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497871-47-3 (Lurbinectedin)

1

Identification

Lurbinectedin Lurbinectedin
Name Lurbinectedin
Formula C41H44N4O10S
MW 784.87
CAS No. 497871-47-3
EINECS
Smiles O[[email protected]@H]([[email protected]@](CC1=CC(C)=C2OC)([H])N(C)[[email protected]]3([H])C1=C2O)N([[email protected]](COC4=O)([H])C5=C(OCO6)C6=C7C)[[email protected]@]3([H])[[email protected]@](SC[[email protected]@]4(NCC8)C9=C8C%10=CC(OC)=CC=C%10N9)([H])C5=C7OC(C)=O
Synonyms PM01183;PM-01183;PM 01183;
InChI InChI=1S/C41H44N4O10S/c1-17-11-20-12-25-39(48)45-26-14-52-40(49)41(38-22(9-10-42-41)23-13-21(50-5)7-8-24(23)43-38)15-56-37(31(45)30(44(25)4)27(20)32(47)33(17)51-6)29-28(26)36-35(53-16-54-36)18(2)34(29)55-19(3)46/h7-8,11,13,25-26,30-31,37,39,42-43,47-48H,9-10,12,14-16H2,1-6H3/t25-,26-,30+,31+,37+,39-,41+/m0/s1
2

Introduction

Lurbinectedin (PM01183) is a new DNA minor groove covalent binder with potent anti-tumour activity; inhibits RMG1 and RMG2 cell growth with IC50 values of 1.25 and 1.16 nM, respectively.

Background Information

Lurbinectedin, also known as?PM01183,? is a?synthetic tetrahydropyrrolo [4, 3, 2-de]quinolin-8(1H)-one alkaloid analogue with potential antineoplastic activity. DNA minor groove-binding agent PM01183 covalently binds to residues lying in the minor groove ......by BOC Sciences
Lurbinectedin (PM01183) is a new DNA minor groove covalent binder with potent anti-tumour activity; inhibits RMG1 and RMG2 cell growth with IC50 values of 1.25 and 1.16 nM, respectively. ......by MedChemexpress Co., Ltd.
Lurbinectedin, also known as PM01183, is a synthetic tetrahydropyrrolo [4, 3, 2-de]quinolin-8(1H)-one alkaloid analogue with potential antineoplastic activity. DNA minor groove-binding agent PM01183 covalently binds to residues lying in the minor groove of DNA, which may result in delayed progression through S phase, cell cycle arrest in the G2/M phase and cell death. ......by MedKoo Biosciences, Inc.
3

Protocol(Only for Reference)

Cell Experiment

Animal Experiment

4

Physical and Chemical Properties

Appearance: EBNumber:EB000124566

Storage condition

Solubility

DMSO: 10 mM by CHEMSCENE, LLC
DMSO: 10 mM by MedChemexpress Co., Ltd.
5

Mechanism and Indication

6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
Lurbinectedin PharmaMar Advanced Solid Tumors 2015/8/1 Phase 2
Lurbinectedin PharmaMar Solid Tumors 2015/8/1 Phase 1
Lurbinectedin PharmaMar Advanced Solid Tumors 2014/7/30 Phase 1
Lurbinectedin PharmaMar Metastatic Breast Cancer|Pancreatic Cancer|Metastatic Colorectal Cancer 2013/4/1 Phase 1
Lurbinectedin PharmaMar Ovarian Cancer 2015/5/1 Phase 3
Lurbinectedin PharmaMar Non-Small Cell Lung Cancer (NSCLC) 2013/10/1 Phase 2
Lurbinectedin PharmaMar Small-cell Lung Cancer 2016/7/1 Phase 3
Lurbinectedin PharmaMar Advanced Solid Tumors 2016/5/6 Phase 1
Lurbinectedin PharmaMar Specific Advanced Solid Tumors 2011/5/1 Phase 1
Lurbinectedin PharmaMar Endometrial Adenocarcinomas|Neuroendocrine Tumors|Small-cell Lung Cancer With Less Than 2 Prior Cytotoxic-containing Lines of Therapy 2011/5/25 Phase 1
Lurbinectedin PharmaMar ADVANCED SOLID TUMORS 2009/3/1 Phase 1
Lurbinectedin PharmaMar Acute Leukemia 2011/5/1 Phase 1
Lurbinectedin PharmaMar Major Advanced Solid Tumors Other Than Colorectal 2011/11/1 Phase 1
Lurbinectedin PharmaMar Breast Cancer 2012/12/1 Phase 2
Lurbinectedin PharmaMar Breast Cancer|Ovarian Cancer|Gynecological Cancer|Head and Neck Carcinoma|Non-small Cell Lung Cancer|Small Cell Lung Cancer|Non-squamous Cell Lung Cancer 2013/9/1 Phase 1
Lurbinectedin Massachusetts General Hospital|Dana-Farber Cancer Institute|PharmaMar Metastatic Sarcoma 2015/8/1 Phase 2
Lurbinectedin Poveda, Andrés, M.D.|AstraZeneca|PharmaMar Advanced Cancer|Ovarian Cancer|Endometrial Cancer|Breast Cancer 2015/7/1 Phase 1|Phase 2
Lurbinectedin - Launched
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Safety Data of Lurbinectedin

