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EGFR-IN-82
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Catalog No. T78788Cas No. 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].
EGFR-IN-82
😃Good
Catalog No. T78788Cas No. 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].
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 25 mg | $1,520 | 6-8 weeks | |
| 50 mg | $1,980 | 6-8 weeks | |
| 100 mg | $2,500 | 6-8 weeks |
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Product Introduction
Bioactivity
Chemical Properties
| 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 superior pharmacokinetic properties to Brigatinib [1]. When administered orally at 15-30 mg/kg for 14-21 days, EGFR-IN-82 moderately inhibits tumor growth in a PC9-EGFR Del19/T790M/C797S xenograft mouse model and significantly inhibits growth in a Ba/F3-EGFR Del19/T790M/C797S xenograft model [1]. Pharmacokinetic analysis in Balb/C mice showed the following parameters [1]: Route: p.o.; Dose: 5 mg/kg; C_max: 1574 ng/mL; AUC_0-t: 15375 ng/mL*h; AUC_0-∞: 15632 ng/mL*h; t_1/2: 3.5 h; MRT: 6 h. |
| Molecular Weight | 694.6 |
| Formula | C32H41BrN9O2P |
| Cas No. | 2568086-81-5 |
Storage & Solubility Information
| Storage | Shipping with blue ice. |
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
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