Bioactivity | DDC-01-163 is a mutant-selective allosteric PROTAC-based EGFR degrader, with an IC50 of 45 nM (Pink: EGFR ligand (HY-151048); Black: linker (HY-W008005); Blue: CRBN ligand (HY-14658))[1]. |
Invitro | DDC-01-163 (0-10 μM) 浓度依赖性地抑制了 L858R/T790M EGFR 突变体 Ba/F3 细胞的增殖,而对野生型 EGFR-Ba/F3 细胞无影响[1]。DDC-01-163在 L858R/T790M 细胞中对 EGFR 显示出IC50/EC50值为96 nM[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> DDC-01-163 相关抗体: |
CAS | 2140806-84-2 |
Formula | C49H51N9O9S |
Molar Mass | 942.05 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Jaebong Jang, et al. Mutant-Selective Allosteric EGFR Degraders are Effective Against a Broad Range of Drug-Resistant Mutations. Angew Chem Int Ed Engl. 2020 Aug 17;59(34):14481-14489. [2]. Surya Kant Tripathi, et al. Allosteric mutant-selective fourth-generation EGFR inhibitors as an efficient combination therapeutic in the treatment of non-small cell lung carcinoma. Drug Discov Today. 2021 Jun;26(6):1466-1472. |