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Chemical Structure : TQB3804
CAS No.: 2267329-76-8
Catalog No.: PC-38032Not For Human Use, Lab Use Only.
TQB3804 (EGFR-IN-7) is a selective, potent, 3rd generation EGFR C797S inhibitor with IC50 of 1.07 nM and 0.13 nM for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) respectively.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $228 | In stock | |
| 10 mg | $378 | In stock | |
| 50 mg | $898 | In stock | |
| 100 mg | $1380 | In stock | |
| 500 mg | Get quote | ||
| 1 g | Get quote |
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TQB3804 (EGFR-IN-7) is a selective, potent, 3rd generation EGFR C797S inhibitor with IC50 of 1.07 nM and 0.13 nM for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) respectively.
TQB3804 displays potent enzymatic activities for EGFRd746-750/T790M/C797S, EGFRL858R/T790M/C797S, EGFRd746-750/T790M, and EGFRL858R/T790M with IC50 of 0.46, 0.13, 0.26, and 0.19 nM respectively, and has similar enzymatic activity for EGFRWT (IC50=1.07 nM) to Osimertinib.
TQB3804 shows expected anti-proliferative activity Ba/F3 (EGFRd746-750/T790M/C797S), NCI-H1975 (EGFRd746-750/T790M/C797S), PC9 (EGFRd746-750), and A431 (EGFRWT), with IC50 of 26.8, 163, 45, and 147 nM, respectively.
TQB3804 inhibits phosphorylation for EGFR in Ba/F3 (EGFRd746-750/T790M/C797S) cell line with IC50 of 18.5 nM.
TQB3804 significantly inhibits tumor growth in the triple mutant Ba/F3 (EGFRd746-750/T790M/C797S), NCI-H1975 (EGFRd746-750/T790M/C797S), and PC9 (EGFRd746-750/T790M/C797S) CDX models.
| M.Wt | 694.62 | |
| Formula | C32H41BrN9O2P | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
2,4-Pyrimidinediamine, 5-bromo-N4-[5-(dimethylphosphinyl)-6-quinoxalinyl]-N2-[2-methoxy-5-methyl-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]- |
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