| CAS NO: | 1226549-49-0 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| Cas No. | 1226549-49-0 |
| 分子式 | C32H31N5O3 |
| 分子量 | 533.62 |
| 溶解度 | DMSO : 250 mg/mL (468.50 mM; Need ultrasonic) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | DBPR112 is an orally active furanopyrimidine-based EGFR inhibitor with IC50s of 15 nM and 48 nM for EGFRWT and EGFRL858R/T790M, respectively. DBPR112 can occupy the ATP-binding site. DBPR112 has significant antitumor efficacy[1]. DBPR112 (compound 78; 0.32-1000 nM; 16 hours) induces reduction of phosphorylated EGFR in a dose-dependent manner[1]. DBPR112 shows the inhibitory activity against HCC827 (CC50=25 nM), H1975 (CC50=620 nM) and A431 Cell (CC50=1.02 μM) cell lines[1]. DBPR112 occupies the ATP-binding site and interacts with surrounding residues by covalent bonding, hydrogen bonds, and hydrophobic interactions, which give it a potent inhibitory activity against WT EGFR[1]. DBPR112 (orally; 20-50 mg/kg; 5 days/week for 2 consecutive weeks) significantly reduces tumor growth in HCC827 tumor model. DBPR112 (orally; 50 mg/kg; once a day for 15 days) has a significant antitumor effect (mean tumor growth inhibition of 34%) in H1975 tumor model[1]. DBPR112 (IV; 5 mg/kg) has a T1/2 of 2.3 hours, a CL of 55.6 mL/min•kg, and a Vss of 8.6 L/kg for rats[1]. [1]. Lin SY, et al. Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer. J Med Chem. 2019 Nov 27;62(22):10108-10123. |
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