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  3. Drug Derivative Topoisomerase Apoptosis
  4. (1S,9R)-Exatecan mesylate

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

Cat. No.: HY-13631I Purity: 99.11%
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(1S,9R)-Exatecan mesylate ((1S,9R)-DX8951f) is a non-prodrug camptothecin derivative and a topoisomerase I inhibitor (IC50=0.975 μg/mL in mice and 0.82 μg/mL in humans). (1S,9R)-Exatecan mesylate blocks enzyme activity and induces apoptosis by stabilizing the enzyme-DNA cleavable complex. (1S,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. (1S,9R)-Exatecan mesylate is widely used in preclinical studies of various cancers such as pancreatic cancer, lung cancer, breast cancer, and leukemia.
The chiral isomer of (1S,9R)-Exatecan mesylate is (1R,9R)-Exatecan mesylate (HY-13631J).

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(1S,9R)-Exatecan mesylate

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

CAS No. : 2938875-54-6

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Based on 1 publication(s) in Google Scholar

Other Forms of (1S,9R)-Exatecan mesylate:

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

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Description

(1S,9R)-Exatecan mesylate ((1S,9R)-DX8951f) is a non-prodrug camptothecin derivative and a topoisomerase I inhibitor (IC50=0.975 μg/mL in mice and 0.82 μg/mL in humans). (1S,9R)-Exatecan mesylate blocks enzyme activity and induces apoptosis by stabilizing the enzyme-DNA cleavable complex. (1S,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. (1S,9R)-Exatecan mesylate is widely used in preclinical studies of various cancers such as pancreatic cancer, lung cancer, breast cancer, and leukemia[1][2].
The chiral isomer of (1S,9R)-Exatecan mesylate is (1R,9R)-Exatecan mesylate (HY-13631J).

IC50 & Target

Camptothecins

 

In Vitro

(1S,9R)-Exatecan (mesylate) (48 h exposure; additional 5 days culture post-exposure) and its hydrochloride form (DX-8951a) potently inhibit the growth of SUIT-2, KP-1N, SUIT-2/CPT-11, and KP-1N/CPT-11 human pancreatic carcinoma cells in vitro with IC50 values ranging from 0.079 to 0.69 ng/mL, and show lower cross-resistance in CPT-11-resistant cell lines compared to other camptothecin analogs[1].
(1S,9R)-Exatecan (mesylate) (0.16-10 μg/mL; 10 min at 37°C) (tested as DX-8951a) inhibits topoisomerase I activity from SUIT-2 human pancreatic carcinoma cells with an IC50 of 0.82 μg/mL, showing 2.8-fold stronger inhibition than SN-38[1].
(1S,9R)-Exatecan (mesylate) (0.8-500 ng/mL; 24 h) (tested as DX-8951a) dose-dependently induces DNA fragmentation, a marker of apoptosis, in SUIT-2 human pancreatic carcinoma cells, with 60% fragmentation observed at 20 ng/mL after 24 h of incubation, and is more potent than SN-38[1].
(1S,9R)-Exatecan (mesylate) (0.05 μg/mL; 24 h) (tested as DX-8951a) induces morphological features of apoptotic cell death, including chromatin condensation, nuclear fragmentation, and cytoplasmic vacuolation, in SUIT-2 human pancreatic carcinoma cells after 24 h of incubation[1].
(1S,9R)-Exatecan (mesylate) (Doses yielding GI50 values; 3 days post-drug addition) potently inhibits the proliferation of 31 human cancer cell lines and mouse leukemia P388 cells, with an overall mean GI50 of 2.09 ng/mL, and shows greater potency than comparison compounds[2].
(1S,9R)-Exatecan (mesylate) (Doses yielding IC50 values) potently inhibits P388 cell-derived topoisomerase I activity with an IC50 of 0.975 μg/mL, and is more potent than comparison compounds[2].
(1S,9R)-Exatecan (mesylate) (Doses yielding GI50 values; 3 days post-drug addition) retains potent cytotoxic activity against P-glycoprotein-overexpressing PC-6/VCR cells, overcoming P-glycoprotein-mediated multidrug resistance[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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

Apoptosis Analysis[1]

Cell Line: SUIT-2
Concentration: 0.8-500 ng/mL
Incubation Time: 24 h
Result: Induced DNA fragmentation in a dose-dependent manner.
Caused approximately 60% DNA fragmentation at 20 ng/mL.
Achieved equivalent fragmentation at a 5-times lower concentration than SN-38.

