1. Protein Tyrosine Kinase/RTK
  2. PDGFR
    Bcr-Abl
  3. GZD856

GZD856 

Cat. No.: HY-101489
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GZD856 is a novel and orally bioavailable PDGFRα/β inhibitor with IC50s of 68.6 and 136.6 nM, respectively. Anti-lung cancer activities. Also a Bcr-AblT315I inhibitor with IC50s of 19.9 and 15.4 nM for Bcr-Abl and T315I mutant.

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

GZD856 Chemical Structure

GZD856 Chemical Structure

CAS No. : 1257628-64-0

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Description

GZD856 is a novel and orally bioavailable PDGFRα/β inhibitor with IC50s of 68.6 and 136.6 nM, respectively. Anti-lung cancer activities[1]. Also a Bcr-AblT315I inhibitor with IC50s of 19.9 and 15.4 nM for Bcr-Abl and T315I mutant[2].

IC50 & Target[1]

PDGFRα

68.6 nM (IC50)

PDGFRβ

136.6 nM (IC50)

Bcr-Abl

15.4 nM (IC50)

Bcr-AblT315I

19.9 nM (IC50)

In Vitro

GZD856 (0.0032-10 μM, 72 h) exerts antiproliferative activity against a panel of lung cancer cells[1].

GZD856 shows dose-dependent inhibition of PDGFRα and PDGFRβ phosphorylation in H1703 and A549 cells, respectively. The activation of downstream AKT (phosphorylation of S473 but not T308), ERK1/2 and STAT3 is also observed after exposure to GZD856, with no obvious effects on total protein levels[1].

GZD856 induces dose-dependent G0/G1 phase arrest and apoptosis in H1703 cells but not in A549 cells[1].

GZD856 strongly suppresses the proliferation of K562, K562R (Q252H) and murine Ba/F3 cells ectopically expressing Bcr-AblWT and Bcr-AblT315I, with IC50s of 2.2, 67.0, 0.64 and 10.8 nM, respectively[2].

Cell Viability Assay[1]

Cell Line: H1703, A549, Calu-6, 95-D, L-78,HCC827, SPCA-1, H1650, H1299, H522, H332 and H820 NSCLC cells.
Concentration: 0.0032-10 μM
Incubation Time: 72 h
Result: GZD856 displays an IC50 of 0.25 μM against the PDGFRα-overexpressing H1703 cells but is 4–60-fold less potent against PDGFRαnegative human lung cancer cell lines regardless of PDGFRβ expression levels[1].
In Vivo

GZD856 (10 and 30 mg/kg/day, 16 days) displays good in vivo antitumor activity in both H1703 and A549 lung cancer models[1].

A 25-mg/kg oral dose of GZD856 exhibits a long half-life of 22.2 h, optimal plasma exposure (Cmax, 899.5 μg/L) and a good oral bioavailability of 78%[1].

GZD856 (10 mg/kg/day, 8 days, oral) potently suppresses tumor growth in mouse bearing xenograft K562 and Ba/F3 cells expressing Bcr-AblT315I[2].

Animal Model: Male CB17-SCID mice (H1703 and A549 cancer cells)[1]
Dosage: 10, 30 mg/kg
Administration: Oral gavage,daily,16 consecutive days
Result: GZD856 exhibits dose-dependent antitumor efficacy in the xenografted mouse with H1703 cancer cells, with tumor growth inhibition (TGI) values of 20.8% and 74.1% at dosages of 10 and 30 mg/kg/day, respectively. GZD856 also displays obvious in vivo antitumor effects in A549- xenograft mice, with a TGI value of 51.1% at 30 mg/kg[1].
Molecular Weight

532.56

Formula

C₂₉H₂₇F₃N₆O

CAS No.

1257628-64-0

SMILES

O=C(NC1=CC=C(CN2CCN(C)CC2)C(C(F)(F)F)=C1)C3=CC=C(C)C(C#CC4=CN5C(N=C4)=CC=N5)=C3

Shipping

Room temperature in continental US; may vary elsewhere

Storage

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

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