DBPR112
- CAS No.
- 1226549-49-0
- Chemical Name:
- DBPR112
- Synonyms
- DBPR112;DBPR-112,DBPR112;(S,E)-4-(dimethylamino)-N-(3-(4-((2-hydroxy-1-phenylethyl)amino)-6-phenylfuro[2,3-d]pyrimidin-5-yl)phenyl)but-2-enamide;2-Butenamide, 4-(dimethylamino)-N-[3-[4-[[(1S)-2-hydroxy-1-phenylethyl]amino]-6-phenylfuro[2,3-d]pyrimidin-5-yl]phenyl]-, (2E)-
- CBNumber:
- CB45821402
- Molecular Formula:
- C32H31N5O3
- Molecular Weight:
- 533.62
- MDL Number:
- MFCD32263034
- MOL File:
- 1226549-49-0.mol
DBPR112 price
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
ChemScene | CS-0105123 | DBPR112 98.07% | 1226549-49-0 | 5mg | $450 | 2021-12-16 | Buy |
ChemScene | CS-0105123 | DBPR112 98.07% | 1226549-49-0 | 10mg | $800 | 2021-12-16 | Buy |
ChemScene | CS-0105123 | DBPR112 98.07% | 1226549-49-0 | 25mg | $1650 | 2021-12-16 | Buy |
ChemScene | CS-0105123 | DBPR112 98.07% | 1226549-49-0 | 50mg | $2550 | 2021-12-16 | Buy |
ChemScene | CS-0105123 | DBPR112 98.07% | 1226549-49-0 | 100mg | $3800 | 2021-12-16 | Buy |
DBPR112 Chemical Properties,Uses,Production
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
Raw materials
Preparation Products
DBPR112 Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
Fan De(Beijing) Biotechnology Co., Ltd. | 15911056312 | liming@bio-fount.com | China | 9730 | 58 |
DC Chemicals | 021-58447131 13564518121 | sales@dcchemicals.com | China | 9412 | 58 |
cjbscvictory | 13348960310 13348960310 | 3003867561@qq.com | China | 10011 | 58 |
TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24017 | 58 |
RD International Technology Co., Limited | 18024082417 | market@ubiochem.com | China | 9168 | 58 |
Supplier | Advantage |
---|---|
TargetMol Chemicals Inc. | 58 |
Aladdin Scientific | 58 |
Fan De(Beijing) Biotechnology Co., Ltd. | 58 |
DC Chemicals | 58 |
cjbscvictory | 58 |
TargetMol Chemicals Inc. | 58 |
RD International Technology Co., Limited | 58 |