| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
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| ln Vitro |
Concentration-dependent growth abnormalities in ESCs are caused by TP-472 (1 µM, 3 µM; 24-216 hours) [2]. At dosages of 5 and 10 μM, TP-472 (0.1-10 μM; 24 hours) efficiently suppresses the development of BRAF mutant melanoma cell lines [3]. At doses of 5 and 10 µM, TP-472 also significantly reduces the long-term survival of several melanoma cell lines (M14, SKMEL-28, A375, and A2058; this effect lasts for two weeks) [3]. When A375 cells are treated with TP-472 (5–10 μM) for 24 hours, the genes that encode several extracellular matrix (ECM) proteins, such as integrins, collagen, and fibronectin, are downregulated [3]. In A375 cells, TP-472 (0.1-10 μM; 24 hours) induces pro-apoptotic genes (BAX, MDM2, CDKN1A) to be upregulated [3].
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| ln Vivo |
TP-472 (20 mg/kg; i.p.; 3 times per week; for 5 weeks) effectively suppressed subcutaneous tumor growth in a melanoma xenograft mice model [3].
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: Embryonic Stem Cells Tested Concentrations: 1 µM, 3 µM Incubation Duration: 24 hrs (hours), 72 hrs (hours), 120 hrs (hours), 168 hrs (hours), 216 hrs (hours) Experimental Results: Concentration-dependent growth defects in ESCs. Cell proliferation assay[3] Cell Types: M14 and SKMEL-28 cells[3] Tested Concentrations: 0.1 μM, 0.5 μM, 1 μM, 2 μM, 5 μM, 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: Effectively inhibited the growth of both BRAF mutant melanoma cell lines. Western Blot Analysis[3] Cell Types: A375 Cell Tested Concentrations: 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: Result in upregulation of pro-apoptotic genes. |
| Animal Protocol |
Animal/Disease Models: NSG mice (male, five to six weeks old) injected with A375-MA2 cells [3]
Doses: 20 mg/kg Route of Administration: intraperitoneal (ip) injection; three times a week; for 5 consecutive weeks Experimental Results: Dramatically inhibited melanoma subcutaneoustumor growth in xenograft mouse models. |
| References |
|
| Molecular Formula |
C₂₀H₁₉N₃O₂
|
|---|---|
| Molecular Weight |
333.38
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| Exact Mass |
333.147
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| CAS # |
2079895-62-6
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| PubChem CID |
123773279
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.681
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| LogP |
1.25
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| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
25
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| Complexity |
533
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
RPBMXJHQYJLPDN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H19N3O2/c1-12-4-5-14(20(25)22-15-6-7-15)10-16(12)17-11-18(13(2)24)23-9-3-8-21-19(17)23/h3-5,8-11,15H,6-7H2,1-2H3,(H,22,25)
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| Chemical Name |
3-(6-acetylpyrrolo[1,2-a]pyrimidin-8-yl)-N-cyclopropyl-4-methylbenzamide
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| Synonyms |
TP472 TP 472
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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 : ~100 mg/mL (~299.96 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.50 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 (7.50 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9996 mL | 14.9979 mL | 29.9958 mL | |
| 5 mM | 0.5999 mL | 2.9996 mL | 5.9992 mL | |
| 10 mM | 0.3000 mL | 1.4998 mL | 2.9996 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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