Chemical Structure : DS06652923
CAS No.:
DS06652923
(DS 06652923)
Catalog No.: PC-22888Not For Human Use, Lab Use Only.
DS06652923 is a potent, and orally available EGFR-triple-mutant inhibitor with IC50 of 2.0 nM, 0.89 nM and 6.0 nM for del19/T790M/C797S, L858R/T790M/C797S and WT EGFR resceptively.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
DS06652923 is a potent, and orally available EGFR-triple-mutant inhibitor with IC50 of 2.0 nM, 0.89 nM and 6.0 nM for del19/T790M/C797S, L858R/T790M/C797S and WT EGFR resceptively.
DS06652923 shows potent and selective growth inhibition against Ba/F3 EGFR del19/T90M/C797S cells with GI50 of 9.4 nM, with weak activity against Wildtype Ba/F3 (GI50=760 nM).
DS06652923 inhibits only 14 of the 161 kinases (including 6 mutated EGFR) by more than 50 % at 200 nM.
DS06652923 (12.5 mg/kg (bid), 25 mg/kg (qd), 25 mg/kg (bid), and 100 mg/kg (qd), p.o.) dose-dependent antitumor activity with TGI of 88 %, 111 %, 119 %, and 127 %, respectively, in Balb/c nude mice bearing engineered Ba/F3 (EGFR del19/T790M/C797S) tumors.
Physicochemical Properties
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M.Wt
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629.69
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Formula
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C28H33F2N9O4S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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2-[1-(Cyclopropylsulfonyl)-1H-pyrazol-4-yl]-N-{5-[3-(difluoromethoxy)-1-(1-methylpiperidin-4-yl)-1H-pyrazol-4-yl]-4-(propan-2-yloxy)pyridin-2-yl}pyrimidin-4-amine
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References
1. Kageji H, et al. Bioorg Med Chem. 2024 Jul 30;111:117862.
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