Sabarubicin hydrochloride
Sabarubicin hydrochloride (MEN 10755 hydrochloride) is a disaccharide analog of Doxorubicin (HY-15142A). Sabarubicin hydrochloride stimulates topoisomerase II-mediated DNA cleavage, induces DNA strand breaks and Apoptosis. Sabarubicin hydrochloride binds to and stabilizes telomeric G-quadruplex DNA. Sabarubicin hydrochloride is applicable to research related to ovarian tumors, breast cancer and lung cancer.
For research use only. We do not sell to patients.
- CAS No.: 169317-77-5
- Formula: C32H38ClNO13
- Molecular Weight:680.10
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Sabarubicin (1 h exposure; 72 h incubation post-treatment) hydrochloride inhibits the growth of A2780 ovarian tumor cells with an IC50 of 0.39 μM[1].
Sabarubicin (1-5 μM; 1 h) hydrochloride induces single-strand DNA breaks in A2780 ovarian tumor cells: after 1 h of exposure to 1 μM of this drug, the damage level reaches 230 rad-equivalent; after 1 h of exposure to 5 μM of this drug, the damage level reaches 367 rad-equivalents, and its damage degree is comparable to that of doxorubicin at lower intracellular concentrations[1].
Sabarubicin (24 h) hydrochloride potently inhibits the growth of non-small cell lung cancer H460 cells, with an IC50 value of 0.076 μM[2].
Sabarubicin (24 h) hydrochloride potently inhibits the growth of small cell lung cancer GLC4 cells, with an IC50 value of 0.036 μM[2].
Sabarubicin (1-5 μM; 1 h) hydrochloride accumulates in A2780 ovarian tumor cells, reaching an accumulation level of 27 pmol/106 cells after treatment at 1 μM for 1 hour and 159 pmol/106 cells after treatment at 5 μM for 1 hour[1].
Sabarubicin hydrochloride binds to the telomeric 21-mer G-quadruplex DNA, forming non-fluorescent 1:1 and 2:1 complexes with binding constants of log (K11/M-1) = 5.78 and log (K21/M-2) = 11.48[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Sabarubicin (4 mg/kg; i.v.; every 4 days; 5 doses) hydrochloride achieves 80% tumour volume inhibition and a 0.8 Log Cell Kill in H460 non-small cell lung carcinoma xenografts in female nude mice[2].
Sabarubicin (6 mg/kg; i.v.; every 4 days; 5 doses) hydrochloride achieves 75% tumour volume inhibition and a 1.2 Log Cell Kill in GLC4 small-cell lung carcinoma xenografts in female nude mice[2].
Sabarubicin (6 mg/kg; i.v.; every 3 or 4 days; five injections) hydrochloride achieves 96% tumor volume inhibition and a log10 cell kill of 2.2, and induces significantly higher early apoptosis than Doxorubicin (HY-15142A) in MX-1 human breast carcinoma xenografts in athymic Swiss nude mice[1].
Sabarubicin (hydrochloride) (6 mg/kg; i.v.; every 3 or 4 days; five injections) achieves 91% tumor volume inhibition in POVD human small-cell lung cancer xenografts in athymic Swiss nude mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Athymic Swiss nude mice (10-12 weeks old)[1]
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Dosage:6 mg/kg
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Administration:i.v.; every 3 or 4 days; five injections
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Result:Achieved 99% tumor volume inhibition.
Reached a log10 cell kill value greater than 6.
Showed statistically different tumor volumes from doxorubicin-treated mice (P<.05).
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Animal Model:Athymic Swiss nude mice (10-12 weeks old)[1]
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Dosage:6 mg/kg
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Administration:i.v.; every 3 or 4 days; five injections
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Result:Achieved 96% tumor volume inhibition.
Reached a log10 cell kill value of 2.2.
Showed statistically different tumor volumes from doxorubicin-treated mice (P<.0001).
Induced a high apoptotic index as early as 1 day after the last treatment, with values notably higher than doxorubicin at all time points (e.g., ~6% apoptotic index at day 1, compared to ~1% for doxorubicin).
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Animal Model:Athymic Swiss nude mice (10-12 weeks old)[1]
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Dosage:6 mg/kg
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Administration:i.v.; every 3 or 4 days; five injections
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Result:Achieved 91% tumor volume inhibition.
Reached a log10 cell kill value of 1.9.
Showed statistically different tumor volumes from doxorubicin-treated mice (P<.005).
Induced a high apoptotic index at all time points, with values notably higher than doxorubicin (e.g., ~5.5% apoptotic index at day 3, compared to ~3% for doxorubicin).
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Animal Model:nude mice (female)[2]
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Dosage:4 mg/kg
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Administration:i.v.; every 4 days; 5 doses
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Result:Achieved a tumour volume inhibition (TVI%) of 80%.
Achieved a Log Cell Kill (LCK) of 0.8.
Resulted in 0 toxic deaths (0/5 mice).
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Animal Model:nude mice (female)[2]
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Dosage:6 mg/kg
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Administration:i.v.; every 4 days; 5 doses
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Result:Achieved a tumour volume inhibition (TVI%) of 75%.
Achieved a Log Cell Kill (LCK) of 1.2.
Resulted in 0 toxic deaths (0/5 mice).
Chemical Information
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CAS No. 169317-77-5
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Molecular Weight 680.10
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Formula C32H38ClNO13
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SMILES
OC1=C2C(C(C3=CC=CC=C3C2=O)=O)=C(O)C([C@H]4O[C@H]5C[C@@H]([C@@H]([C@@H](O5)C)O[C@H]6C[C@@H]([C@@H]([C@@H](O6)C)O)N)O)=C1C[C@](O)(C4)C(CO)=O.Cl
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Synonyms
MEN 10755 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Arcamone F, et al. Doxorubicin disaccharide analogue: apoptosis-related improvement of efficacy in vivo. Journal of the National Cancer Institute. 1997 Aug 20;89(16):1217-23. [Content Brief]
[2]. Bigioni M, et al. Antitumour effect of combination treatment with Sabarubicin (MEN 10755) and cis-platin (DDP) in human lung tumour xenograft. Cancer chemotherapy and pharmacology. 2008 Sep;62(4):621-9. [Content Brief]
[3]. Mazzini S, et al. Interaction between double helix DNA fragments and the new antitumor agent sabarubicin, Men10755. Bioorganic & medicinal chemistry. 2010 Feb 15;18(4):1497-506. [Content Brief]
[4]. Manet I, et al. Affinity of the anthracycline antitumor drugs Doxorubicin and Sabarubicin for human telomeric G-quadruplex structures. Physical chemistry chemical physics : PCCP. 2011 Jan 14;13(2):540-51. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Sabarubicin hydrochloride Related Classifications
HY-13745A Related Classifications
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- Sabarubicin
- 169317-77-5
- MEN 10755
- MEN10755
- MEN-10755
- Drug Derivative
- DNA/RNA Synthesis
- DNA Alkylator/Crosslinker
- Apoptosis
- G-quadruplex
- topoisomerase II
- lung cancer
- ovarian tumors
- DNA intercalator
- human non-small cell lung carcinoma H460 cells
- human A2780 ovarian tumor cells
- apoptosis
- human telomeric G-quadruplex DNA
- human small-cell lung carcinoma GLC4 cells
- breast carcinoma
- Inhibitor
- inhibitor
- inhibit