| Size | Price | Stock | Qty |
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| 25mg |
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Purity: ≥98%
This product has been discontinued from InvivoChem. PU-H71 (also known as NSC-750424; PU-H-71) is a novel, highly potent and selective inhibitor of HSP90 with anticancer activity. It inhibits HSP90 with IC50 of 51 nM. PU-H71 showed anti-tumor effects in TNBC xenografts, including complete response and tumor regression, without toxicity to the host are achieved with this agent. PU-H71 induces efficient and sustained downregulation and inactivation, both in vitro and in vivo, of these proteins.
| ln Vitro |
Zelavespib is a strong Hsp90 product with an IC50 of 51 nM in MDA-MB-468 cells. Zelavespib inhibits the growth of multiple 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. This inhibition is consistent with G2-M blockade associated. Zelavespib (10-1000 nM) can significantly induce triple-negative breast cancer (TNBC). Zelavespib (0.5, 1 μM) can also induce potential cancer proteins in TNBC [1]. Zelavespib (0.5 μM) reduces and senescence BCR signaling disruption. Zelavespib (0.25-10 μM) is cytotoxic to CLL cells. Additionally, Zelavespib (0-1μM) reduces CLL viability by inducing mitochondria and antagonizes survival signals from the CLL microenvironment at 0.5 μM [2]. Zelavespib (0.05 μM) induces MDA-MB-231, BT-474, and MCF7 cells, and TNF-α enhances this induction. Zelavespib (0.05 μM) promotes IKKβ and activates NF-κB activity induced by TNF-α processing [3].
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| ln Vivo |
In MDA-MB-468 tumor-bearing mice, zelavespib (75 mg/kg, i.p.) resulted in intratumoral accumulation, extended downregulation of antitumor driving molecules, and completed and retained responses at nontoxic levels. Zelavespib (75 mg/kg, intraperitoneally, for 3 weeks) slows the growth of tumors; this action is linked to the downregulation of several malignant kinesins regulated by Hsp90 [1].
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| Animal Protocol |
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| References |
[1]. Caldas-Lopes E, et al. Hsp90 inhibitor PU-H71, a multimodal inhibitor of malignancy, induces complete responses in triple-negative breast cancer models. Proc Natl Acad Sci U S A. 2009 May 19;106(20):8368-73.
[2]. Guo A, et al. HSP90 stabilizes B-cell receptor kinases in a multi-client interactome: PU-H71 induces CLL apoptosis in a cytoprotective microenvironment. Oncogene. 2017 Jun 15;36(24):3441-3449. [3]. Qu Z, et al. PU-H71 effectively induces degradation of IκB kinase β in the presence of TNF-α. Mol Cell Biochem. 2014 Jan;386(1-2):135-42 |
| Molecular Formula |
C18H21IN6O2S
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| Molecular Weight |
512.37
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| CAS # |
873436-91-0
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| Related CAS # |
Zelavespib hydrochloride
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| SMILES |
NC1=C2N=C(SC3=C(I)C=C(OCO4)C4=C3)N(CCCNC(C)C)C2=NC=N1
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.88 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.88 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.88 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9517 mL | 9.7586 mL | 19.5171 mL | |
| 5 mM | 0.3903 mL | 1.9517 mL | 3.9034 mL | |
| 10 mM | 0.1952 mL | 0.9759 mL | 1.9517 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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Products are for research use only; We do not sell to patients
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