BX-2819
BX-2819 is a Hsp90 inhibitor with an IC50 value of 41 nM. BX-2819 inhibits the proliferation of cancer cells. BX-2819 can significantly inhibit the growth of NCI-N87 and HT-29 tumors in nude mice.
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- CAS No.: 1184181-50-7
- Formule: C21H24N4O4S
- Masse moléculaire:428.50
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Activité biologique
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HSP90 41 nM (IC50) |
HSP70 |
BX-2819 (0.001-10 μM, 16 h) can inhibit the expression of ErbB2 protein and significantly enhances the expression of Hsp70 in HT-29, OVCAR3 and SKBR3[1].
BX-2819 (0.001-10 μM, 72 h) can inhibit cell proliferation in SKBR3 (IC50=14 nM), SKOV3 (IC50 = 36 nM), 50 MKN45 (IC50=72 nM), NCI-N87 (IC50= 7 nM) tumor cancer cells[1].
BX-2819 (100 μM) has no significant cytotoxic effects on cells in HepG2 and RPTEC cells[1] .
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI-N87, MKN-45
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Concentration:0.001 μM, 0.01 μM, 0.1 μM, 1 μM, 10 μM
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Incubation Time:16 h
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Result:Significantly inhibited the expression of ErbB2, Raf1 and c-Met proteins.
BX-2819 (2 mk/kg, intravenous injection (i.v.), single dose) shows relatively short serum half-life (t1/2=0.8 h), high clearance rate (CL=159 mL/min/kg), and large distribution volume (Vss=4.5 L) in rats[1].
Pharmacokinetic parameters of BX-2819 in rats (n = 4) [1]
| Dose（mg/kg） | Route | T1/2(h) | AUCinf(μg h/mL) | CL (mL/min) | Vss(L/kg) |
| 2 | iv | 0.8 | 0.23 | 159 | 4.5 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SKOV3, HT-29 and NCI-N87 xenograft models in nude mice[1]
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Dosage:100 mg/kg
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Administration:Intraperitoneal injection (i.p.), twice a week
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Result:Significantly inhibited ErbB2 expression, effectively inhibited Hsp90 for a long time, and enhanced Hsp70 expression.
Could enter the plasma after intraperitoneal injection.
Significantly decreased in tumor growth and final tumor burden.
Chemical Information
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CAS No. 1184181-50-7
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Masse moléculaire 428.50
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Formule C21H24N4O4S
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SMILES
CCOC(NCC1=CC=C(C=C1)N2C(NN=C2C3=C(C=C(C(C(C)C)=C3)O)O)=S)=O
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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)
BX-2819 Related Classifications
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