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Chemical Structure : OBX02-011
CAS No.: 2349336-18-9
Catalog No.: PC-47006Not For Human Use, Lab Use Only.
OBX02-011 is a potent, reversible, fourth-generation EGFR tyrosine kinase inhibitor (TKI) that overcomes the EGFR C797S mutation, inhibits triple mutants Del19/T790M/C797S and L858R/T790M/C797S with IC50 of 0.134 and 2.09 nM, respectively.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $268 | In stock | |
| 25 mg | $458 | In stock | |
| 50 mg | $758 | In stock | |
| 100 mg | $1180 | In stock | |
| 200 mg | Get quote | ||
| 1 g | Get quote |
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OBX02-011 is a potent, reversible, fourth-generation EGFR tyrosine kinase inhibitor (TKI) that overcomes the EGFR C797S mutation, inhibits triple mutants Del19/T790M/C797S and L858R/T790M/C797S with IC50 of 0.134 and 2.09 nM, respectively.
OBX02-011 occupied the ATP-binding site in a similar manner to WZ-4002.
OBX02-011 showed broad activity at low nanomolar concentrations against mutant EGFRs, more potent in Del19/T790M/C797S and L858R/T790M than in other EGFR mutations.
OBX02-011 was highly effective against EGFR triple mutations, and showed substantial selectivity compared with WT EGFR (IC50= 1471 nM in WT, 96.3 nM in Del19/T790M/C797S, and 94.8 nM in L858R/T790M/C797S) in Ba/F3 cell lines expressing EGFR.
OBX02-011 (25 mg/kg, i. p.) effectively inhibited tumor growth and EGFR activity, leading to enhanced survival in transgenic mouse models (EGFRL858R/T790M/C797S).
| M.Wt | 615.194 | |
| Formula | C29H39ClN8O3S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
N-(2-((5-chloro-2-((2-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)amino)pyrimidin-4-yl)amino)phenyl)-N-methylmethanesulfonamide |
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1. Yun Jung Choi, et al. Cancer Res. 2022 Jun 14;canres.0394.2022-2-3 21:03:12.200.
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