Cell Cytotoxicity Assay[2]

Cell Line: 31 human cancer cell lines (breast, colon, stomach, lung, ovarian, leukemia) and mouse leukemia P388 cells
Concentration: Doses yielding GI50 values
Incubation Time: 3 days post-drug addition
Result: Exhibited strong antiproliferative activity with mean GI50 values of 2.02 ng/mL against breast cancer cell lines, 2.92 ng/mL against colon cancer cell lines, 1.53 ng/mL against stomach cancer cell lines, 0.877 ng/mL against lung cancer cell lines, and 4.33 ng/mL against other cell lines including ovarian cancer, human leukemia, and mouse leukemia.
Achieved an overall mean GI50 value of 2.09 ng/mL across all 32 cell lines.

Cell Cytotoxicity Assay[2]

Cell Line: Human non-small cell lung cancer PC-6 cells and its P-glycoprotein-overexpressing variant PC-6/VCR cells
Concentration: Doses yielding GI50 values; 5 μg/mL verapamil (co-treatment with PC-6/VCR cells)
Incubation Time: 3 days post-drug addition
Result: Achieved GI50 values of 0.0896 ng/mL for PC-6 cells and 0.0690 ng/mL for PC-6/VCR cells (without verapamil, first set), with a degree of resistance of 0.8.
Achieved GI50 values of 0.179 ng/mL for PC-6 cells and 0.182 ng/mL for PC-6/VCR cells (without verapamil, second set), with a degree of resistance of 1.0.
Reduced the GI50 value of PC-6/VCR cells to 0.156 ng/mL (with 5 μg/mL verapamil), with a VR (+)/VR (−) ratio of 0.86.
In Vivo

(1S,9R)-Exatecan (mesylate) (3.125-18.75 mg/kg; i.v.; every 4 days; 4 doses) produces statistically significant tumor growth inhibition of 68% to 79% against SUIT-2 pancreatic cancer xenografts in nude mice across a wide dose range, with no associated body weight loss or toxicity-related mortality[1].
(1S,9R)-Exatecan (mesylate) (3.125-18.75 mg/kg; i.v.; every 4 days; 4 doses) produces statistically significant tumor growth inhibition of 72% against CPT-11-resistant SUIT-2/CPT-11 pancreatic cancer xenografts in nude mice at its maximum tolerable dose, with transient body weight loss and no toxicity-related mortality[1].
(1S,9R)-Exatecan (mesylate) (2.5-10 mg/kg; i.v.; every 5 days; 4 doses) produces dose-dependent, statistically significant inhibition of liver metastasis from SUIT-2 pancreatic cancer in nude mice, with 78% liver tumor score inhibition and 3/7 tumor-free mice at the highest tested dose, and no significant body weight loss[1].
(1S,9R)-Exatecan (mesylate) (3.325-50 mg/kg; i.v.; three doses at 4-day intervals) exhibits dose-dependent, potent antitumor activity against human gastric adenocarcinoma SC-6 xenografts in nude mice, with a maximal tumor growth inhibition by weight of 92% at a total i.v. dose of 50 mg/kg (three doses at 4-day intervals) without causing toxic deaths[2].

