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Exatecan

Catalog No. T11249 CAS 171335-80-1

Synonyms: DX-8951, DX-8951f

Exatecan (DX-8951f) is a DNA topoisomerase I (TOP1) inhibitor with an IC50 value of 2.2 μM (0.975 μg/mL).Exatecan has antitumor activity and may be used in cancer research.

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Exatecan, CAS 171335-80-1

Pack Size	Availability	Price/USD
10 mg	In stock	$ 30.00
25 mg	In stock	$ 64.00
50 mg	In stock	$ 93.00
100 mg	In stock	$ 138.00
500 mg	In stock	$ 339.00

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Purity: 99.69%

Purity: 99.64%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Exatecan (DX-8951f) is a DNA topoisomerase I (TOP1) inhibitor with an IC50 value of 2.2 μM (0.975 μg/mL).Exatecan has antitumor activity and may be used in cancer research.
Targets&IC50	Topo I:2.2 μM
In vitro	Exatecan (DX-8951f) displays cytotoxic activities against PC-6, and PC-6/SN2-5 cells, with mean GI50s of 0.186 and 0.395 ng/mL, respectively.[2] Exatecan (34 nM) stabilizes DNA-TopoI complexes in PC-6 and PC-6/SN2-5 cells.[2] Exatecan is a potent topoisomerase I inhibitor, with an IC50 of 0.975 μg/mL.[2] Exatecan significantly inhibits the proliferation of several cancer cell lines, with mean GI50s of 2.02 ng/mL, 2.92 ng/mL, 1.53 ng/mL, and 0.877 ng/mL for breast cancer cells, colon cancer cells, stomach cancer cells, and lung cancer cells, respectively.[2]
In vivo	Exatecan (DX-8951f) (3.325-50 mg/kg; i.v.) exhibits antitumor activities in the mice model bearing tumor cells, without toxic death.[3] Exatecan (15, 25 mg/kg; i.v.) highly inhibits MIA-PaCa, BxPC-3 primary tumor growth in the MIA-PaCa-2 early-stage model and early-stage model of BxPC-3. Exatecan also significantly suppresses BxPC-3 lymphatic metastasis and completely eliminates lung metastasis in the BxPC-3 late-stage cancer model.[3]

Synonyms	DX-8951, DX-8951f
Molecular Weight	435.45
Formula	C24H22FN3O4
CAS No.	171335-80-1

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 21.77 mg/mL (50 mM), Sonication is recommended.

References and Literature

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. 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. 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.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Anti-Cancer Approved Drug Library Bioactive Compounds Library Max FDA-Approved & Pharmacopeia Drug Library Approved Drug Library Bioactive Compound Library

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Related compounds with same targets

Irinotecan Aldoxorubicin hydrochloride Rubicordifolin Lucidin primeveroside (±)-10-Hydroxycamptothecin CH-0793076 AuM1Gly Topoisomerase II inhibitor 14

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Exatecan 171335-80-1 DNA Damage/DNA Repair Topoisomerase DX8951 DX-8951 DX 8951 DX-8951f inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.