YH-IV-173
YH-IV-173 is a BRG1 (SMARCA4) bromodomain binder with higher affinity for BRG1 than for BRM. YH-IV-173 acts as a sensitizing agent when combined with Temozolomide (HY-17364), modulating glioblastoma (GBM) cell proliferation and tumor growth. YH-IV-173 treatment alone shows weak effects on glioblastoma cell growth and tumor growth.
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- CAS No.: 2616813-99-9
- Formule: C20H19FN2O
- Masse moléculaire:322.38
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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
Description
IC50 & Target
[1]|
BRG1 |
In Vitro
YH-IV-173 (11d) (48 h) potently sensitizes MT330 human glioblastoma cells to Temozolomide (TMZ) (HY-17364)-induced apoptosis[1].
YH-IV-173(up to 7 days) potently enhances the antiproliferative effect of Temozolomide in LN229 human glioblastoma cells[1].
YH-IV-173 (30 μM; 3 hr) binds to the BRG1 bromodomain in MT330 human glioblastoma cells, as demonstrated by increased protein thermostability in CETSA[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) (female; five-week-old; ~25 g; subcutaneous flank xenograft model established via flank injection of luciferase-expressing MT330 GBM cells)[1]
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Dosage:10 mg/kg
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Administration:i.p.; weekly; initiated 1 week after tumor cell injection
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Result:Exhibited only a slight inhibitory effect on subcutaneous GBM tumor growth as a single agent.
Resulted in tumor volume reaching 1000 mm3 by 3 weeks post-administration as a single agent, requiring euthanasia of mice.
When combined with Temozolomide, produced a tumor growth inhibitory effect.
Chemical Information
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CAS No. 2616813-99-9
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Masse moléculaire 322.38
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Formule C20H19FN2O
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SMILES
O=C(/C=C/N1[C@@H]2C[C@H](C1)N(C3=CC=C(F)C=C3)C2)C4=CC=CC=C4
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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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
YH-IV-173 Related Classifications
HY-144720 Related Classifications
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