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)[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.; every 4 days; 4 doses
Result: Produced tumor growth inhibition (IR) rates of 68%, 78%, 68%, and 79%, respectively.
Resulted in mean tumor weights of 0.235±0.057 g, 0.164±0.053 g, 0.236±0.100 g, and 0.154±0.027 g, respectively.
Caused no body weight loss in any treated group, and no mice died of toxicity.\nAt total dose of 75 mg/kg, produced a tumor growth inhibition (IR) rate of 72% with a mean tumor weight of 0.250±0.061 g; caused maximum body weight loss of 14.6% on day 31.
At total doses of 50 mg/kg, 25 mg/kg, and 12.5 mg/kg, resulted in IR rates of 33%, 13%, and 20% with mean tumor weights of 0.595±0.130 g, 0.776±0.157 g, and 0.712±0.065 g, respectively; caused maximum body weight loss of 6.1% (day 21), 8.7% (day 15), and 3.2% (day 15), respectively.
Caused no mice to die of toxicity in any treated group.
Animal Model: BALB/c-nu/nu (male, 6 weeks old)[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.; every 5 days; 4 doses
Result: At total dose of 40 mg/kg, produced a liver tumor growth score inhibition rate of 78%, with a mean liver tumor score of 0.7±0.9, mean liver weight of 1.594±0.154 g, and 3/7 mice with no visible liver tumor nodules; found 2/7 mice with visible spleen tumor nodules, and 0/7 mice with ascites, with 3/7 mice being tumor-free.
At total dose of 20 mg/kg, resulted in a liver tumor growth score inhibition rate of 69%, with a mean liver tumor score of 1.0±0.6, mean liver weight of 1.594±0.163 g, 5/6 mice with liver tumor nodules, 2/6 mice with spleen tumor nodules, 0/6 mice with ascites, and 1/6 mice tumor-free.
At total dose of 10 mg/kg, resulted in a liver tumor growth score inhibition rate of 28%, with a mean liver tumor score of 2.3±1.1, mean liver weight of 1.780±0.197 g, 6/6 mice with liver tumor nodules, 3/6 mice with spleen tumor nodules, 2/6 mice with ascites (mean volume 0.1±0.1 mL, 97% inhibition), and 0/6 mice tumor-free.
Caused no significant body weight loss.
Animal Model: BALB/c-nu/nu (male, 5 or 6 weeks old, human gastric adenocarcinoma SC-6 cells transplanted s.c.)[2]
Dosage: 3.325 mg/kg; 6.25 mg/kg; 12.5 mg/kg; 25 mg/kg; 50 mg/kg
Administration: i.v.; three doses at 4-day intervals
Result: Achieved 54% maximal tumor growth inhibition by volume (day 12) and 43% tumor growth inhibition by weight at total dose 3.325 mg/kg, with 3.8% maximal body weight reduction (day 6) and 0 toxic deaths.
Achieved 72% maximal tumor growth inhibition by volume (day 14) and 58% statistically significant tumor growth inhibition by weight at total dose 6.25 mg/kg, with 2.6% maximal body weight reduction (day 6) and 0 toxic deaths.
Achieved 82% maximal tumor growth inhibition by volume (day 17) and 73% statistically significant tumor growth inhibition by weight at total dose 12.5 mg/kg, with 5.9% maximal body weight reduction (day 6) and 0 toxic deaths.
Achieved 95% maximal tumor growth inhibition by volume (day 17) and 90% statistically significant tumor growth inhibition by weight at total dose 25 mg/kg, with 7.0% maximal body weight reduction (day 6) and 0 toxic deaths.
Achieved 96% maximal tumor growth inhibition by volume (day 17) and 92% statistically significant tumor growth inhibition by weight at total dose 50 mg/kg, with 12.5% maximal body weight reduction (day 12) and 0 toxic deaths.
Molecular Weight

531.55

Formula

C25H26FN3O7S
CAS No.
Appearance

Solid

Color

White to yellow

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
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Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (94.06 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 (sealed storage, away from moisture and light). 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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Purity & Documentation

Purity: 99.11%

SDS (396 KB)

COA (261 KB) HNMR (342 KB) RP-HPLC (553 KB)

Handling Instructions (2659 KB)
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 (sealed storage, away from moisture and light). 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
40 mM 0.0470 mL 0.2352 mL 0.4703 mL 1.1758 mL
50 mM 0.0376 mL 0.1881 mL 0.3763 mL 0.9406 mL
60 mM 0.0314 mL 0.1568 mL 0.3135 mL 0.7839 mL
80 mM 0.0235 mL 0.1176 mL 0.2352 mL 0.5879 mL
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(1S,9R)-Exatecan mesylate Related Classifications

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Keywords:

(1S,9R)-Exatecan2938875-54-6(1S,9R)-DX8951fDrug DerivativeTopoisomeraseApoptosisDrug derivativexenograft tumorapoptosiscolon cancerpancreatic cancerDNA topoisomerase Ibreast cancermultidrug resistanceP-glycoproteingastric adenocarcinomamalignant cellsInhibitorinhibitorinhibit

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