2. Protein Tyrosine Kinase/RTK Apoptosis
  3. PDGFR Bcr-Abl Apoptosis
  4. GZD856 formic

GZD856 formic is a potent and orally active PDGFRα/β inhibitor, with IC50s of 68.6 and 136.6 nM, respectively. GZD856 formic is also a Bcr-AblT315I inhibitor, with IC50s of 19.9 and 15.4 nM for native Bcr-Abl and the T315I mutant. GZD856 formic has antitumor activity. GZD856 (formic) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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

GZD856 formic Chemical Structure

GZD856 formic Chemical Structure

CAS No. : 2804039-78-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 509 In-stock
Solution
10 mM * 1 mL in DMSO USD 509 In-stock
Solid
5 mg USD 400 In-stock
10 mg USD 680 In-stock
25 mg USD 1350 In-stock
50 mg USD 2200 In-stock
100 mg USD 3400 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of GZD856 formic:

GZD856 formic Related Antibodies

Top Publications Citing Use of Products

View All PDGFR Isoform Specific Products:

View All Isoforms
PDGFR PDGFRβ PDGFRα

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GZD856 formic is a potent and orally active PDGFRα/β inhibitor, with IC50s of 68.6 and 136.6 nM, respectively. GZD856 formic is also a Bcr-AblT315I inhibitor, with IC50s of 19.9 and 15.4 nM for native Bcr-Abl and the T315I mutant. GZD856 formic has antitumor activity[1][2]. GZD856 (formic) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target[1][2]

PDGFRα

68.6 nM (IC50)

PDGFRβ

136.6 nM (IC50)

Bcr-AblT315I

15.4 nM (IC50)

Bcr-Abl

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 (0.3-3 μM; 24-28 h) induces a dose-dependent G0/G1 phase arrest and apoptosis in H1703 but not A549 cells[1].
GZD856 (0.1-10 μM; 6 h) dose-dependently inhibits the PDGFRα/β phosphorylation and downstream signaling in H1703 and A549 cells[1].
GZD856 inhibits 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].

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

GZD856 formic Related Antibodies

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 hours
Result: Inhibited PDGFRα-overexpressing H1703 cells, with an IC50 of 0.25 μM.

Apoptosis Analysis[1]

Cell Line: H1703 and A549 NSCLC cells
Concentration: 0.3, 1, 3 μM
Incubation Time: 24, 48 hours
Result: Led to 54.1% apoptosis in H1703 cells at the concentration of 3.0 µM, whereas only 15.5% apoptotic A549 cells were observed under similar conditions.
Decreased the CDK4, cyclin D2, CDK2 and Cyclin E protein levels and activated of PARP and Caspase-3 cleavage in H1703 cells.

Western Blot Analysis[1]

Cell Line: H1703 and A549 NSCLC cells
Concentration: 0.1-10 μM
Incubation Time: 6 hours
Result: Inhibited the phosphorylation of PDGFRα and PDGFRβ in a dose-dependent manner.
Observed the activation of downstream AKT, ERK1/2 and STAT3, with no obvious effects on total protein levels.
In Vivo

GZD856 (10-30 mg/kg, p.o. once daily for 16 d) displays good antitumor activity in both H1703 and A549 lung cancer models and is well tolerated. GZD856 inhibits brain and liver metastasis of lung cancer cells in an A549-Luc orthotopic model[1].
GZD856 (10?mg/kg; p.o. once daily for 8 d) potently inhibits tumor growth in mouse bearing xenograft K562 and Ba/F3 cells expressing Bcr-AblT315I[2].
GZD856 (5 mg/kg; a single i.v.) exhibits a long half-life (T1/2=19.97 h), optimal plasma exposure (Cmax=934.38 μg/L) and a AUC0-∞ (8165.8 μg/L?h) in rats[1].
GZD856 (25 mg/kg; a single p.o.) exhibits a long half-life (T1/2=22.2 h), optimal plasma exposure (Cmax=899.5 μg/L) and a good oral bioavailability (BA=78%) in rats[1].

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

Animal Model: Male CB17-SCID mice implanted with H1703 and A549 cancer cells[1]
Dosage: 10, 30 mg/kg
Administration: Oral gavage once daily for 16 days
Result: Displayed antitumor effects in H1703-xenograft mice, with tumor growth inhibition (TGI) values of 20.8% and 74.1% at dosages of 10 and 30 mg/kg, respectively.
Displayed antitumor effects in A549-xenograft mice, with a TGI value of 51.1% at 30 mg/kg.
Was well tolerated in all of the tested groups, with no mortality or significant loss of body weight.
Animal Model: Sprague-Dawley (SD) rats (180-220 g)[1]
Dosage: 5 mg/kg for i.v.; 25 mg/kg for p.o. (Pharmacokinetic Analysis)
Administration: A single intravenous injection and oral administration
Result: I.v.: T1/2=19.97 h; Cmax=934.38 μg/L; AUC0-∞=8165.8 µg/L•h.
P.o.: T1/2=22.2 h; Cmax=899.5 μg/L; BA=78%.
Molecular Weight

578.58

Formula

C30H29F3N6O3
CAS No.
Appearance

Solid

Color

Off-white to light yellow

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.OC=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (172.84 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7284 mL 8.6418 mL 17.2837 mL
5 mM 0.3457 mL 1.7284 mL 3.4567 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7284 mL 8.6418 mL 17.2837 mL 43.2092 mL
5 mM 0.3457 mL 1.7284 mL 3.4567 mL 8.6418 mL
10 mM 0.1728 mL 0.8642 mL 1.7284 mL 4.3209 mL
15 mM 0.1152 mL 0.5761 mL 1.1522 mL 2.8806 mL
20 mM 0.0864 mL 0.4321 mL 0.8642 mL 2.1605 mL
25 mM 0.0691 mL 0.3457 mL 0.6913 mL 1.7284 mL
30 mM 0.0576 mL 0.2881 mL 0.5761 mL 1.4403 mL
40 mM 0.0432 mL 0.2160 mL 0.4321 mL 1.0802 mL
50 mM 0.0346 mL 0.1728 mL 0.3457 mL 0.8642 mL
60 mM 0.0288 mL 0.1440 mL 0.2881 mL 0.7202 mL
80 mM 0.0216 mL 0.1080 mL 0.2160 mL 0.5401 mL
100 mM 0.0173 mL 0.0864 mL 0.1728 mL 0.4321 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

GZD856 formic Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GZD8562804039-78-7GZD 856GZD-856PDGFRBcr-AblApoptosisPlatelet-derived growth factor receptorPDGFRαPDGFRβT315ImutantantitumorInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
GZD856 formic
Cat. No.:
HY-101489A
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (252 KB) Français - FR (252 KB) Deutsch - DE (252 KB) Norwegian - NO (252 KB) Español - ES (252 KB) Swedish - SV (252 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.