1. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
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  3. DBPR112

DBPR112 

Cat. No.: HY-128778
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DBPR112 is an orally active Furanopyrimidine-Based Epidermal Growth Factor Receptor 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.

For research use only. We do not sell to patients.

DBPR112 Chemical Structure

DBPR112 Chemical Structure

CAS No. : 1226549-49-0

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Description

DBPR112 is an orally active Furanopyrimidine-Based Epidermal Growth Factor Receptor 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].

IC50 & Target[1]

EGFRWT

15 nM (IC50)

EGFRL858R/T790M

48 nM (IC50)

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: H1975 cells
Concentration: 0.32, 1.6, 8.0, 40, 200, 1000 nM
Incubation Time: 16 hours
Result: Induced reduction of phosphorylated EGFR in a dose-dependent manner in H1975 cells.
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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.
Molecular Weight

533.62

Formula

C₃₂H₃₁N₅O₃

CAS No.

1226549-49-0

SMILES

O=C(NC1=CC=CC(C2=C(C3=CC=CC=C3)OC4=NC=NC(N[[email protected]@H](C5=CC=CC=C5)CO)=C42)=C1)/C=C/CN(C)C

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

DBPR112DBPR 112DBPR-112EGFREpidermal growth factor receptorErbB-1HER1OrallyFuranopyrimidineATPHCC827H1975Inhibitorinhibitorinhibit

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