(1R,9R)-Exatecan mesylate
Based on 1 Customer Validation
(1R,9R)-Exatecan mesylate ((1R,9R)-DX8951f) is a non-prodrug camptothecin derivative and a potent topoisomerase I inhibitor (IC50=0.975 μg/mL in mice and 0.82 μg/mL in humans). (1R,9R)-Exatecan mesylate blocks enzyme activity and induces apoptosis by stabilizing the enzyme-DNA cleavable complex. (1R,9R)-Exatecan mesylate not only effectively inhibits the proliferation of various malignant tumor cells and tumor growth, but also circumvents P-glycoprotein-mediated multidrug resistance. (1R,9R)-Exatecan mesylate is widely used in preclinical studies of multiple cancers including pancreatic cancer, lung cancer, breast cancer, and leukemia. The low-activity isomer of (1R,9R)-Exatecan mesylate is (1S,9R)-Exatecan mesylate (HY-13631I).
For research use only. We do not sell to patients.
- Purity: 99.49%
- CAS No.: 2938875-39-7
- Formula: C25H26FN3O7S
- Molecular Weight:531.55
-
Storage:
4°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
Bioactive Compound Library Max
HY-L181
-
Bioactive Compound Library
HY-L001
-
Apoptosis Compound Library
HY-L003
-
Cell Cycle/DNA Damage Compound Library
HY-L004
-
Anti-Cancer Compound Library
HY-L025
-
Anti-Aging Compound Library
HY-L034
-
Anti-Lung Cancer Compound Library
HY-L075
-
Cell Death Library
HY-L162
-
Anti-Drug-Resistant Compound Library
HY-L169
-
MCE Bioactive Compound Library
HY-L001V
-
Protein Kinase Compound Library
HY-L196
-
Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
-
High-Throughput Bioactive Compound Library
HY-L205
All Topoisomerase Isoforms
More
Biological Activity
|
Camptothecins |
(1R,9R)-Exatecan mesylate potently inhibits the growth of SUIT-2 and KP-1N human pancreatic cancer cell lines in vitro, with 48 h IC50 values of 0.079 ng/mL and 0.12 ng/mL, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
(1R,9R)-Exatecan (mesylate) (18.75 mg/kg; i.v.; once every 4 days; 4 doses) achieves a 72% tumor growth inhibition rate against CPT-11-resistant SUIT-2/CPT-11 pancreatic cancer xenografts in nude mice at its maximum tolerable dose[1].
(1R,9R)-Exatecan (mesylate) (2.5-10 mg/kg; i.v.; once every 5 days; 4 doses) dose-dependently inhibits liver metastasis of SUIT-2 pancreatic cancer in nude mice, achieving a 78% liver tumor growth score inhibition rate and 100% ascites inhibition at a total dose of 40 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:BALB/c-nu/nu (male, 6 weeks old, subcutaneous xenograft of human pancreatic carcinoma SUIT-2 cells)[1]
-
Dosage:3.125 mg/kg (total 12.5 mg/kg); 6.25 mg/kg (total 25 mg/kg); 12.5 mg/kg (total 50 mg/kg); 18.75 mg/kg (total 75 mg/kg)
-
Administration:i.v.; once every 4 days; 4 doses
-
Result:Achieved a 79% tumor growth inhibition rate with mean tumor weight of 0.154 ± 0.027 g at total dose 75 mg/kg.
Achieved a 68% tumor growth inhibition rate with mean tumor weight of 0.236 ± 0.100 g at total dose 50 mg/kg.
Achieved a 78% tumor growth inhibition rate with mean tumor weight of 0.164 ± 0.053 g at total dose 25 mg/kg.
Achieved a 68% tumor growth inhibition rate with mean tumor weight of 0.235 ± 0.057 g at total dose 12.5 mg/kg.
Caused no body weight loss in any treated group.
-
Animal Model:BALB/c-nu/nu (male, 6 weeks old, subcutaneous xenograft of CPT-11-resistant human pancreatic carcinoma SUIT-2/CPT-11 cells)[1]
-
Dosage:3.125 mg/kg (total 12.5 mg/kg); 6.25 mg/kg (total 25 mg/kg); 12.5 mg/kg (total 50 mg/kg); 18.75 mg/kg (total 75 mg/kg)
-
Administration:i.v.; once every 4 days; 4 doses
-
Result:Achieved a 72% tumor growth inhibition rate with mean tumor weight of 0.250 ± 0.061 g at total dose 75 mg/kg; caused maximum body weight loss of 14.6% on day 31.
