| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| Other Sizes |
|
Purity: ≥98%
Pifithrin-μ (NSC303580) is a novel and potent inhibitor of p53 binding and p53-mediated apoptosis with a Kd of 0.82 mM in vitro. It has neuroprotective and antitumor properties.
| Targets |
MDM-2/p53; HSP70
|
|||
|---|---|---|---|---|
| ln Vitro |
Pifithrin-μ interferes with p53 binding to mitochondria and inhibits rapid p53-dependent apoptosis of primary cell cultures of mouse thymocytes in response to gamma radiation.[1] In acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML) cell lines, as well as in primary AML blasts, Pifithrin-μ, an inhibitor of inducible HSP70, significantly reduced cell viability. The IC50 values ranged from 2.5 to 12.7 μM. Apoptosis and cell cycle arrest are induced by Pifithrin-μ in primary AML blasts in a dose-dependent manner, with a median IC50 of 8.9 μM (range 5.7-37.2 μM). Additionally, Pifithrin-μ decreases AKT and ERK1/2 in NALM-6 cells while increasing caspase-3's active form. [2] Pifithrin-μ promotes TRAIL-induced apoptosis and arrests the growth of cancer cells. It also increases Annexin V(+) cells in both caspase-dependent and caspase-independent ways. [3]
|
|||
| ln Vivo |
Pifithrin-μ (40 mg/kg, ip) protects C57B1/6J mice exposed to 8 or 9 Gy of total body gamma radiation from p53-dependent apoptosis. [1] Pifithrin-μ significantly improves TRAIL's ability to inhibit the growth of the MiaPaca-2 tumor in a xenograft mouse model. [3]
|
|||
| Cell Assay |
By staining with 0.5% methylene blue and calculating optical density with a Multiscan Ascent microplate reader, the number of attached cells is inferred. Using 0.1% trypan blue2 staining or FACScan analysis of annexin- or propidium iodide (PI)-positive cells, cell viability in suspension of short-term culture of primary thymocytes is assessed.
|
|||
| Animal Protocol |
|
|||
| References | ||||
| Additional Infomation |
2-phenylethynesulfonamide is a member of benzenes.
|
| Molecular Formula |
C8H7NO2S
|
|
|---|---|---|
| Molecular Weight |
181.21
|
|
| Exact Mass |
181.019
|
|
| Elemental Analysis |
C, 53.03; H, 3.89; N, 7.73; O, 17.66; S, 17.69
|
|
| CAS # |
64984-31-2
|
|
| Related CAS # |
|
|
| PubChem CID |
327653
|
|
| Appearance |
White to light brown solid powder
|
|
| Density |
1.4±0.1 g/cm3
|
|
| Boiling Point |
351.7±25.0 °C at 760 mmHg
|
|
| Melting Point |
135.0 to 139.0 °C
|
|
| Flash Point |
166.5±23.2 °C
|
|
| Vapour Pressure |
0.0±0.8 mmHg at 25°C
|
|
| Index of Refraction |
1.634
|
|
| LogP |
2
|
|
| Hydrogen Bond Donor Count |
1
|
|
| Hydrogen Bond Acceptor Count |
3
|
|
| Rotatable Bond Count |
1
|
|
| Heavy Atom Count |
12
|
|
| Complexity |
295
|
|
| Defined Atom Stereocenter Count |
0
|
|
| SMILES |
S(C#CC1C([H])=C([H])C([H])=C([H])C=1[H])(N([H])[H])(=O)=O
|
|
| InChi Key |
ZZUZYEMRHCMVTB-UHFFFAOYSA-N
|
|
| InChi Code |
InChI=1S/C8H7NO2S/c9-12(10,11)7-6-8-4-2-1-3-5-8/h1-5H,(H2,9,10,11)
|
|
| Chemical Name |
2-phenylethynesulfonamide
|
|
| Synonyms |
|
|
| HS Tariff Code |
2934.99.03.00
|
|
| 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 (e.g. under nitrogen), 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)
|
| Solubility (In Vitro) |
DMSO: ~36 mg/mL (~198.7 mM)
Water: <1 mg/mL (slightly soluble or insoluble) Ethanol: N/A |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (11.48 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 20.8 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: ≥ 2.08 mg/mL (11.48 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 20.8 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: ≥ 2.08 mg/mL (11.48 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 1% DMSO +30% polyethylene glycol+1% Tween 80 : 10 mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.5185 mL | 27.5923 mL | 55.1846 mL | |
| 5 mM | 1.1037 mL | 5.5185 mL | 11.0369 mL | |
| 10 mM | 0.5518 mL | 2.7592 mL | 5.5185 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.
 |
|---|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
