2. Membrane Transporter/Ion Channel Cell Cycle/DNA Damage
  3. EAAT DNA/RNA Synthesis DNA Alkylator/Crosslinker
  4. 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.

For research use only. We do not sell to patients.

QBS10072S dihydrochloride

QBS10072S dihydrochloride Chemical Structure

CAS No. : 1802735-31-4

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QBS10072S dihydrochloride Related Antibodies

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Description

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[1][2][3].

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.

QBS10072S dihydrochloride Related Antibodies
In Vivo

QBS10072S (10 mg/kg; i.v.; once a week; 8 weeks) dihydrochloride produces highly significant tumor growth inhibition in a subcutaneous TNBC xenograft model with no obvious toxicity[2].
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.

Animal Model: athymic nu/nu (female, 5 weeks old, intracranially injected with luciferase-expressing U251 human GBM cells)[1]
Dosage: 10 mg/kg
Administration: i.v.; once weekly; 4 and 6 weeks
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.
Animal Model: athymic nu/nu (female, 5 weeks old, intracranially injected with luciferase-expressing LN229 human GBM cells)[1]
Dosage: 2, 4 and 8 mg/kg
Administration: i.v.; once every two weeks; three total doses
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).
Molecular Weight

406.18

Formula

C15H24Cl4N2O2
CAS No.
SMILES

ClCCN(C1=CC(C[C@H](N)CC(O)=O)=C(C=C1)C)CCCl.Cl.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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QBS10072S dihydrochloride Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

QBS10072S1802735-31-4EAATDNA/RNA SynthesisDNA Alkylator/CrosslinkerExcitatory amino acid transporter Glutamate transporter| L-type amino acid transporter 1glioblastomaALK-negative anaplastic large cell lymphomaSèzary syndromeT-cell lymphomaperipheral T-cell lymphoma not otherwise specifiedangioimmunoblastic T-cell lymphomaLAT1LAT2SLC7A5Inhibitorinhibitorinhibit

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QBS10072S dihydrochloride
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