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183322-45-4 (PD153035 (Hydrochloride))

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Identification

PD153035 (Hydrochloride) PD153035 (Hydrochloride)
Name PD153035 (Hydrochloride)
Formula C16H15BrClN3O2
MW 396.67
CAS No. 183322-45-4
EINECS
Smiles COC1=CC2=NC=NC(NC3=CC=CC(Br)=C3)=C2C=C1OC.[H]Cl
Synonyms N-(3-bromophenyl)-6,7-dimethoxyquinazolin-4-amine hydrochloride
InChI 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
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Introduction

PD153035 Hcl (ZM 252868; AG 1517) is a potent and specific inhibitor of EGFR with Ki and IC50 of 5.2 pM and 29 pM; little effect against PGDFR, FGFR, CSF-1, InsR and Src. IC50 value: 5.2/29 pM(Ki/IC50) [1] Target: EGFR in vitro: 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 [1].

Background Information

PD153035 Hcl (ZM 252868; AG 1517) is a potent and specific inhibitor of EGFR with Ki and IC50 of 5.2 pM and 29 pM; little effect against PGDFR, FGFR, CSF-1, InsR and Src. IC50 value: 5.2/29 pM(Ki/IC50) [1] Target: EGFR in vitro: 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 [1]. 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 [2]. in vivo: In A431 human epidermoid tumors grown as xenografts in immunodeficient nude mice, PD153035 at 80 mg/kg inhibit EGF receptor tyrosine kinase activity [3]. PD153035 improves glucose tolerance, insulin sensitivity, and signaling and reduces subclinical inflammation in HFD-fed mice [4]. ......by MedChemexpress Co., Ltd.
PD153035 HCl is a potent and specific inhibitor of EGFR with Ki and IC50 of 5.2 pM and 29 pM in cell-free assays; little effect noted against PGDFR, FGFR, CSF-1, InsR and Src. ......by Selleck Chemicals LLC
PD153035 Hcl (ZM 252868; AG 1517) is a potent and specific inhibitor of EGFR with Ki and IC50 of 5.2 pM and 29 pM; little effect against PGDFR, FGFR, CSF-1, InsR and Src. ......by Target Molecule Corp.
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Protocol(Only for Reference)

Cell Experiment

Cell lines A431, Difi, DU145, MDA-MB-468 and ME180
Conditions 0-3 μM; 72 hours
Method Cells 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.
Source Selleck Chemicals LLC

Animal Experiment

Animal Models A431 cells are injected into the outbred nude mice.
Dosage ≤80 mg/kg
Formulation PD153035 is dissolved in water.
Administration Administered via i.p.
Source Selleck Chemicals LLC
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Physical and Chemical Properties

Appearance:Light yellow to yellow Solid EBNumber:EB000029024

Storage condition

Solubility

DMSO <1.2mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL by MedChemexpress Co., Ltd.
(25°C) * In vitro DMSO 0.5 mg/mL (1.26 mM); Water<1 mg/mL (<1 mM); Ethanol<1 mg/mL (<1 mM); In vivo 30% Propylene glycol, 5% Tween 80, 65% D5W30 mg/mL by Selleck Chemicals LLC
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Mechanism and Indication

Signaling Pathways JAK/STAT Signaling Protein Tyrosine Kinase/RTK
Target EGFR
Research Area Cancer
Indications
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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
PD153035 (Hydrochloride) - Not Found
PD153035 (Hydrochloride) - No Development Reported
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Safety Data of PD153035 (Hydrochloride)

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Spectral Information

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Suppliers List

Company Price and Availability Country/Region
CHEMSCENE, LLC 10mg/USD65(In stock);50mg/USD248(In stock);100mg/USD420(In stock) USA
MedChemexpress Co., Ltd. 5mg/USD50(In stock);10mg/USD65(In stock);50mg/USD248(In stock);100mg/USD420(In stock) USA
Selleck Chemicals LLC 10mg/USD90(In stock);50mg/USD370(In stock);200mg/USD970(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. 10mg/USD59(In stock);50mg/USD248(In stock);100mg/USD388(In stock) China
Target Molecule Corp. 10mg/USD75();25mg/USD133();50mg/USD213() USA
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Related Products

Other Forms of 183322-45-4

Name CAS No Formula MW
PD153035 153436-54-5 C16H14BrN3O2 360.21

Recommended Compounds in EGFR

Name CAS No Formula MW
Ginsenoside Rh2 78214-33-2 C36H62O8 622.87
Mutated EGFR-IN-1 1421372-66-8 C25H31N7O 445.56
AZD-9291 (mesylate) 1421373-66-1 C29H37N7O5S 595.71
Mutant EGFR inhibitor 1421373-62-7 C27H30ClN7O2 520.03
AZD-9291 1421373-65-0 C28H33N7O2 499.61
WHI-P180 (hydrochloride) 153437-55-9 C16H16ClN3O3 333.77
WHI-P180 211555-08-7 C16H15N3O3 297.31
Gefitinib (hydrochloride) 184475-55-6 C22H25Cl2FN4O3 483.36
Erlotinib (mesylate) 248594-19-6 C23H27N3O7S 489.54
BGB-102 807640-87-5 C22H25BrN4O2 457.36
Poziotinib 1092364-38-9 C23H21Cl2FN4O3 491.34
CO-1686 (hydrobromide) 1446700-26-0 C27H29BrF3N7O3 636.46
CO-1686 1374640-70-6 C27H28F3N7O3 555.55
CNX-2006 1375465-09-0 C26H27F4N7O2 545.53
PD 168393 194423-15-9 C17H13BrN4O 369.22
AG 18 118409-57-7 C10H6N2O2 186.17
Afatinib (dimaleate) 850140-73-7 C32H33ClFN5O11 718.08
Chrysophanic acid 481-74-3 C15H10O4 254.24
AG-1478 153436-53-4 C16H14ClN3O2 315.75
Mubritinib 366017-09-6 C25H23F3N4O2 468.47

Recommended Compounds in Same Indication

Name CAS No Formula MW
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Route of Synthesis

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References

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More Information

PD153035 (Hydrochloride)

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