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    PD153035 HCl (SU5271; ZM252868)
    PD153035 HCl (SU5271; ZM252868)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem 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. It inhibits EGFR with Ki and IC50 values of 5.2 pM and 29 pM in cell-free assays, respectively.

    References: Science. 1994 Aug 19;265(5175):1093-5; Invest New Drugs. 1996;13(4):295-302.  2018 Jun 28;424:19-29. 

    Related CAS: 586347-97-9 (nitrate); 183322-45-4 (HCl); 153436-54-5 (free base); 205195-07-9 (xHCl); 

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    Molecular Weight (MW)396.67
    FormulaC₁₆H₁₅BrClN₃O₂
    CAS No.183322-45-4 HCI
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    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
    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;
    SMILES CodeN-(3-bromophenyl)-6,7-dimethoxyquinazolin-4-amine hydrochloride
    Chemical NAmeCOC1=CC2=NC=NC(NC3=CC=CC(Br)=C3)=C2C=C1OC.[H]Cl


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    In Vitro

    In vitro activity: PD 153035 shows a potent and selective inhibitory effect on tyrosine phosphorylation induced with EGF with IC50 of 15 nM and 14 nM in Swiss 3T3 fibroblast and A-431 human epidermoid carcinoma cells, respectively. PD153035 shows growth inhibitory effects in cultures of EGF receptor-overexpressing human cancer cell lines including A431, Difi, DU145, MDA-MB-468 and ME180 cells with IC50 of 0.22 μM, 0.3μM, 0.4 μM, 0.68 μM and 0.95 μM, respectively. PD153035 induces a dose-dependent growth inhibition in nasopharyngeal carcinoma (NPC) cells including NPC-TW01, NPC-TW04, and HONE1 cell lines with IC50 of 12.9 μM, 9.8 μM and 18.6μM, respectively. A recent study shows that PD153035 abolishes COX-2 expression induced by the PAR(2)-activating peptide 2-furoyl-LIGRLO-NH(2) (2fLI) in Caco-2 colon cancer cells.


    Kinase 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. The reaction is initiated by the addition of ATP. After 10 minutes at room temperature, the reaction is terminated by addition of 2 mL of 75 mM phosphoric acid, and the solution is passed through a 2.5-cm phosphocellulose filter disk that binds the peptide. The filter is washed five times with 75 mM phosphoric acid and placed in a vial with 5 mL of scintillation fluid. The uninhibited control activity produces approximately 100,000 cpm.


    Cell Assay: Cells (A431, Difi, DU145, MDA-MB-468 and ME180) are seeded in sixwell plates. The next day, cells are changed to medium containing 0.5% FBS for 18 hours, and then PD153035 is added at various concentrations to the cultures. After 72 hours of treatment, cells are washed once with PBS, harvested with 0.1% human trypsin-l mM EDTA in PBS, and counted with a Coulter counter. The CMK cells grow in suspension and, therefore, do not require trypsinization.

    In VivoIn A431 human epidermoid tumors grown as xenografts in immunodeficient nude mice, PD153035 at 80 mg/kg inhibit EGF receptor tyrosine kinase activity. PD153035 improves glucose tolerance, insulin sensitivity, and signaling and reduces subclinical inflammation in HFD-fed mice. Pretreatment of EGFR inhibitors by 24 hours significantly enhances the cytotoxic effect of doxorubicin, paclitaxel, cisplatin, and 5-fluororuacil in NPCTW04 cells.
    Animal modelA431 cells are injected into the outbred nude mice.
    Formulation & DosageDissolved in water.; 80 mg/kg; i.p. injection
    References

    Science. 1994 Aug 19;265(5175):1093-5; Invest New Drugs. 1996;13(4):295-302.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    PD153035 HCl

    PD153035 reverses ABCG2 mediated drug resistance by blocking the function of ABCG2 transporter.  2018 Jun 28;424:19-29.

    PD153035 HCl

    PD153035 increases the intracellular concentration of [3H]-MX in ABCG2 overexpressing cells.  2018 Jun 28;424:19-29.

    PD153035 HCl

    PD153035 increases ABCG2 hydrolysis of ATP.  2018 Jun 28;424:19-29.

    PD153035 HCl

    PD153035 decreases expression of ABCG2 on ABCG2 overexpressing cells.  2018 Jun 28;424:19-29.

    PD153035 HCl

    The effect of PD153035 on the growth of ABCG2-expressing tumors in nude athymic mice.  2018 Jun 28;424:19-29.

    PD153035 HCl

    Binding geometry of PD153035 into ABCG2 binding pocket by Glide docking algorithms.  2018 Jun 28;424:19-29.


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