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Cat. No.: HY-13631U

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Exatecan hydrochloride

(Synonyms: DX-8951 hydrochloride)

7 Cited Publications

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Based on 7 publication(s) in Google Scholar

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

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

CAS No.: 144008-87-7
Formule: C₂₄H₂₃ClFN₃O₄
Masse moléculaire:471.91

Stockage:

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

Data Sheet (278 KB)

Exatecan hydrochloride Chemical Structure

CAS No.: 144008-87-7

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Activité biologique
- Description
- IC₅₀ & Target
Chemical Information
Publications (7)
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
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Activité biologique

Description

Exatecan (DX-8951) hydrochloride 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^[1]

Topoisomerase I

2.2 μM (IC₅₀)

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Chemical Information

CAS No. 144008-87-7
Masse moléculaire 471.91
Formule C₂₄H₂₃ClFN₃O₄
SMILES

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

DX-8951 hydrochloride
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Publications (7)

All In Vivo Efficacy StudyCell Proliferation/Viability AssayHistological Imaging/StainingPK/PD AnalysisCell Imaging/Staining

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Journal Impact Factor

Cancer Res

Radiation-Triggered Payload Release Enhances Bispecific Antibody Efficacy. [Abstract]

2025 Oct 9. PMID: 41066595
Acta Pharmacol Sin

HER3 upregulation reduces DS-8201 sensitivity in HER2-positive tumor cells by ATR/CHK1/FoxO1 signaling cascade. [Abstract]

2025 Sep 10. PMID: 40931042
Mol Cancer Ther

AMT-562, a Novel HER3-targeting Antibody-Drug Conjugate, Demonstrates a Potential to Broaden Therapeutic Opportunities for HER3-expressing Tumors. [Abstract]

2023 Sep 5;22(9):1013-1027. PMID: 37302522

Exatecan hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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).
Cornell University

2025.
Cornell University

2025.
Research Square Preprint

2024 Nov 06.
Patent

US20240191272A1.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (278 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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]

Calculators

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

Exatecan hydrochloride

7 Cited Publications

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Activité biologique
- Description
- IC₅₀ & Target
Chemical Information
Publications (7)
Pureté et documentation
Références

1/16
1/16

Exatecan hydrochloride purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2023 Sep 5;22(9):1013-1027. [Abstract]

Customer Validation
In vivo efficacy of AMT-562, Ab562-T1000-Exatecan (10 mg/kg; i.v.), and P-GGFG-DXd in PC9 xenograft model.
1/16

Exatecan hydrochloride purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2023 Sep 5;22(9):1013-1027. [Abstract]

Customer Validation
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.
1/16

Exatecan hydrochloride purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2023 Sep 5;22(9):1013-1027. [Abstract]

Customer Validation
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.
1/16

Exatecan hydrochloride purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2023 Sep 5;22(9):1013-1027. [Abstract]

Customer Validation
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.
1/16

Exatecan hydrochloride purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2023 Sep 5;22(9):1013-1027. [Abstract]

Customer Validation
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).

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Exatecan hydrochloride

Publications Citing Use of MedChemExpress (MCE) Exatecan hydrochloride

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Activité biologique

Chemical Information

Publications (7)

Pureté et documentation

Références

Calculators

Help & FAQs

Exatecan hydrochloride Related Classifications

HY-13631U Related Classifications