Achieved a 33% tumor growth inhibition rate with mean tumor weight of 0.595 ± 0.130 g at total dose 50 mg/kg; caused maximum body weight loss of 6.1% on day 21.
Achieved a 13% tumor growth inhibition rate with mean tumor weight of 0.776 ± 0.157 g at total dose 25 mg/kg; caused maximum body weight loss of 8.7% on day 15.
Achieved a 20% tumor growth inhibition rate with mean tumor weight of 0.712 ± 0.065 g at total dose 12.5 mg/kg; caused maximum body weight loss of 3.2% on day 15.
Caused no treatment-related deaths in any group.
-
Animal Model:BALB/c-nu/nu (male, 6 weeks old, liver metastasis model via intrasplenic injection of human pancreatic carcinoma SUIT-2 cells)[1]
-
Dosage:2.5 mg/kg (total 10 mg/kg); 5 mg/kg (total 20 mg/kg); 10 mg/kg (total 40 mg/kg)
-
Administration:i.v.; once every 5 days; 4 doses
-
Result:Achieved a 78% liver tumor growth score inhibition rate with mean liver tumor growth score of 0.7 ± 0.9, 3/7 liver tumor incidence, mean liver weight of 1.594 ± 0.154 g, 2/7 spleen tumor incidence, 100% ascites inhibition with 0.0 ± 0.0 mL ascites volume, 0/7 ascites incidence, and 3/7 tumor-free mice at total dose 40 mg/kg.
Achieved a 69% liver tumor growth score inhibition rate with mean liver tumor growth score of 1.0 ± 0.6, 5/6 liver tumor incidence, mean liver weight of 1.594 ± 0.163 g, 2/6 spleen tumor incidence, 100% ascites inhibition with 0.0 ± 0.0 mL ascites volume, 0/6 ascites incidence, and 1/6 tumor-free mice at total dose 20 mg/kg.
Achieved a 28% liver tumor growth score inhibition rate with mean liver tumor growth score of 2.3 ± 1.1, 6/6 liver tumor incidence, mean liver weight of 1.780 ± 0.197 g, 3/6 spleen tumor incidence, 97% ascites inhibition with 0.1 ± 0.1 mL ascites volume, and 2/6 ascites incidence at total dose 10 mg/kg.
Chemical Information
-
CAS No. 2938875-39-7
-
Appearance Solid
-
Molecular Weight 531.55
-
Formula C25H26FN3O7S
-
Color Gray to brown
-
SMILES
O=S(C)(O)=O.O=C1[C@@](O)(CC)C2=C(CO1)C(N3CC4=C5C6=C(CC[C@H]5N)C(C)=C(F)C=C6N=C4C3=C2)=O
-
Synonyms
(1R,9R)-DX8951f
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
Solvent & Solubility
DMSO : 16.67 mg/mL (31.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
-
Data Sheet (286 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Handling Instructions (2659 KB)
References
[1]. Takiguchi S, et al. Antitumor effect of DX-8951, a novel camptothecin analog, on human pancreatic tumor cells and their CPT-11-resistant variants cultured in vitro and xenografted into nude mice. Jpn J Cancer Res. 1997;88(8):760-769. [Content Brief]
[2]. 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;86(8):776-782. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8813 mL | 9.4065 mL | 18.8129 mL | 47.0323 mL |
| 5 mM | 0.3763 mL | 1.8813 mL | 3.7626 mL | 9.4065 mL | |
| 10 mM | 0.1881 mL | 0.9406 mL | 1.8813 mL | 4.7032 mL | |
| 15 mM | 0.1254 mL | 0.6271 mL | 1.2542 mL | 3.1355 mL | |
| 20 mM | 0.0941 mL | 0.4703 mL | 0.9406 mL | 2.3516 mL | |
| 25 mM | 0.0753 mL | 0.3763 mL | 0.7525 mL | 1.8813 mL | |
| 30 mM | 0.0627 mL | 0.3135 mL | 0.6271 mL | 1.5677 mL |
(1R,9R)-Exatecan mesylate Related Classifications
HY-13631J Related Classifications
Powered by Bioz