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Merck
CN

SML3461

Exatecan mesylate

≥98% (HPLC), topoisomerase-I inhibitor, powder

Synonym(s):

(1S,9S)-9-Ethyl-5-fluoro-9-hydroxy-4-methyl-10,13-dioxo-2,3,9,10,13,15-hexahydro-1H,12H-benzo[de]pyrano[3′,4′:6,7]indolizino[1,2-b]quinoline-1-amine methanesulfonate, DX8951f

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About This Item

Empirical Formula (Hill Notation):
C24H22FN3O4· CH3SO3H
CAS Number:
169869-90-3
Molecular Weight:
531.55
NACRES:
NA.77
UNSPSC Code:
12352200
MDL number:
MFCD04113012

Key Documents

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Product Name

Exatecan mesylate, ≥98% (HPLC)

InChI key

BICYDYDJHSBMFS-GRGFAMGGSA-N

SMILES string

O=C1N2C(C3=NC4=CC(F)=C(C(CC[C@@H]5N)=C4C5=C3C2)C)=CC6=C1COC([C@@]6(CC)O)=O.OS(=O)(C)=O

InChI

1S/C24H22FN3O4.CH4O3S/c1-3-24(31)14-6-18-21-12(8-28(18)22(29)13(14)9-32-23(24)30)19-16(26)5-4-11-10(2)15(25)7-17(27-21)20(11)19;1-5(2,3)4/h6-7,16,31H,3-5,8-9,26H2,1-2H3;1H3,(H,2,3,4)/t16-,24-;/m0./s1

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

DMSO: 2 mg/mL, clear (Warmed)

storage temp.

-10 to -25°C

Quality Level

100

Related Categories

Biochem/physiol Actions

Exatecan mesylate is a water soluble camptothecin (CPT) analog that exhibits a stronger topoisomerase-I inhibitory and antitumor activities and is highly effective against P-glycoprotein (P-gp) mediated multi-drug resistant cells. Several of the exatecan derivative based antibody-drug and peptide-drug conjugate payloads display high therapeutic indices universally across solid tumors.
Water soluble camptothecin (CPT) analog that exhibits a stronger topoisomerase-I inhibitory and antitumor activities

pictograms

Skull and crossbonesHealth hazard
GHS06,GHS08

signalword

Danger

Hazard Classifications

Acute Tox. 2 Oral - Muta. 1B - Repr. 1B

Storage Class

6.1A - Combustible acute toxic Cat. 1 and 2 / very toxic hazardous materials

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000321231
0000321230
0000321231
0000321230
0000229013

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N Joto et al.
International journal of cancer, 72(4), 680-686 (1997-08-07)
We previously reported that DX-8951f, a novel water-soluble camptothecin analog, significantly inhibits the growth of various human and murine tumors in vitro and in vivo. The antitumor effects and topoisomerase I inhibitory activity of DX-8951f are stronger than those of
Jie Chen et al.
Molecular medicine reports, 19(1), 477-489 (2018-11-16)
Unresectable advanced pancreatic cancer (APC) is a highly lethal malignancy. Although numerous chemotherapeutic regimens are available, evidence regarding the survival extension, the life quality improvement, the associated risks and occurrence rates of adverse effects, is required. The effects of 19
Ghassan K Abou-Alfa et al.
Journal of clinical oncology : official journal of the American Society of Clinical Oncology, 24(27), 4441-4447 (2006-09-20)
Exatecan mesylate is a hexacyclic, water-soluble, topoisomerase-1 inhibitor. Exatecan has single-agent and combination activity with gemcitabine in advanced pancreatic cancer. A multicenter, randomized, phase III trial comparing exatecan plus gemcitabine versus gemcitabine alone in advanced pancreatic cancer was conducted. Eligibility

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