| Identification | Back Directory | [Name]
DBPR112 | [CAS]
1226549-49-0 | [Synonyms]
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)- | [Molecular Formula]
C32H31N5O3 | [MDL Number]
MFCD32263034 | [MOL File]
1226549-49-0.mol | [Molecular Weight]
533.62 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 250 mg/mL (468.50 mM; Need ultrasonic) | [form ]
Solid | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
Gozanertinib is an orally active furanopyrimidine-based EGFR inhibitor with IC50s of 15 nM and 48 nM for EGFRWT and EGFRL858R/T790M, respectively. Gozanertinib can occupy the ATP-binding site. Gozanertinib has significant antitumor efficacy[1]. | [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]. | [in vivo]
Gozanertinib (orally; 20-50 mg/kg; 5 days/week for 2 consecutive weeks) significantly reduces tumor growth in HCC827 tumor model. Gozanertinib (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].
Gozanertinib (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].
| Animal Model: | HCC827 tumor model (6- to 8-week-old athymic NU-Fox1nu nude mice)[1] | | Dosage: | 20, 50 mg/kg | | Administration: | Orally; 5 days/week for 2 consecutive weeks (days 1-5 and 8-12) | | Result: | Significantly reduced tumor growth.
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| Animal Model: | Rats[1] | | Dosage: | 5 mg/kg for IV and 20 mg/kg for PO (Pharmacokinetic Analysis) | | Administration: | IV or PO | | Result: | Had a T1/2 of 2.3 hours, a CL of 55.6 mL/min?kg, and a Vss of 8.6 L/kg by IV.
Had a T1/2 of 3.4 hours, a Cmax of 508 ng/mL and an AUC of 2978 ng/mL?h by PO.
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| [IC 50]
EGFRWT: 15 nM (IC50); EGFRL858R/T790M: 48 nM (IC50) | [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. |
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| Company Name: |
cjbscvictory
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| Tel: |
13348960310 13348960310 |
| Website: |
https://www.weikeqi-biotech.com/ |
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