| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
|
Purity: ≥98%
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. In cell-free assays, it inhibits EGFR with Ki and IC50 values of 5.2 pM and 29 pM, respectively.
| Targets |
EGFR (Ki = 6 pM); EGFR (IC50 = 25 pM)
|
|---|---|
| ln Vitro |
PD153035 has a 14 nM IC50 and prevents EGF-stimulated receptor autophosphorylation in human epidermoid carcinoma A431 cells[1]. Even at 50 μM, PD153035 has minimal impact on src tyrosine kinases, insulin receptor, PDGFR, FGFR, CSF-1 receptor, or CSF-1 receptor. When applied to fibroblasts or human epidermoid carcinoma cells, PD153035 quickly suppresses the autophosphorylation of the EGF receptor at low nanomolar concentrations. It also specifically prevents EGF-mediated cellular processes such as mitogenesis, early gene expression, and oncogenic transformation[2]. Starting at less than micromolar concentrations, PD153035 inhibits the growth of EGF receptor-positive cell lines in a dose-dependent manner; in most cases, the IC50 is less than 1 pM[3].
|
| ln Vivo |
PD153035 levels after a single intraperitoneal (i.p.) dose of 80 mg/kg rise to 50 and 22 μM in the tumor and plasma within 15 minutes. While PD 153035's plasma levels drop below 1 μM after three hours, the drug stays at micromolar concentrations in tumors for at least twelve hours. Tumors quickly reduce the tyrosine phosphorylation of the EGF receptor by 80–90%[4].
|
| Enzyme Assay |
Enzyme reactions are performed in a total volume of 0.1 mL containing 25 mM Hepes (pH 7.4), 5 mM MgCl2, 2 mM MnCl2, 50 μM sodium vanadate, 0.5 to 1.0 ng of enzyme (which also contains enough EGF to make the final concentrations 2 μg/mL), 10 μM ATP containing 1 μCi of [32P]ATP, varying concentrations of PD153035, and 200 μM of a substrate peptide based on a portion of phospholipase C-γl having the sequence Lys-His-Lys-Lys-Leu-Ala-Glu-Gly-Ser-Ala-Tyr472-Glu-Glu-Val. ATP is added to the mixture to start the reaction. The reaction is stopped after 10 minutes at room temperature by adding 2 mL of 75 mM phosphoric acid. The mixture is then run through a 2.5-cm phosphocellulose filter disk, which binds the peptide. The filter is put in a vial with 5 mL of scintillation fluid after being cleaned five times with 75 mM phosphoric acid. An estimated 100,000 cpm are produced by the uninhibited control activity.
|
| Cell Assay |
PD153035 is applied to various EGF receptor-overexpressing cell lines (A43 1, Difi, MDA-MB-468, MDA-MB-231, DU145, SiHa, C4i, and MEl 80) at escalating 0.125-2.5 p.M. concentrations. The impact of growth inhibitors in monolayer cell culture is evaluated[3].
|
| Animal Protocol |
Mice: PD153035 (80 mg/kg) or a vehicle is injected into mice, and after 20 and 180 minutes, the rumours are removed and extracts are made. Four iterations of the experiment are conducted, using two mice at each time point. ANOVA is used in each of the four experiments to compare the inhibition of EGF-stimulation by PD 153035[3].
|
| References |
|
| Molecular Formula |
C₁₆H₁₅BRCLN₃O₂
|
|---|---|
| Molecular Weight |
396.67
|
| Exact Mass |
395.00362
|
| Elemental Analysis |
C, 48.45; H, 3.81; Br, 20.14; Cl, 8.94; N, 10.59; O, 8.07
|
| CAS # |
183322-45-4
|
| Related CAS # |
PD153035;153436-54-5
|
| Appearance |
Solid powder
|
| SMILES |
COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=CC=C3)Br)OC.Cl
|
| InChi Key |
ZJOKWAWPAPMNIM-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C16H14BrN3O2.ClH/c1-21-14-7-12-13(8-15(14)22-2)18-9-19-16(12)20-11-5-3-4-10(17)6-11;/h3-9H,1-2H3,(H,18,19,20);1H
|
| Chemical Name |
N-(3-bromophenyl)-6,7-dimethoxyquinazolin-4-amine;hydrochloride
|
| Synonyms |
SU-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
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: ~0.5 mg/mL (~1.3 mM)
Water: <1 mg/mL Ethanol: <1 mg/mL |
|---|---|
| Solubility (In Vivo) |
30% propylene glycol, 5% Tween 80, 65% D5W: 30mg/mL (Please use freshly prepared in vivo formulations for optimal results.)
|
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5210 mL | 12.6049 mL | 25.2099 mL | |
| 5 mM | 0.5042 mL | 2.5210 mL | 5.0420 mL | |
| 10 mM | 0.2521 mL | 1.2605 mL | 2.5210 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(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.
PD153035 reversesABCG2mediated drug resistance by blocking the function of ABCG2 transporter.Cancer Lett.2018 Jun 28;424:19-29. |
PD153035 increases the intracellular concentration of [3H]-MX in ABCG2 overexpressing cells.Cancer Lett.2018 Jun 28;424:19-29. |
PD153035 increases ABCG2 hydrolysis of ATP.Cancer Lett.2018 Jun 28;424:19-29. |
PD153035 decreases expression of ABCG2 on ABCG2 overexpressing cells.Cancer Lett.2018 Jun 28;424:19-29. |
The effect of PD153035 on the growth of ABCG2-expressing tumors in nude athymic mice.Cancer Lett.2018 Jun 28;424:19-29. |
Binding geometry of PD153035 into ABCG2 binding pocket by Glide docking algorithms.Cancer Lett.2018 Jun 28;424:19-29. |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
