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PD153035 HCl (SU5271; ZM252868)

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PD153035 HCl (SU5271; ZM252868)
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Cat #: V0568 CAS #: 183322-45-4 Purity ≥ 98%

Description: PD153035 HCl (SU-5271; ZM-252868), the hydrochloride salt of PD153035 (also called PD-153035), is an ATP competitive EGFR inhibitor with potential antineoplastic activity.

References: Bridges AJ, et al. Tyrosine kinase inhibitors. 8. An unusually steep structure-activity relationship for analogues of 4-(3-bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a potent inhibitor of the epidermal growth factor receptor. J Med Chem. 1996 Jan 5;39(1):267-76.

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Molecular Weight (MW)396.67
Molecular FormulaC₁₆H₁₅BrClN₃O₂
CAS No.183322-45-4
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 0.5 mg/mL (1.3 mM)r
Water: <1 mg/mLr
Ethanol: <1 mg/mL
Solubility In Vivo30% propylene glycol, 5% Tween 80, 65% D5W: 30mg/mL
SMILES CodeCOC1=CC2=NC=NC(NC3=CC=CC(Br)=C3)=C2C=C1OC.[H]Cl
SynonymsSU-5271 HCl , PD 153035; PD-153035; SU 5271 HCl; SU5271 HCl; ZM-252868 HCl; ZM 252868 HCl; ZM252868 HCl; PD153035; PD153035 HCl; PD 153035 HCl; PD-153035 HCl; PD 153035 hydrochloride; PD-153035 hydrochloride; PD153035 hydrochloride; ZM 252868; Tyrphostin AG 1517; AG 1517; ZM-252868; ZM252868; SU-5271, SU 5271; SU5271;
ProtocolIn VitroPD153035 inhibits EGF-stimulated receptor autophosphorylation in A431 human epidermoid carcinoma cells, with an IC50 of 14 nM.
In VivoPD153035 levels in the plasma and tumor rise to 50 and 22 μM within 15 minutes following a single i.p. dose of 80 mg/kg. While the plasma levels of PD 153035 falls below 1 μM by 3 hours, in the tumors it remains at micromolar concentrations for at least 12 hours. The tyrosine phosphorylation of the EGF receptor is rapidly suppressed by 80-90% in the tumors.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.5210 mL12.6049 mL25.2099 mL50.4197 mL
5mM0.5042 mL2.5210 mL5.0420 mL10.0839 mL
10mM0.2521 mL1.2605 mL2.5210 mL5.0420 mL
20mM0.1260 mL0.6302 mL1.2605 mL2.5210 mL
Quality Control Documentation
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: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.