EGFR-IN-82 (Compound 8a) is a potent, orally active inhibitor of EGFR, exhibiting IC50 values of 0.09 nM for EGFR L858R/T790M/C797S and 0.06 nM for EGFR Del19/T790M/C797S. It lacks significant inhibitory effects on EGFR WT. Demonstrating anti-proliferative properties, EGFR-IN-82 also inhibits tumor growth in nude mice, rendering it applicable in non-small cell lung cancer research [1].

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EGFR-IN-82, CAS 2568086-81-5

Pack Size	Availability	Price/USD
25 mg	6-8 weeks	$ 1,520.00
50 mg	6-8 weeks	$ 1,980.00
100 mg	6-8 weeks	$ 2,500.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

Storage & Solubility Information

Description	EGFR-IN-82 (Compound 8a) is a potent, orally active inhibitor of EGFR, exhibiting IC50 values of 0.09 nM for EGFR L858R/T790M/C797S and 0.06 nM for EGFR Del19/T790M/C797S. It lacks significant inhibitory effects on EGFR WT. Demonstrating anti-proliferative properties, EGFR-IN-82 also inhibits tumor growth in nude mice, rendering it applicable in non-small cell lung cancer research [1].
In vitro	EGFR-IN-82 (compound 8a), following a 72 hour exposure, significantly inhibited the growth of Ba/F3-EGFR Del19/T790M/C797S cells, with an IC50 value of 12.7 nM, yet exhibited no notable effect on the proliferation of A431 cells [1].
In vivo	EGFR-IN-82 (compound 8a) exhibits pharmacokinetic properties superior to Brigatinib [1]. When administered orally at doses of 15 - 30 mg/kg over 14 - 21 days, EGFR-IN-82 moderately inhibits tumor growth in a PC9-EGFR Del19/T790M/C797S xenograft mouse model and markedly inhibits tumor growth in a Ba/F3-EGFR Del19/T790M/C797S xenograft mouse model [1]. Pharmacokinetic analysis in Balb/C mice demonstrated the following parameters [1]: Route Dose (mg/kg), C max (ng/mL), AUC 0-t (ng/mLh), AUC 0-∞ (ng/mLh), t 1/2 (h), MRT (h), p.o. 5, 1574, 15375, 15632, 3.5, 6.

Molecular Weight	694.6
Formula	C32H41BrN9O2P
CAS No.	2568086-81-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

EGFR-IN-82 2568086-81-5 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR inhibitor inhibit

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