QBS10072S
QBS10072S is a LAT1-selective substrate with blood-brain barrier permeability that inhibits tumor growth. QBS10072S enters LAT1-expressing tumor cells via LAT1-mediated active transport, induces interstrand DNA cross-linking and cell apoptosis, and reduces leptomeningeal dissemination. QBS10072S 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.: 1802735-28-9
- Formule: C15H22Cl2N2O2
- Masse moléculaire:333.25
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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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Help & FAQs
Activité biologique
QBS10072S 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 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) induces dose-dependent cytotoxicity in human TNBC MDA-MB-231 cells[2].
QBS10072S 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) 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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1802735-28-9
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Masse moléculaire 333.25
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Formule C15H22Cl2N2O2
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SMILES
CC1=C(C[C@@H](CC(O)=O)N)C=C(N(CCCl)CCCl)C=C1
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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
[2]. Deng J, et al. A Novel Brain-Permeant Chemotherapeutic Agent for the Treatment of Brain Metastasis in Triple-Negative Breast Cancer. Mol Cancer Ther. 2021;20(11):2110-2116. [Content Brief]
[3]. 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 Related Classifications
HY-164401 Related Classifications
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- QBS10072S
- 1802735-28-9
- DNA Alkylator/Crosslinker
- Apoptosis
- diffuse intrinsic pontine glioma
- aggressive T-cell lymphomas
- apoptosis
- DNA interstrand crosslinks
- leptomeningeal metastasis
- glioblastoma multiforme
- L-type amino acid transporter 1
- triple-negative breast cancer brain metastasis
- LAT1/SLC7A5
- blood-brain barrier
- Inhibitor
- inhibitor
- inhibit