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. Nr.: 1184181-50-7
- Formel: C21H24N4O4S
- Molecular Weight:428.50
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
HSP90 41 nM (IC50) |
HSP70 |
In Vitro
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. Further protocols information, click here.
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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.
In Vivo
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. Nr. 1184181-50-7
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Molecular Weight 428.50
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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