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183320-51-6 (OSI-420)

1

Identification

OSI-420 OSI-420
Name OSI-420
Formula C21H22ClN3O4
MW 415.87
CAS No. 183320-51-6
EINECS
Smiles OCCOC1=CC2=C(N=CN=C2NC3=CC=CC(C#C)=C3)C=C1OCCOC.Cl
Synonyms Desmethyl Erlotinib;CP-473420;OSI420;OSI 420;CP473420;CP 473420; 2-((4-((3-ethynylphenyl)amino)-7-(2-methoxyethoxy)quinazolin-6-yl)oxy)ethanol hydrochloride
InChI InChI=1S/C21H21N3O4.ClH/c1-3-15-5-4-6-16(11-15)24-21-17-12-19(27-8-7-25)20(28-10-9-26-2)13-18(17)22-14-23-21;/h1,4-6,11-14,25H,7-10H2,2H3,(H,22,23,24);1H
2

Introduction

OSI-420 (Desmethyl Erlotinib,CP-473420) is an active metabolite of erlotinib which is an orally active EGFR tyrosin kinase inhibitor with IC50 of 2 and 20 nM for the inhibition of human EGFR and EGFR autophosphorylation in tumor cells. IC50 value: Target: in vitro: OSI-420 is the major metabolite of Erlotinib in human plasma.

Background Information

OSI-420 (CP-473420) is an active metabolite of erlotinib which is an orally active EGFR tyrosin kinase inhibitor with IC50 of 2 and 20 nM for the inhibition of human EGFR and EGFR autophosphorylation in tumor cells. ......by BOC Sciences
OSI-420 is an active metabolite of erlotinib, which is a potent EGFR tyrosin kinase inhibitor. ......by MedChemexpress Co., Ltd.
Shelf life: >2 years if stored properly Drug formulation: ......by MedKoo Biosciences, Inc.
OSI-420 is the active metabolite of Erlotinib (EGFR inhibitor with IC50 of 2 nM). ......by Selleck Chemicals LLC
OSI-420 is the active metabolite of Erlotinib (EGFR inhibitor with IC50 of 2 nM). ......by Target Molecule Corp.
3

Protocol(Only for Reference)

Cell Experiment

Cell lines A549, H322, H3255, H358 H661, H1650, H1975, H1299, H596 cells
Conditions 30 nM-20 μM; 72 hour
Method Exponentially growing cells are seeded in 96-well plastic plates and exposed to serial dilutions of erlotinib, pemetrexed, or the combination at a constant concentration ratio of 4:1 in triplicates for 72 h. Cell viability is assayed by cell count and the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Growth inhibition is expressed as the percentage of surviving cells in drug-treated versus PBS-treated control cells (which is considered as 100% viability). The IC50 value is the concentration resulting in 50% cell growth inhibition by a 72-h exposure to drug(s) compared with untreated control cells and is calculated by the CalcuSyn software.
Source Selleck Chemicals LLC

Animal Experiment

Animal Models Male 5-week-old BALB-nu/nu mice with HPAC
Dosage 50 mg/kg
Formulation 6% Captisol
Administration Oral administration
Source Selleck Chemicals LLC
4

Physical and Chemical Properties

Appearance:White to off-white solid EBNumber:EB000028699

Storage condition

Solubility

DMSO by MedChemexpress Co., Ltd.
(25°C) * In vitro DMSO 83 mg/mL warming (199.58 mM); Water<1 mg/mL (<1 mM); Ethanol<1 mg/mL (<1 mM) by Selleck Chemicals LLC
5

Mechanism and Indication

6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
OSI-420 University of Athens Metastatic non small cell lung cancer 2012/1/31 Phase 4 Clinical
OSI-420 Roche Holding AG Metastatic non small cell lung cancer 2014/1/31 2016/7/31 Phase 4 Clinical
OSI-420 Roche Holding AG Metastatic non small cell lung cancer 2011/9/30 2013/9/30 Phase 4 Clinical
OSI-420 Roche Holding AG Metastatic non small cell lung cancer 2012/5/31 2015/12/31 Phase 4 Clinical
OSI-420 Cantonal Hospital of St. Gallen Cancer 2011/9/30 2014/5/31 Phase 4 Clinical
OSI-420 - Launched
OSI-420 - No Development Reported
7

Safety Data of OSI-420

8

Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
BOC Sciences
CHEMSCENE, LLC 5mg/USD144();10mg/USD252() USA
MedChemexpress Co., Ltd. 5mg/USD144();10mg/USD252() USA
MedKoo Biosciences, Inc. USA
Selleck Chemicals LLC 5mg/USD170(In stock);10mM/1mLIn DMSO/USD280(In stock);10mg/USD320(In stock);50mg/USD770(In stock);200mg/USD1670(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD144();10mg/USD252() China
Target Molecule Corp. 10mg/USD201();50mg/USD529() USA
10

Related Products

Other Forms of 183320-51-6

Name CAS No Formula MW
OSI-420 (free base) 183321-86-0 C21H21N3O4 379.41

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
PD168393 194423-15-9 C17H13BrN4O 369.2153
AG 18 118409-57-7 C10H6N2O2 186.17
Afatinib (dimaleate) 850140-73-7 C32H33ClFN5O11 718.08
Chrysophanol 481-74-3 C15H10O4 254.2375
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
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
PU-H71 873436-91-0 C18H21IN6O2S 512.37
MGCD-265 analog 875337-44-3 C26H20FN5O2S2 517.5977
AT-101 90141-22-3 C30H30O8 518.55
Tivantinib 905854-02-6 C23H19N3O2 369.42
Sunitinib 557795-19-4 C22H27FN4O2 398.47
Motesanib (Diphosphate) 857876-30-3 C22H29N5O9P2 569.44
Octreotide (acetate) 79517-01-4 C51H70N10O12S2 1079.29
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
AXL1717 477-47-4 C22H22O8 414.41
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Route of Synthesis

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References

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More Information

OSI-420

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