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Cat. No.: HY-13631U

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Exatecan hydrochloride

Name: Exatecan hydrochloride
Brand: MedChemExpress
SKU: HY-13631U
Availability: PreOrder

(Synonyms: DX-8951 hydrochloride)

7 Cited Publications

Customer Review

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.

For research use only. We do not sell to patients.

CAS No.: 144008-87-7
Formula: C₂₄H₂₃ClFN₃O₄
Molecular Weight:471.91

Storage:

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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Top Publications Citing

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One-stop CDMO Service

One-Stop Platform：From Independent R&D to Pilot-Scale Production

Biological Activity
- Description
- IC₅₀ & Target
Chemical Information
Publications (7)
Protocols (1)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

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)

All ADC Payloads Isoforms :

All Topoisomerase Isoforms :

Chemical Information

CAS No. 144008-87-7
Molecular Weight 471.91
Formula 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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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.

Protocols

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (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)
Handling Instructions (2659 KB)

References

[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

Molarity Calculator

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

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Dilution Calculator

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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.

Bioz

Keywords

Exatecan hydrochloride

7 Cited Publications

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Biological Activity
- Description
- IC₅₀ & Target
Chemical Information
Publications (7)
Protocols
Purity & Documentation
References

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

All ADC Payloads Isoforms

All Topoisomerase Isoforms