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248594-19-6 (Erlotinib (mesylate))

1

Identification

Erlotinib (mesylate) Erlotinib (mesylate)
Name Erlotinib (mesylate)
Formula C23H27N3O7S
MW 489.54
CAS No. 248594-19-6
EINECS
Smiles CS(=O)(O)=O.COCCOC1=CC2=NC=NC(NC3=CC=CC(C#C)=C3)=C2C=C1OCCOC
Synonyms Tarceva;CP-358774;OSI-774;NSC 718781;R 1415; N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine methanesulfonate
InChI InChI=1S/C22H23N3O4.CH4O3S/c1-4-16-6-5-7-17(12-16)25-22-18-13-20(28-10-8-26-2)21(29-11-9-27-3)14-19(18)23-15-24-22;1-5(2,3)4/h1,5-7,12-15H,8-11H2,2-3H3,(H,23,24,25);1H3,(H,2,3,4)
2

Introduction

Erlotinib mesylate (R 1415; CP-358774; OSI-774)is a directly acting inhibitor of human EGFR tyrosine kinase with an IC50 of 2 nM. IC50 Value: 2 nM [1] in vitro: CP-358,774 inhibits the proliferation of DiFi human colon tumor cells at submicromolar concentrations in cell culture and blocks cell cycle progression at the G1 phase.

Background Information

Erlotinib mesylate (R 1415; CP-358774; OSI-774)is a directly acting inhibitor of human EGFR tyrosine kinase with an IC50 of 2 nM. IC50 Value: 2 nM [1] in vitro: CP-358,774 inhibits the proliferation of DiFi human colon tumor cells at submicromolar concentrations in cell culture and blocks cell cycle progression at the G1 phase. This inhibitor produces a marked accumulation of retinoblastoma protein in its underphosphorylated form and accumulation of p27KIP1 in DiFi cells, which may contribute to the cell cycle block [1]. Erlotinib increased NOX4 mRNA and protein expression by increasing its promoter activity and mRNA stability in FaDu cells [2]. in vivo: At doses of 100 mg/kg, CP-358,774 completely prevents EGF-induced autophosphorylation of EGFR in human HN5 tumors growing as xenografts in athymic mice and of the hepatic EGFR of the treated mice [1]. Erlotinib had no single agent antitumor activity, raised serum-VEGF levels, and lacked a synergistic effect in combination with sorafenib [3]. Toxicity: The most common adverse event was skin disorder, followed by diarrhea. Although 45.6% of the patients in this study received erlotinib as a fourth-line or subsequent treatment, the results from this study were similar to those of clinical studies [4]. Clinical trial: A Safety Study in Patients With Advanced Solid Tumors. Phase 1 ......by MedChemexpress Co., Ltd.
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

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Physical and Chemical Properties

Appearance: EBNumber:EB000014001

Storage condition

Solubility

DMSO by MedChemexpress Co., Ltd.
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Mechanism and Indication

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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
Erlotinib (mesylate) Eisai Inc Metastatic non small cell lung cancer 2010/2/28 2013/12/31 Phase 2 Clinical
Erlotinib (mesylate) Eisai Inc Metastatic non small cell lung cancer 2004/12/31 2008/6/1 Phase 2 Clinical
Erlotinib (mesylate) Genentech Inc Glioblastoma 2003/7/31 2005/10/31 Phase 2 Clinical
Erlotinib (mesylate) Sarah Cannon Research Institute Renal cell carcinoma 2004/6/30 2011/8/31 Phase 2 Clinical
Erlotinib (mesylate) - Launched
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Safety Data of Erlotinib (mesylate)

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Spectral Information

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Suppliers List

Company Price and Availability Country/Region
Apexbio Technology LLC 100mg/USD51();500mg/USD153() USA
CHEMSCENE, LLC USA
MedChemexpress Co., Ltd. 100mg/USD50(Get quote);500mg/USD75(Get quote) USA
Shanghai Haoyuan Chemexpress Co., Ltd. 100mg/USD55(Get quote);500mg/USD165(Get quote) China
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Related Products

Other Forms of 248594-19-6

Name CAS No Formula MW
Erlotinib impurity B 183321-83-7 C21H20ClN3O3 397.85
Erlotinib impurity A 183321-85-9 C21H20ClN3O3 397.85
Erlotinib 183321-74-6 C22H16D8ClN3O4 437.95
Erlotinib (Hydrochloride) 183319-69-9 C22H24ClN3O4 429.9
Erlotinib (D6 hydrochloride) 1189953-78-3 C22H18D6ClN3O4 435.93

Recommended Compounds in EGFR Autophagy

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
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
AST-1306 (TsOH) 1050500-29-2 C31H26ClFN4O5S 621.08

Recommended Compounds in Same Indication

Name CAS No Formula MW
LDK378 1032900-25-6 C28H36ClN5O3S 558.14
Pemetrexed (disodium) 150399-23-8 C20H19N5Na2O6 471.37
Volasertib 755038-65-4 C34H50N8O3 618.81
ALK inhibitor 1 761436-81-1 C23H28BrN7O3S 562.48
Olaparib 763113-22-0 C24H23FN4O3 434.46
Afatinib (dimaleate) 850140-73-7 C32H33ClFN5O11 718.08
MGCD-265 875337-44-3 C26H20FN5O2S2 517.6
AT-101 90141-22-3 C30H30O8 518.55
Tivantinib 905854-02-6 C23H19N3O2 369.42
Tivozanib 475108-18-0 C22H19ClN4O5 454.86
Sunitinib 557795-19-4 C22H27FN4O2 398.47
Pazopanib (Hydrochloride) 635702-64-6 C21H24ClN7O2S 473.98
Motesanib (Diphosphate) 857876-30-3 C22H29N5O9P2 569.44
LY2603618 911222-45-2 C18H22BrN5O3 436.3
Crizotinib 877399-52-5 C21H22Cl2FN5O 450.34
Ganetespib 888216-25-9 C20H20N4O3 364.4
Axitinib 319460-85-0 C22H18N4OS 386.47
Carboplatin 41575-94-4 C6H12N2O4Pt 371.25
Lenvatinib 417716-92-8 C21H19ClN4O4 426.85
Temozolomide 85622-93-1 C6H6N6O2 194.15
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Route of Synthesis

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References

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More Information

Erlotinib (mesylate)

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