NSC 373981
NSC 373981 is a CARD11 G4 stabilizer. NSC 373981 stabilizes the CARD11 G4 structure and inhibits CARD11 transcription in cells. NSC 373981 also inhibits BCL2 and MYC. NSC 373981 suppresses the transcription of KRAS and TERT. NSC 373981 exhibits anticancer activity against diffuse large B-cell lymphoma.
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- CAS No.: 95455-02-0
- Formule: C14H11NO4
- Masse moléculaire:257.24
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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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Activité biologique
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BCL2 |
K-RAS |
NSC 373981 (24 h; 37°C) exhibits stability across acidic, neutral, and basic conditions, and in human and mouse plasma following 24-hour incubation at 37°C[1].
NSC 373981 (2.5-10.0 µM; 24 h) represses CARD11, BCL2, and MYC mRNA expression in a dose-dependent manner in RIVA, HBL1, and HT DLBCL cells, with additional effects on KRAS and TERT in RIVA and HT cells, but has no effect on CARD11 expression in VAL DLBCL or GM22671 benign B cells[2].
NSC 373981 (0.02-40 µM; 72 h) exhibits low micromolar cytotoxicity in RIVA, HT, and GM22671 cells, with higher cytotoxicity in cells where it represses multiple oncogene mRNA levels, and cytotoxicity does not correlate with basal CARD11 expression[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:ABC DLBCL (RIVA, HBL1), GCB DLBCL (HT, VAL), benign GC B (GM22671) cells
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Concentration:2.5, 5.0, 10.0 µM
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Incubation Time:24 h
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Result:Caused a significant, dose-dependent repression of CARD11 mRNA levels (45-90% reduction at 10 µM) in RIVA, HBL1, and HT cells.
Induced concurrent dose-dependent decreases in BCL2 and MYC mRNA levels in RIVA, HBL1, and HT cells.
Reduced KRAS mRNA by 25-30% in RIVA cells and TERT mRNA by 40-55% in HT cells at 10 µM.
Showed no significant change in CARD11 mRNA levels in VAL and GM22671 cells.
Reduced MYC mRNA in GM22671 cells at 10 µM.
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 (male)[1]
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Dosage:37.5 mg/kg (i.v.); 150 mg/kg (i.p.)
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Administration:i.v.; single dose; i.p.; single dose
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Result:Achieved peak plasma concentration >5.9 μg/mL, terminal elimination half-life 1.2 hours, volume of distribution 694 mL, and plasma clearance 390 mL/hr following i.v. administration.
Reached peak plasma concentration 2.1 μg/mL at 15 minutes, terminal elimination half-life 36.8 hours, and 58% bioavailability following i.p. administration.
Detected multiple Phase I and Phase II metabolites in plasma, urine, feces, and bile, including those from aromatic nitro group reduction, primary alcohol moiety oxidation, benzylic hydroxylation, naphthalene moiety hydroxylation/dihydrodiol formation, and Phase II conjugation reactions.
Chemical Information
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CAS No. 95455-02-0
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Masse moléculaire 257.24
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Formule C14H11NO4
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SMILES
OCCC1=C([N+]([O-])=O)OC2=CC=C3C=CC=CC3=C21
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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)
NSC 373981 Related Classifications
HY-182706 Related Classifications
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