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| ln Vitro |
In MV4-11, Molm-13, and BaF3 cells (transformed ITD, ITD-D835V, and ITD-F691L mutations), PF15 (0-1000 nM; 72 h) exhibits strong anti-proliferation activity[1]. The phosphorylation of FLT3 and STAT5 in BaF3-FLT3-ITD cells is significantly inhibited by PF15 (1, 3, 10, 30, 100, 300, 1000 nM; 6 h), which also clearly causes FLT3 degradation in a dose-dependent manner[1]. In both BaF3-FLT3-ITD-D835V and BaF3-FLT3-ITD-F691L cells, PF15 (10, 30, 100, 300, and 1000 nM; 6 hours) significantly reduces the phosphorylation of FLT3 and STAT5 at 100 nM[1]. From one hour to twenty-four hours, FLT3 degradation is induced by PF15 (100 nM; 1, 3, 6, 12, 24 h) in a time-dependent manner[1]. FLT3 degradation is induced by PF15 (15.6, 31.2, 62.5, 125, 250, 500, 1000, and 2000 nM; 24 h); the DC50 for this is 76.7 nM[1].
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| ln Vivo |
PF15 (10 or 20 mg/kg; ip; once daily for 10 days) shows good tumor growth inhibition with an inhibitory rate of 58.4% at dosage of 10 mg/kg, and when up to 20 mg/kg displays higher inhibitory rate[1]. PF15 (twice daily (20 mg/kg), once daily (40 mg/kg); 12 days; ip) prolongs the median survival up to 15 days (negative control group is 11 days) in BaF3-FLT3-ITD in situ model[1].
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: MV4-11, Molm-13, BaF3 cells (transformed ITD, ITD-D835V, and ITD-F691L mutations) Tested Concentrations: 0-1000 nM Incubation Duration: 72 h Experimental Results: demonstrated anti-proliferation activity with IC50s of 4.83 nM (MV4-11), 4.01 nM (Molm-13) and 7.85 , 120.1, 116.6 nM (for transformed BaF3 cells harboring ITD, ITD-D835V, and ITD-F691L mutations respectively). Western Blot Analysis[1] Cell Types: BaF3-FLT3-ITD, BaF3-FLT3-ITD-D835V, BaF3- FLT3-ITD-F691L cells Tested Concentrations: 1, 3, 10, 30, 100, 300, 1000 nM Incubation Duration: 6 h Experimental Results: Induced FLT3 degradation when at 3 nM and in a dose-dependent manner in BaF3-FLT3-ITD cells . Dramatically inhibited the phosphorylation of FLT3 and STAT5 when concentration up to 30 nM in BaF3-FLT3-ITD cells, and at 100 nM in both BaF3-FLT3-ITD-D835V and BaF3-FLT3-ITD-F691L cells. Western Blot Analysis[1] Cell Types: BaF3-FLT3-ITD cells Tested Concentrations: 100 nM Incubation Duration: 1, 3, 6, 12, 24 h Experimental Results: Dramatically induced FLT3 degradatio |
| Animal Protocol |
Animal/Disease Models: Female NOD/SCID (severe combined immunodeficient) mouse (BaF3-FLT3-ITD xenograft model)[1].
Doses: 10 or 20 mg/kg Route of Administration: intraperitoneal (ip) injection; one time/day for 10 days. Experimental Results: Achieved good tumor growth inhibition with an inhibitory rate of 58.4% (10 mg/kg), meanwhile, when at 20 mg/kg displayed higher inhibitory rate. Hardly caused side effects on heart, liver, and kidney (both of the treatment groups). Animal/Disease Models: Female BALB/c nude mice (BaF3-FLT3-ITD in situ model)[1]. Doses: 20, 40 mg/kg Route of Administration: intraperitoneal (ip) injection; twice (two times) daily (20 mg/kg), one time/day (40 mg /kg); 12 days. Experimental Results: Prolonged the median survival from 11days to 15 days (both of the treatment groups). |
| References |
[1]. Chen Y, et al. Degrading FLT3-ITD protein by proteolysis targeting chimera (PROTAC). Bioorg Chem. 2022 Feb;119:105508.
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| Molecular Formula |
C44H49N13O6
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|---|---|
| Molecular Weight |
855.94
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| CAS # |
2892631-70-6
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| Related CAS # |
PF15 TFA
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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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 (116.83 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.92 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 (2.92 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1683 mL | 5.8415 mL | 11.6831 mL | |
| 5 mM | 0.2337 mL | 1.1683 mL | 2.3366 mL | |
| 10 mM | 0.1168 mL | 0.5842 mL | 1.1683 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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