| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| ln Vitro |
NCI-H929 cells treated with TP-064 (1 μM) for 72 hours show an increase in the G1 phase and a decrease in the S and G2/M phase proportions [1]. In both TP-064-sensitive and -insensitive cells, treatment with TP-064 (0.03-3 μM; 72 hours) lowers dimethyl-BAF155 levels in a dose-dependent manner [1]. A dose-dependent manner was observed in the inhibition of NCI-H929, RPMI8226, and MM.1R cell growth by TP-064 (10 nM-10 μM; 6 days) treatment, but no effect was observed on acute myeloid leukemia, colon, or lung cancer cell lines [1].
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| ln Vivo |
In C57BL/6 mice, TP-064 (10 mg/kg; intraperitoneal injection; three times within five days) causes neutrophilia associated to peritonitis [2].
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| Cell Assay |
Cell cycle analysis[1]
Cell Types: NCI-H929 cells Tested Concentrations: 1 μM Incubation Duration: 72 hrs (hours) Experimental Results: Induced G1 cell cycle arrest in NCI-H929 cells. Western Blot Analysis[1] Cell Types: NCI-H929, KMS-27 and U266B1 Cell Tested Concentrations: 0.03 μM, 0.1 μM, 0.3 μM, 1 μM, 3 μM Incubation Duration: 72 hrs (hours) Experimental Results: Dimethyl-BAF155 levels diminished. |
| References |
[1]. Kazuhide Nakayama, et al. TP-064, a potent and selective small molecule inhibitor of PRMT4 for multiple myeloma. Oncotarget. 2018 Apr 6;9(26):18480-18493.
[2]. Yiheng Zhang, et al. PRMT4 inhibitor TP-064 inhibits the pro-inflammatory macrophage lipopolysaccharide response in vitro and ex vivo and induces peritonitis-associated neutrophilia in vivo. Biochim Biophys Acta Mol Basis Dis. 2021 Jul 24;1867(11):166212. |
| Molecular Formula |
C28H34N4O2
|
|---|---|
| Molecular Weight |
458.606
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| Exact Mass |
458.2682
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| CAS # |
2080306-20-1
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| SMILES |
C(N(C)CC1C=CN=C(C2CCN(CCNC)CC2)C=1)(=O)C1=CC=CC(OC2=CC=CC=C2)=C1
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| Synonyms |
TP064 TP 064 TP-064
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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 |
| 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) |
DMSO : ~125 mg/mL (~272.57 mM)
H2O : ≥ 50 mg/mL (~109.03 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.54 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 (4.54 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 (4.54 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 | 2.1805 mL | 10.9025 mL | 21.8050 mL | |
| 5 mM | 0.4361 mL | 2.1805 mL | 4.3610 mL | |
| 10 mM | 0.2181 mL | 1.0903 mL | 2.1805 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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