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153436-54-5 (PD153035)

1

Identification

PD153035 PD153035
Name PD153035
Formula C16H14BrN3O2
MW 360.21
CAS No. 153436-54-5
EINECS
Smiles COC1=CC(C(NC2=CC(Br)=CC=C2)=NC=N3)=C3C=C1OC
Synonyms 4-[(3-Bromophenyl)amino]-6,7-dimethoxyquinazoline hydrochloride; N-(3-bromophenyl)-6,7-dimethoxyquinazolin-4-amine
InChI InChI=1S/C16H14BrN3O2/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)
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Introduction

PD153035(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(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.
Shelf life: >2 years if stored properly Drug formulation: ......by MedKoo Biosciences, Inc.
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 Target Molecule Corp.
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

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Physical and Chemical Properties

Appearance:White to off-white Solid EBNumber:EB000029023

Storage condition

Solubility

DMSO by MedChemexpress Co., Ltd.
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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 - Discontinued
PD153035 - No Development Reported
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Safety Data of PD153035

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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) USA
MedChemexpress Co., Ltd. 5mg/USD50(In stock);10mg/USD65(In stock);50mg/USD248(In stock) USA
MedKoo Biosciences, Inc. USA
Shanghai Haoyuan Chemexpress Co., Ltd. 10mg/USD59(In stock);50mg/USD248(In stock) China
Shanghai Paulshinechem Co., Ltd. China
Target Molecule Corp. 10mg/USD56();25mg/USD101();50mg/USD168() USA
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Related Products

Other Forms of 153436-54-5

Name CAS No Formula MW
PD153035 (Hydrochloride) 183322-45-4 C16H15BrClN3O2 396.67

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

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