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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]. | [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 |
| 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.
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| [IC 50]
HSP90: 41 nM (IC50); HSP70 | [References]
[1] Feldman RI, et al. Potent triazolothione inhibitor of heat-shock protein-90. Chem Biol Drug Des. 2009 Jul;74(1):43-50. DOI:10.1111/j.1747-0285.2009.00833.x |
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