| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
HSP90 51 nM (IC50, MDA-MB-468 cells)
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|---|---|
| ln Vitro |
Zelavespib hydrochloride has an IC50 of 51 nM in MDA-MB-468 cells, making it a strong Hsp90 inhibitor. Zelavespib suppresses the proliferation of many tumor cells, with IC50s of 65 ± 8 nM, 140 ± 5 nM, and 87 ± 3 nM, respectively, against MDA-MB-468, MDA-MB-231, and HCC-1806 cells. This inhibition is in line with the related G2-M blockage. Triple-negative breast cancer (TNBC) is significantly apoptotic when zelavespib (10-1000 nM) is administered. Additionally, zelavespib (0.5, 1 μM) downregulates oncoproteins linked to TNBC's capacity for invasion [1]. BCR signaling kinase is reduced and depleted by zelavespib (0.5 μM). Zelavespib (0.25–10 μM) has little effect on resting B cells or PBMC, but it is cytotoxic to CLL cells. Furthermore, at 0.5 μM, zelavespib (0-1μM) antagonizes survival signals from the CLL microenvironment and decreases CLL viability by causing mitochondrial apoptosis [2]. TNF-α boosted the induction of apoptosis in MDA-MB-231, BT-474, and MCF7 cells induced by zelavespib (0.05 μM). Zelavespib (0.05 μM) has the ability to inhibit TNF-α-induced NF-κB transcriptional activity and degrade IKKβ [3].
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| ln Vivo |
Zelavespib (75 mg/kg, i.p.) in tumor-bearing MDA-MB-468 mice resulted in intratumoral accumulation, extended downregulation of antitumor driving molecules, and completed and preserved responses at nontoxic levels. Tumor growth is inhibited by zelavespib (75 mg/kg, intraperitoneally, for 3 weeks), which is linked to the downregulation of several malignant kinesins controlled by Hsp90 [1].
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| References |
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| Molecular Formula |
C18H22CLIN6O2S
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|---|---|
| Molecular Weight |
548.83
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| CAS # |
2095432-24-7
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| Related CAS # |
Zelavespib;873436-91-0
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| Appearance |
Light yellow to yellow solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
H2O :~15.38 mg/mL (~28.02 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8221 mL | 9.1103 mL | 18.2206 mL | |
| 5 mM | 0.3644 mL | 1.8221 mL | 3.6441 mL | |
| 10 mM | 0.1822 mL | 0.9110 mL | 1.8221 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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