PD153035 | CAS 153436-54-5 (free base)

PD153035

This product is for research use only, not for human use. We do not sell to patients.

For small sizes, please check our retail website as below: www.invivochem.com

Size	Price	Stock
250mg	$650	Check With Us
500mg	$1050	Check With Us
1g	$1575	Check With Us

: [email protected] [email protected]

Cat #: V3248 CAS #: 153436-54-5 (free base) Purity ≥ 98%

Description: PD153035 is reported to be a novel, potent, specific, and ATP competitive inhibitor of EGFR (Epidermal growth factor receptor) tyrosine kinase with Ki and IC50 of 5.2 pM and 29 pM in cell-free assays, and to a lesser degree, of the closely related HER2/neu receptor; PD153035 inhibits EGF-dependent EGFR phosphorylation in a variety of human cancer cell lines over-expressing EGFRs, which include A431, Difi, DU145, MDA-MB-468, ME180 and C4i, with IC50 of 0.22 μM, 0.3 μM, 0.4 μM, 0.68 μM, 0.95 μM and 2.5 μM respectively.

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

Top Publications Citing Invivochem Products

Product Catalog 2022

Guide to Product Handling

Publications Citing InvivoChem Products

Product Promise

Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	360.2
Molecular Formula	C16H14BrN3O2
CAS No.	153436-54-5 (free base)
Storage	-20℃ for 3 years in powder formr
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: 10 mMr
	Water: <1 mg/mLr
	Ethanol: <1 mg/mL
Solubility In Vivo	30% propylene glycol, 5% Tween 80, 65% D5W: 30mg/mL
SMILES Code	COC1=CC2=NC=NC(NC3=CC=CC(Br)=C3)=C2C=C1OC
Synonyms	PD153035; PD 153035; PD-153035; ZM 252868; Tyrphostin AG 1517; AG 1517; ZM 252868; ZM-252868; ZM252868; SU-5271, SU 5271; SU5271;

Protocol	In Vitro	PD153035 (SU 5271) inhibits EGF-stimulated receptor autophosphorylation in A431 human epidermoid carcinoma cells, with an IC50 of 14 nM.
Protocol	In Vivo	PD153035 (SU 5271) 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 PD153035 (SU 5271) 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	1mg	5mg	10mg	20mg
1mM	2.7762 mL	13.8812 mL	27.7624 mL	55.5247 mL
5mM	0.5552 mL	2.7762 mL	5.5525 mL	11.1049 mL
10mM	0.2776 mL	1.3881 mL	2.7762 mL	5.5525 mL
20mM	0.1388 mL	0.6941 mL	1.3881 mL	2.7762 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

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)

Volume_(start)

Concentration_(final)

Volume_(final)

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.