| Company Name: |
DC Chemicals
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021-58447131 13564518121 |
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sales@dcchemicals.com |
| Products Intro: |
Product Name:DBPR112
CAS:1226549-49-0
Purity:98% HPLC Package:100mg，250mg，1g
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| Company Name: |
cjbscvictory
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| Tel: |
13348960310 13348960310 |
| Email: |
3003867561@qq.com |
| Products Intro: |
Product Name:DBPR112
CAS:1226549-49-0
Purity:98% Package:5mg；10mg；20mg；50mg；100mg；200mg
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| | DBPR112 Basic information |
| Product Name: | DBPR112 | | Synonyms: | DBPR112;2-Butenamide, 4-(dimethylamino)-N-[3-[4-[[(1S)-2-hydroxy-1-phenylethyl]amino]-6-phenylfuro[2,3-d]pyrimidin-5-yl]phenyl]-, (2E)-;(S,E)-4-(dimethylamino)-N-(3-(4-((2-hydroxy-1-phenylethyl)amino)-6-phenylfuro[2,3-d]pyrimidin-5-yl)phenyl)but-2-enamide;DBPR-112,DBPR112 | | CAS: | 1226549-49-0 | | MF: | C32H31N5O3 | | MW: | 533.62 | | EINECS: | | | Product Categories: | | | Mol File: | 1226549-49-0.mol |  |
| | DBPR112 Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMSO : 250 mg/mL (468.50 mM; Need ultrasonic) | | form | Solid | | color | Off-white to light yellow |
| | DBPR112 Usage And Synthesis |
| Biological Activity | 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]. | | References | [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. |
| | DBPR112 Preparation Products And Raw materials |
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