2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. HSP
  4. 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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BX-2819 Chemical Structure

BX-2819 Chemical Structure

CAS No. : 1184181-50-7

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BX-2819 Related Antibodies

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Description

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[1].

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.

BX-2819 Related Antibodies

Western Blot Analysis[1]

Cell Line: NCI-N87, MKN-45
Concentration: 0.001 μM, 0.01 μM, 0.1 μM, 1 μM, 10 μM
Incubation Time: 16 h
Result: Significantly inhibited the expression of ErbB2, Raf1 and c-Met proteins.
In Vivo

BX-2819 (100 mg/kg, intraperitoneal injection (i.p.), twice a week) significantly inhibits ErbB2 protein expression in NCI-N87 and SKOV3 tumor mice, and significantly reduces tumor growth and final tumor load in HT-29 and NCI-N87 tumor mice[1].
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.

Animal Model: SKOV3, HT-29 and NCI-N87 xenograft models in nude mice[1]
Dosage: 100 mg/kg
Administration: Intraperitoneal injection (i.p.), twice a week
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.
Molecular Weight

428.50

Formula

C21H24N4O4S
CAS No.
SMILES

CCOC(NCC1=CC=C(C=C1)N2C(NN=C2C3=C(C=C(C(C(C)C)=C3)O)O)=S)=O
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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BX-2819 Related Classifications

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Help & FAQs
  • 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:

BX-28191184181-50-7BX2819BX 2819HSPHeat shock proteinsHsp90NCI-N87HT-29 SKBR3SKOV3MKN45HT-29HepG2RPTECColon cancerOvarian cancerInhibitorinhibitorinhibit

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