2. Others Cell Cycle/DNA Damage Apoptosis
  3. Drug Derivative Topoisomerase Apoptosis
  4. (1R,9R)-Exatecan mesylate

(1R,9R)-Exatecan mesylate  (Synonyms: (1R,9R)-DX8951f)

Cat. No.: HY-13631J Purity: 99.49% ee.: 99.96%
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(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.

(1R,9R)-Exatecan mesylate

(1R,9R)-Exatecan mesylate Chemical Structure

CAS No. : 2938875-39-7

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(1R,9R)-Exatecan mesylate Related Antibodies

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Description

(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[1][2]. The low-activity isomer of (1R,9R)-Exatecan mesylate is (1S,9R)-Exatecan mesylate (HY-13631I).
IC50 & Target

Camptothecins

 

In Vitro

(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 Related Antibodies
In Vivo

(1R,9R)-Exatecan (mesylate) (3.125-18.75 mg/kg; i.v.; once every 4 days; 4 doses) exhibits potent dose-dependent antitumor activity against SUIT-2 pancreatic cancer xenografts in nude mice, with tumor growth inhibition rates ranging from 68% to 79% across tested doses[1].
(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.
Molecular Weight

531.55

Formula

C25H26FN3O7S
CAS No.
Appearance

Solid

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
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
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8813 mL 9.4065 mL 18.8129 mL
5 mM 0.3763 mL 1.8813 mL 3.7626 mL
View the 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.

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In Vivo Dissolution Calculator
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Purity & Documentation
References

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
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(1R,9R)-Exatecan mesylate Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

(1R,9R)-Exatecan2938875-39-7(1R,9R)-DX8951fDrug DerivativeTopoisomeraseApoptosisDrug derivativeovarian cancerpancreatic cancergastric adenocarcinomanon-small cell lung cancersmall cell lung cancerP-glycoproteincolon cancerbreast cancertopoisomerase IapoptosisInhibitorinhibitorinhibit

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