1. Cell Cycle/DNA Damage
  2. Topoisomerase

Exatecan Mesylate (Synonyms: DX8951f)

Cat. No.: HY-13631A Purity: 98.09%
Data Sheet SDS Handling Instructions

Exatecan Mesylate (DX-8951) is a totally synthetic analogue of the topoisomerase I-inhibitor camptothecin, which was synthesised to impart increased aqueous solubility, greater tumour efficacy, and less toxicity than camptothecin itself.

For research use only. We do not sell to patients.
Exatecan Mesylate Chemical Structure

Exatecan Mesylate Chemical Structure

CAS No. : 169869-90-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 1375 In-stock
1 mg USD 660 In-stock
5 mg USD 1176 In-stock
10 mg USD 1800 In-stock
50 mg   Get quote  
100 mg   Get quote  

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Other Forms of Exatecan Mesylate:

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  • Technical Information

  • Purity & Documentation

  • References

Description

Exatecan Mesylate (DX-8951) is a totally synthetic analogue of the topoisomerase I-inhibitor camptothecin, which was synthesised to impart increased aqueous solubility, greater tumour efficacy, and less toxicity than camptothecin itself. IC50 value: Target: topoisomerase I Exatecan was given as i.v. infusion over 30 min at a dose of 0.5mg/m2 every day for five consecutive days, repeated every 21 days. Seventy-four percentage of cycles could be given without dose or schedule modification. The main toxicity was haematotoxicity with grade 3/4 neutropenia in 49%, grade 3/4 thrombocytopenia in 23%, and grade 3/4 anaemia in 15% of patients, respectively [1]. The most common drug-related toxicity was neutropenia. Non-hematologic toxicities were mostly mild to moderate; the most common were nausea, vomiting and anorexia. Plasma concentrations of DX-8951 (the anhydrous form of DX-8951f) were well described using a linear 2-compartment PK model. All concentrations and dose events were simultaneously modeled and explained by the population PK model. There was no evidence of non-linearity in the elimination PK, auto-inhibition or induction of DX-8951 clearance over the five days of administration [2]. Thirty-one patients were treated with 100 courses of exatecan at 6 dose-schedule levels. The incidence of the principal dose-limiting toxicities, neutropenia and thrombocytopenia, was unacceptably high at exatecan doses exceeding 0.15 mg/m(2)/day as a 21-day CIVI, which was determined to be the MTD for both MP and HP patients [3].

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References
Molecular Weight

531.55

Formula

C₂₅H₂₆FN₃O₇S

CAS No.

169869-90-3

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: 15.3 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 98.09%

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Product Name:
Exatecan Mesylate
Cat. No.:
HY-13631A
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