QBS10072S dihydrochloride
QBS10072S dihydrochloride is a LAT1-selective substrate with blood-brain barrier permeability that inhibits tumor growth. QBS10072S dihydrochloride enters LAT1-expressing tumor cells via LAT1-mediated active transport, induces interstrand DNA cross-linking and cell apoptosis, and reduces leptomeningeal dissemination. QBS10072S dihydrochloride can be used in studies related to glioblastoma multiforme, diffuse intrinsic pontine glioma, triple-negative breast cancer brain metastases, and aggressive T-cell lymphoma.
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- CAS No.: 1802735-31-4
- Formule: C15H24Cl4N2O2
- Masse moléculaire:406.18
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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
QBS10072S dihydrochloride induces significant cytotoxicity in LAT1-expressing GBM cell lines (including those with high and low MGMT expression) and minimal cytotoxicity in LAT1-negative normal human astrocytes[1].
QBS10072S dihydrochloride is preferentially cytotoxic to human TNBC cell lines (MDA-MB-157, MDA-MB-468, HCC1806, DU4475, MDA-MB-231-BR3, MDA-MB-231, HCC1937, BT-549) with LC50 values of 1 to 10 μM, while human ER-positive breast cancer cell lines (MCF-7, EMT6) are less sensitive[2].
QBS10072S (log[QBS] = -9 to log[QBS] = -3) dihydrochloride induces dose-dependent cytotoxicity in human TNBC MDA-MB-231 cells[2].
QBS10072S dihydrochloride induces dose-dependent cytotoxicity in LAT1-positive Hut78, HH, MJ, and H9 T-cell lymphoma cell lines[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
QBS10072S (8 mg/kg; i.v.; once a week; 9 weeks; i.p.; twice a week; 9 weeks) dihydrochloride significantly reduces intracranial tumor growth, extends survival, and decreases leptomeningeal dissemination in a TNBC brain metastasis model with no obvious toxicity[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:athymic nu/nu (female, 5 weeks old, intracranially injected with luciferase-expressing U251 human GBM cells)[1]
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Dosage:10 mg/kg
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Administration:i.v.; once weekly; 4 and 6 weeks
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Result:Achieved 95% tumor growth inhibition (TGI) at Day 35 and extended median survival from 37 days (vehicle) to 70 days with 10 mg/kg weekly for 6 weeks.
Achieved 86% TGI at Day 35 and extended median survival to 45 days with 10 mg/kg weekly for 4 weeks.
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Animal Model:athymic nu/nu (female, 5 weeks old, intracranially injected with luciferase-expressing LN229 human GBM cells)[1]
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Dosage:2, 4 and 8 mg/kg
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Administration:i.v.; once every two weeks; three total doses
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Result:Induced dose-dependent tumor growth inhibition: 72% TGI at 2 mg/kg, 73% at 4 mg/kg, and 84% at 8 mg/kg at Day 53; extended median survival from 56 days (vehicle) to 66.5 days (2 mg/kg), 71 days (4 mg/kg), and 74 days (8 mg/kg).
Chemical Information
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CAS No. 1802735-31-4
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Masse moléculaire 406.18
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Formule C15H24Cl4N2O2
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SMILES
ClCCN(C1=CC(C[C@H](N)CC(O)=O)=C(C=C1)C)CCCl.Cl.Cl
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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]. Ozawa T, et al. A Novel Blood-Brain Barrier-Permeable Chemotherapeutic Agent for the Treatment of Glioblastoma. Cureus. 2021;13(8):e17595. Published 2021 Aug 31. [Content Brief]
[2]. Murga-Zamalloa C, et al. Successful anti-tumor effects with two novel bifunctional chemotherapeutic compounds that combine a LAT1 substrate with cytotoxic moieties in aggressive T-cell lymphomas. Leuk Res Rep. 2023;21:100398. Published 2023 Nov 22. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
QBS10072S dihydrochloride Related Classifications
HY-164401A Related Classifications
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- QBS10072S
- 1802735-31-4
- EAAT
- DNA/RNA Synthesis
- DNA Alkylator/Crosslinker
- L-type amino acid transporter 1
- glioblastoma
- ALK-negative anaplastic large cell lymphoma
- Sèzary syndrome
- T-cell lymphoma
- peripheral T-cell lymphoma not otherwise specified
- angioimmunoblastic T-cell lymphoma
- LAT1
- LAT2
- SLC7A5
- Inhibitor
- inhibitor
- inhibit