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DBPR112

Catalog No. T10965 CAS 1226549-49-0

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.

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DBPR112, CAS 1226549-49-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 116.00
5 mg	In stock	$ 289.00
10 mg	In stock	$ 538.00
25 mg	In stock	$ 868.00
50 mg	In stock	$ 1,180.00
100 mg	In stock	$ 1,590.00
1 mL * 10 mM (in DMSO)	In stock	$ 339.00

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Purity: 98.29%

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Description	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.
Targets&IC50	EGFR (WT):15 nM, EGFR (L858R/T790M):48 nM
In vitro	DBPR112 (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].
In vivo	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].

Molecular Weight	533.62
Formula	C32H31N5O3
CAS No.	1226549-49-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 225 mg/mL (421.6 mM), Sonication is recommended.

References and Literature

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 Sep 27.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Tyrosine Kinase Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Anti-Cancer Drug Library Inhibitor Library Kinase Inhibitor Library Anti-Lung Cancer Compound Library Bioactive Compound Library Covalent Inhibitor Library

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Keywords

DBPR112 1226549-49-0 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR DBPR-112 DBPR 112 inhibitor inhibit

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