Exatecan mesylate dihydrate (Synonyms: DX-8951 mesylate dihydrate)

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Exatecan (DX-8951) mesylate dihydrate is a DNA topoisomerase I inhibitor, with an IC₅₀ of 2.2 μM (0.975 μg/mL), and can be used in cancer research.

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No. CAS : 197720-53-9

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Other In-stock Forms of Exatecan mesylate dihydrate:

Exatecan Exatecan mesylate

Other Forms of Exatecan mesylate dihydrate:

Exatecan-d₅ mesylate In-stock
DXd In-stock
DXd-d₅ In-stock
Deruxtecan In-stock
Deruxtecan-d₂ In-stock
Gly-Gly-Phe-Gly-NH-O-CO-Exatecan hydrochloride In-stock
(1S,9R)-Exatecan mesylate In-stock
(1R,9R)-Exatecan mesylate In-stock
Gly-Gly-Phe-Gly-NH-O-CO-Exatecan In-stock
(1R)-Deruxtecan In-stock
Exatecan In-stock
Exatecan mesylate In-stock
Deruxtecan-d₄ Obtener un presupuesto
Deruxtecan-d₆ Obtener un presupuesto
Deruxtecan-d₄-1 Obtener un presupuesto
(1R,9S)-Dxd Obtener un presupuesto

23 Publications Citing Use of MCE Exatecan mesylate dihydrate

In Vivo Efficacy Study

Cell Proliferation/Viability Assay

Histological Imaging/Staining

PK/PD Analysis

Cell Imaging/Staining

: Exatecan mesylate dihydrate purchased from MedChemExpress. Usage Cited in: Mol Cancer. 2025 Oct 13;24(1):253. [Abstract]; Western blot analysis of B1-5V (BRCA1-) and B2-4V (BRCA2-) cells treated with PBS (NT, no treatment), V66-exatecan (100 nM) ADC for 1-24 h, or V66 alone (24 h). In samples treated with V66-exatecan ADC, a time-dependent accumulation of DNA damage is observed, as indicated by the increased γH2AX and pATM signals, along with a time-dependent down-regulation of TOP1.

: Exatecan mesylate dihydrate purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2023 Sep 5;22(9):1013-1027. [Abstract]; In vivo efficacy of AMT-562, Ab562-T1000-Exatecan (10 mg/kg; i.v.), and P-GGFG-DXd in PC9 xenograft model.

: Exatecan mesylate dihydrate purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2023 Sep 5;22(9):1013-1027. [Abstract]; In vitro cytotoxicity of Exatecan and DXd in HER3-expressing cells. Cells were incubated with a concentration series of Exatecan or DXd for 5 days. Cell viability was measured by CCK-8 and IC50 for each cell line was calculated from cell viability-concentration plot.

: Exatecan mesylate dihydrate purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2023 Sep 5;22(9):1013-1027. [Abstract]; Representative hematoxylin and eosin staining of toxicity organs of AMT-562 and Ab562-T1000-Exatecan (ADC; 30 mg/kg; i.v.). Scale bar, 200 mm.

: Exatecan mesylate dihydrate purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2023 Sep 5;22(9):1013-1027. [Abstract]; Single dose pharmacokinetic profiles of AMT-562 (ADC) and Ab562-GGFG-DXd in mice. ADCs were intravenously administered to mice at the dose of 10 mg/kg.

: Exatecan mesylate dihydrate purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2023 Sep 5;22(9):1013-1027. [Abstract]; Patient-derived colon cancer organoids response to AMT-562 (ADC) and P-GGFG-DXd. Representative images of brightfield (left) and live/dead cells (right) for CO117 was shown. Colon cancer PDOs were treated with AMT-562 or P-GGFG-DXd at a serial concentration for 6 days. Live cells were stained by Calcein AM (green) and dead cells by PI (red).

: Exatecan mesylate dihydrate purchased from MedChemExpress. Usage Cited in: Pharmaceuticals (Basel). 2021 Mar 9;14(3):247. [Abstract]; Tra-Exa-PSAR10 and Tra-Exa-PSAR0 (0.01-10 nM, 6 days). In vitro cytotoxicity of ADCs in breast and gastric HER2+ and HER2- (MCF-7) cancer cell lines after 6-day exposure to trastuzumab conjugates, as assayed by MTT assay, n = 3.

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Topoisomerase Topo I Topo II DNA gyrase

Actividad biológica
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Descripciòn

Exatecan (DX-8951) mesylate dihydrate is a DNA topoisomerase I inhibitor, with an IC₅₀ of 2.2 μM (0.975 μg/mL), and can be used in cancer research^[1]^[2]^[3].

IC₅₀ & Target

Camptothecins

Cellular Effect

Cell Line	Type	Value	Description	References
A549	GI₅₀	0.914 14 Compound: 42; DX-8951f	Growth inhibition of human A549 cells incubated for 72 hrs by MTT assay Growth inhibition of human A549 cells incubated for 72 hrs by MTT assay	[PMID: 38421819]
HCT-116	GI₅₀	0.347 14 Compound: 42; DX-8951f	Growth inhibition of human HCT-116 cells incubated for 72 hrs by MTT assay Growth inhibition of human HCT-116 cells incubated for 72 hrs by MTT assay	[PMID: 38421819]
K562	GI₅₀	10.4 14 Compound: 42; DX-8951f	Growth inhibition of human K562 cells incubated for 72 hrs by MTT assay Growth inhibition of human K562 cells incubated for 72 hrs by MTT assay	[PMID: 38421819]
MCF7	GI₅₀	0.322 14 Compound: 42; DX-8951f	Growth inhibition of human MCF7 cells incubated for 72 hrs by MTT assay Growth inhibition of human MCF7 cells incubated for 72 hrs by MTT assay	[PMID: 38421819]

Peso molecular

567.58

Fòrmula

C₂₄H₂₂FN₃O₄S.CH₄O₃S.2H₂O

No. CAS

197720-53-9

SMILES

CS(=O)(O)=O.N[C@@H]1C2=C3C(C(N4C3)=CC([C@](O)(C(OC5)=O)CC)=C5C4=O)=NC6=CC(F)=C(C)C(CC1)=C62.O.O

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[1]. Mitsui I, et al. A new water-soluble camptothecin derivative, DX-8951f, exhibits potent antitumor activity against human tumors in vitro and in vivo. Jpn J Cancer Res. 1995 Aug;86(8):776-82. [Content Brief]

[2]. Sun FX, et al. Efficacy of camptothecin analog DX-8951f (Exatecan Mesylate) on human pancreatic cancer in an orthotopic metastatic model. Cancer Res. 2003 Jan 1;63(1):80-5. [Content Brief]

[3]. Joto N, et al. DX-8951f, a water-soluble camptothecin analog, exhibits potent antitumor activity against a human lung cancer cell line and its SN-38-resistant variant. Int J Cancer. 1997 Aug 7;72(4):680-6. [Content Brief]

Exatecan mesylate dihydrate Related Classifications

Calculadora de molaridad
Calculadora de dilución

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Exatecan mesylate dihydrate197720-53-9DX-8951 mesylate dihydrateADC PayloadTopoisomeraseADC CytotoxinInhibitorinhibitorinhibit

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