1. PROTAC Protein Tyrosine Kinase/RTK
  2. PROTACs FLT3
  3. PF15

PF15 is a PROTAC connected by ligands for FLT3 kinase and CRBN. PF15 is a high selective FLT3-ITD degrader, with a DC50 of 76.7 nM. PF15 significantly inhibits the proliferation of FLT3-ITD-positive cells, can down-regulate the phosphorylation of FLT3 and STAT5. PF15 also inhibits tumor growth in mouse models and can be used in study of leukemia.

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PF15 Chemical Structure

PF15 Chemical Structure

CAS No. : 2892631-70-6

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Description

PF15 is a PROTAC connected by ligands for FLT3 kinase and CRBN. PF15 is a high selective FLT3-ITD degrader, with a DC50 of 76.7 nM. PF15 significantly inhibits the proliferation of FLT3-ITD-positive cells, can down-regulate the phosphorylation of FLT3 and STAT5. PF15 also inhibits tumor growth in mouse models and can be used in study of leukemia[1].

In Vitro

PF15 (0-1000 nM; 72 h) shows good anti-proliferation activity in MV4-11, Molm-13 and BaF3 cells (transformed ITD, ITD-D835V, and ITD-F691L mutations)[1].
PF15 (1, 3, 10, 30, 100, 300, 1000 nM; 6 h) obviously induces FLT3 degradation in a dose-dependent manner and (10, 30, 100, 300, 1000 nM; 6 h) dramatically inhibits the phosphorylation of FLT3 and STAT5 in BaF3-FLT3-ITD cells[1].
PF15 (10, 30, 100, 300, 1000 nM; 6 h) sharply downregulates the phosphorylation of FLT3 and STAT5 at 100 nM in both BaF3-FLT3-ITD-D835V and BaF3-FLT3-ITD-F691L cells[1].
PF15 (100 nM; 1, 3, 6, 12, 24 h) induces FLT3 degradation in a time-dependent manner from 1 h to 24 h[1].
PF15 (15.6, 31.2, 62.5, 125, 250, 500, 1000, 2000 nM; 24 h) induces FLT3 degradation with a DC50 of 76.7 nM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: MV4-11, Molm-13, BaF3 cells (transformed ITD, ITD-D835V, and ITD-F691L mutations)
Concentration: 0-1000 nM
Incubation Time: 72 h
Result: Exhibited 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 Line: BaF3-FLT3-ITD, BaF3-FLT3-ITD-D835V, BaF3-FLT3-ITD-F691L cells
Concentration: 1, 3, 10, 30, 100, 300, 1000 nM
Incubation Time: 6 h
Result: 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 Line: BaF3-FLT3-ITD cells
Concentration: 100 nM
Incubation Time: 1, 3, 6, 12, 24 h
Result: Significantly induced FLT3 degradation in a time-dependent manner, and FLT3 completely degraded when at 24 h.

Western Blot Analysis[1]

Cell Line: BaF3-FLT3-ITD cell
Concentration: 15.6, 31.2, 62.5, 125, 250, 500, 1000, 2000 nM
Incubation Time: 24 h
Result: Notably induced FLT3 degradation when at 125 nM, and DC50 was 76.7 nM.
In Vivo

PF15 (10 or 20 mg/kg; i.p.; 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; i.p.) prolongs the median survival up to 15 days (negative control group is 11 days) in BaF3-FLT3-ITD in situ model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female NOD/SCID mice (BaF3-FLT3-ITD xenograft model)[1].
Dosage: 10 or 20 mg/kg
Administration: Intraperitoneal injection; once daily for 10 days.
Result: 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 Model: Female BALB/c nude mice (BaF3-FLT3-ITD in situ model)[1].
Dosage: 20, 40 mg/kg
Administration: Intraperitoneal injection; twice daily (20 mg/kg), once daily (40 mg/kg); 12 days.
Result: Prolonged the median survival from 11days to 15 days (both of the treatment groups).
Molecular Weight

855.94

Formula

C44H49N13O6

CAS No.
SMILES

CC(C)(C1=CC(NC(NC2=CC=C(C=C2)C3=CN(C4=NC=NC(N)=C34)CCCCC5=CN(N=N5)CCCCC(NC6=C7CN(C(C7=CC=C6)=O)C8CCC(NC8=O)=O)=O)=O)=NO1)C

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (116.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table
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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (2.92 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (2.92 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
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Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.1683 mL 5.8415 mL 11.6831 mL 29.2077 mL
5 mM 0.2337 mL 1.1683 mL 2.3366 mL 5.8415 mL
10 mM 0.1168 mL 0.5842 mL 1.1683 mL 2.9208 mL
15 mM 0.0779 mL 0.3894 mL 0.7789 mL 1.9472 mL
20 mM 0.0584 mL 0.2921 mL 0.5842 mL 1.4604 mL
25 mM 0.0467 mL 0.2337 mL 0.4673 mL 1.1683 mL
30 mM 0.0389 mL 0.1947 mL 0.3894 mL 0.9736 mL
40 mM 0.0292 mL 0.1460 mL 0.2921 mL 0.7302 mL
50 mM 0.0234 mL 0.1168 mL 0.2337 mL 0.5842 mL
60 mM 0.0195 mL 0.0974 mL 0.1947 mL 0.4868 mL
80 mM 0.0146 mL 0.0730 mL 0.1460 mL 0.3651 mL
100 mM 0.0117 mL 0.0584 mL 0.1168 mL 0.2921 mL
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PF15 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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PF15
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