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SML3461

Exatecan mesylate

Name: Exatecan mesylate
Brand: SIGMA

≥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

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

Storage condition:

desiccated

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Product Name

Exatecan mesylate, ≥98% (HPLC)

Quality Level

100

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

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

InChI key

BICYDYDJHSBMFS-GRGFAMGGSA-N

Related Categories

Bioactive Small Molecule Inhibitors

Bioactive Small Molecules

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

GHS06,GHS08

signalword

Danger

hcodes

H300,H340,H360F

pcodes

P202 - P264 - P280 - P301 + P310 - P405 - P501

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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DX-8951f, a water-soluble camptothecin analog, exhibits potent antitumor activity against a human lung cancer cell line and its SN-38-resistant variant.

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

Meta‑analysis of current chemotherapy regimens in advanced pancreatic cancer to prolong survival and reduce treatment‑associated toxicities.

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

Randomized phase III study of exatecan and gemcitabine compared with gemcitabine alone in untreated advanced pancreatic cancer.

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

Global Trade Item Number

SKU	GTIN
SML3461-10MG	04065268816882
SML3461-50MG	04065268816899

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