SKU : MC511008
CAS Number : 1202865-65-3
Molecular Formula : C18H23IN6O3S | Molecular Weight : 530.38
Quote RequestPurity | NLT 98% |
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Storage | at 20ºC 2 years |
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Chemical Name | PU-H71 Hydrate(1:x) |
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CAS Number | 1202865-65-3 |
MDL Number | MFCD17215935 |
Molecular Formula | C18H23IN6O3S |
Molecular Weight | 530.38 |
PU-H71 Hydrate(1:x) is a potent Hsp90 inhibitor, with an IC50 of 51 nM in MDA-MB-468 cells. IC50 & Target: IC50: 51 nM (Hsp90, in MDA-MB-468 cells)[1] In Vitro: PU-H71 Hydrate(1:x) is a potent Hsp90 inhibitor, with an IC50 of 51 nM in MDA-MB-468 cells. PU-H71 inhibits the growth of several tumor cells, such as MDA-MB-468, MDA-MB-231 and HCC-1806 cells, with IC50s of 65 ± 8 nM, 140 ± 5 nM and 87 ± 3 nM, respectively, and such inhibition is associated with a G2-M block arrest. PU-H71 (10-1000 nM) induces significant apoptosis in triple-negative breast cancers (TNBCs). PU-H71 (0.5, 1 μM) also downregulates oncoproteins involved in the invasive potential of TNBCs[1]. PU-H71 (0.5 μM) decreases and depletes the BCR signaling kinases. PU-H71 (0.25-10 μM) is cytotoxic to CLL cells but shows minimal effects on PBMC or resting B cells. In addition, PU-H71 (0-1 μM) reduces CLL viability via the induction of mitochondrial apoptosis, and antagonizes the survival signals from CLL microenvironment at 0.5 μM[2]. PU-H71 (0.05 μM) induces apoptosis of MDA-MB-231, BT-474, and MCF7 cells, and such induction is enhanced by TNF-α. PU-H71 (0.05 μM) degradates IKKβ, and down-regulates the NF-κB transcriptional activity induced by TNF-α treatment[3]. In Vivo: PU-H71 (75 mg/kg, i.p.) causes intratumor accumulation, extends down-regulation of anti-tumor driving molecules, completes and retains responses at nontoxic doses in MDA-MB-468 tumor-bearing mice. PU-H71 (75 mg/kg 3×week, i.p.) suppresses the gowth of tumors, and such an effect is associated with down-regulation of several Hsp90-regulated malignancy driving proteins[1].
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