(1R,9R)-Exatecan
(1R,9R)-Exatecan ((1R,9R)-DX8951f) is a non-prodrug Camptothecin (HY-16560) derivative and a potent topoisomerase I (Topo I) inhibitor (IC50=0.975 μg/mL in mice and 0.82 μg/mL in humans). (1R,9R)-Exatecan blocks enzyme activity and induces apoptosis by stabilizing the enzyme-DNA cleavable complex. (1R,9R)-Exatecan 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 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 is (1S,9R)-Exatecan (HY-13631I).
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- CAS No.: 2489613-15-0
- Formule: C24H22FN3O4
- Masse moléculaire:435.45
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
Description
IC50 & Target
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Camptothecins |
In Vitro
(1R,9R)-Exatecan 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.
In Vivo
(1R,9R)-Exatecan (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 (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.
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Animal Model:BALB/c-nu/nu (male, 6 weeks old, subcutaneous xenograft of human pancreatic carcinoma SUIT-2 cells)[1]
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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)
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Administration:i.v.; once every 4 days; 4 doses
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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.
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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]
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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)
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Administration:i.v.; once every 4 days; 4 doses
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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.
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Animal Model:BALB/c-nu/nu (male, 6 weeks old, liver metastasis model via intrasplenic injection of human pancreatic carcinoma SUIT-2 cells)[1]
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Dosage:2.5 mg/kg (total 10 mg/kg); 5 mg/kg (total 20 mg/kg); 10 mg/kg (total 40 mg/kg)
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Administration:i.v.; once every 5 days; 4 doses
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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
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CAS No. 2489613-15-0
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Masse moléculaire 435.45
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Formule C24H22FN3O4
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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
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Synonyms
(1R,9R)-DX-8951
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
(1R,9R)-Exatecan Related Classifications
HY-13631V Related Classifications
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