QBS10072S dihydrochloride
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity : 98.12%
- CAS No.: 1802735-31-4
- Formula: C15H24Cl4N2O2
- Molecular Weight:406.18
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
In Vitro
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.
In Vivo
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).
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Annexin V plus membrane-impermeant dye apoptosis staining
- Patient-Derived Xenograft (PDX)
- Transepithelial/transendothelial electrical resistance assay
- Patient-Derived Orthotopic Xenograft (PDOX)
- Apoptosis Solutions
- Subcutaneous Cell-Line-Derived Xenograft
- Breast Cancer Modeling
- Orthotopic Cell-Line Xenograft
Chemical Information
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CAS No. 1802735-31-4
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Appearance Solid
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Molecular Weight 406.18
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Formula C15H24Cl4N2O2
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Color White to light yellow
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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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 50 mg/mL (123.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (277 KB)
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SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[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]
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. 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 | 2.4620 mL | 12.3098 mL | 24.6196 mL | 61.5491 mL |
| 5 mM | 0.4924 mL | 2.4620 mL | 4.9239 mL | 12.3098 mL | |
| 10 mM | 0.2462 mL | 1.2310 mL | 2.4620 mL | 6.1549 mL | |
| 15 mM | 0.1641 mL | 0.8207 mL | 1.6413 mL | 4.1033 mL | |
| 20 mM | 0.1231 mL | 0.6155 mL | 1.2310 mL | 3.0775 mL | |
| 25 mM | 0.0985 mL | 0.4924 mL | 0.9848 mL | 2.4620 mL | |
| 30 mM | 0.0821 mL | 0.4103 mL | 0.8207 mL | 2.0516 mL | |
| 40 mM | 0.0615 mL | 0.3077 mL | 0.6155 mL | 1.5387 mL | |
| 50 mM | 0.0492 mL | 0.2462 mL | 0.4924 mL | 1.2310 mL | |
| 60 mM | 0.0410 mL | 0.2052 mL | 0.4103 mL | 1.0258 mL | |
| 80 mM | 0.0308 mL | 0.1539 mL | 0.3077 mL | 0.7694 mL | |
| 100 mM | 0.0246 mL | 0.1231 mL | 0.2462 mL | 0.6155 mL |
QBS10072S dihydrochloride Related Classifications
HY-164401A Related Classifications
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Keywords
- 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