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Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
BOC Sciences
CHEMSCENE, LLC 1mg/USD1800();2mg/USD3360() USA
MedChemexpress Co., Ltd. 1mg/USD1800();2mg/USD3360() USA
MedKoo Biosciences, Inc. USA
Shanghai Haoyuan Chemexpress Co., Ltd. 1mg/USD1800();2mg/USD3360() China
10

Related Products

Other Forms of 497871-47-3

Name CAS No Formula MW

Recommended Compounds in Others

Name CAS No Formula MW
(R)-(+)-Etomoxir (sodium salt) 828934-41-4 C15H18ClNaO4 320.74
Dictamine 484-29-7 C12H9NO2 199.21
3,3',5-Triiodo-L-thyronine (sodium) 55-06-1 C15H11I3NNaO4 672.9553
Fabomotizole (hydrochloride) 173352-39-1 C15H22ClN3O2S 343.8721
FPH2 957485-64-2 C14H16ClN5O2S 353.83
α-Tocopherol (phosphate) 38976-17-9 C29H51O5P 510.69
BAMB-4 891025-25-5 C15H12N2O2 252.27
LDN-27219 312946-37-5 C20H16N4O2S2 408.5
ISO-1 478336-92-4 C12H13NO4 235.24
Aurothioglucose 12192-57-3 C6H11AuO5S 392.18
Oxybenzone 131-57-7 C14H12O3 228.24
ITX3 347323-96-0 C22H17N3OS 371.45
Cardiogreen 3599-32-4 C43H47N2NaO6S2 774.96
Skp2 Inhibitor C1 432001-69-9 C18H13BrN2O4S2 465.34
INH1 313553-47-8 C18H16N2OS 308.4
PF6-AM 1268491-69-5 C33H31BO12 630.4
XEN445 1515856-92-4 C18H17F3N2O3 366.33
Disperse Blue 148 52239-04-0 C19H19N5O4S 413.45026
Solvent Blue 35 17354-14-2 C22H26N2O2 350.454
CID-797718 370586-05-3 C12H11NO3 217.2206

Recommended Compounds in Same Indication

Name CAS No Formula MW
AT9283 896466-04-9 C19H23N7O2 381.43
MSX-122 897657-95-3 C16H16N6 292.34
Demeclocycline (hydrochloride) 64-73-3 C21H22Cl2N2O8 501.31
Linsitinib 867160-71-2 C26H23N5O 421.49
Vintafolide 742092-03-1 C86H109N21O26S2 1917.04
Veliparib 912444-00-9 C13H16N4O 244.29
Veliparib (dihydrochloride) 912445-05-7 C13H18Cl2N4O 317.21
Palifosfamide 31645-39-3 C4H11Cl2N2O2P 221.02
NKP-1339 197723-00-5 C14H12Cl4N4NaRu 502.14
Palbociclib (hydrochloride) 827022-32-2 C24H30ClN7O2 483.99
Didox 69839-83-4 C7H7NO4 169.13
Rucaparib 283173-50-2 C19H18FN3O 323.36
DOXO-EMCH 151038-96-9 C37H42N4O13 750.75
OTX-015 202590-98-5 C25H22ClN5O2S 491.99
Rucaparib (phosphate) 459868-92-9 C19H21FN3O5P 421.36
NLG-919 1402836-58-1
AVN-944 297730-17-7 C25H27N5O5 477.51
Marimastat 154039-60-8 C15H29N3O5 331.4079
CB-5083 1542705-92-9 C24H23N5O2 413.47
Voreloxin 175414-77-4 C18H19N5O4S 401.44
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Route of Synthesis

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References

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More Information

Lurbinectedin

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