| Size | Price | |
|---|---|---|
| 25mg | ||
| 50mg | ||
| 100mg | ||
| 250mg |
PF-06726304 acetate, the acetate salt of PF06726304, is a novel and potent EZH2 (Enhancer of zeste homolog 2) inhibitor with antitumor growth activity. It inhibits wild-type and Y641N mutant EZH2 with Kis of 0.7 and 3.0 nM, respectively.
| ln Vitro |
PF-06726304 (Compound 31) inhibits Karpas-422 H3K27me3 with an IC50 of 15 nM [1]. PF-06726304, with an IC50 of 25 nM, suppresses the growth of Karpas-422 cells carrying wild-type EZH2[1].
|
|---|---|
| ln Vivo |
In a subcutaneous Karpas-422 xenograft model, PF-06726304 (200 and 300 mg/kg; BID 20 days) suppresses tumor development and causes a strong modification of downstream indicators [1].
|
| Animal Protocol |
Animal/Disease Models: Female Scid beige mice (6-8 weeks old) using Karpas-422 xenograft model [1]
Doses: 200 and 300 mg/kg Route of Administration: BID for 20 days Experimental Results: Inhibited tumor growth and induced downstream organisms Robust modulation of markers in a subcutaneousKarpas-422 xenograft model. |
| References |
[1]. Kung PP, et al. Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)-ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors. J Med Chem. 2016 Sep 22;59(18):8306-25.
|
| Molecular Formula |
C₂₄H₂₅CL₂N₃O₅
|
|---|---|
| Molecular Weight |
506.38
|
| CAS # |
2080306-28-9
|
| Related CAS # |
PF-06726304;1616287-82-1
|
| SMILES |
ClC1=C(C2C(C)=NOC=2C)C=C(C2=C1C(N(CC1C(NC(C)=CC=1C)=O)CC2)=O)Cl.OC(C)=O
|
| Synonyms |
PF06726304 acetate PF 06726304 acetate
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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 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 | 1.9748 mL | 9.8740 mL | 19.7480 mL | |
| 5 mM | 0.3950 mL | 1.9748 mL | 3.9496 mL | |
| 10 mM | 0.1975 mL | 0.9874 mL | 1.9748 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
