1. Protein Tyrosine Kinase/RTK
  2. PDGFR


Cat. No.: HY-101489
Handling Instructions

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

Size Stock
250 mg Get quote
500 mg Get quote

* Please select Quantity before adding items.

Customer Review

View All PDGFR Isoform Specific Products:

  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References


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

IC50: 68.6 nM (PDGFRα), 136.6 nM (PDGFRβ)[1];68.6 nM (Bcr-Abl), 136.6 nM (T315I mutant)[2]

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].
Solvent & Solubility
In Vitro: 

10 mM in DMSO

Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8777 mL 9.3886 mL 18.7772 mL
5 mM 0.3755 mL 1.8777 mL 3.7554 mL
10 mM 0.1878 mL 0.9389 mL 1.8777 mL
*Please refer to the solubility information to select the appropriate solvent.
Molecular Weight









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


Room temperature in continental US; may vary elsewhere

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Inquiry Online

Your information is safe with us. * Required Fields.

Product name



Applicant name *


Email address *

Phone number *


Organization name *

Country or Region *


Requested quantity *


Bulk Inquiry

Inquiry Information

Product Name:
Cat. No.:


Cat. No.: HY-101489