PF-06465469
Based on 2 publication(s) in Google Scholar
PF-06465469 is a covalent inhibitor of ITK with an IC50 of 2 nM. PF-06465469 also inhibits BTK. PF-06465469 inhibits cell migration in response to CXCL12. PF-06465469 decreases PD-1 and LAG-3 expression. PF-06465469 can be used to study leukemia and T-cell lymphoma.
For research use only. We do not sell to patients.
- Purity: 99.48%
- CAS No.: 1407966-77-1
- Formula: C30H33N7O2
- Molecular Weight:523.63
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) PF-06465469
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Biological Activity
IC50: 2 nM (ITK)[1]
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Cell Line
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Type | Value | Description | References |
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| Jurkat | IC50 |
0.031 μM
Compound: 41, PF-06465469
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Covalent inhibition of ITK in human Jurkat cells assessed as inhibition of anti-CD3 antibody-stimulated PLCgamma phosphorylation pre-incubated before anti-CD3 antibody challenge by Western blotting
Covalent inhibition of ITK in human Jurkat cells assessed as inhibition of anti-CD3 antibody-stimulated PLCgamma phosphorylation pre-incubated before anti-CD3 antibody challenge by Western blotting
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[PMID: 23098091] |
PF-06465469 (2 µM, 24 h) reduces ITK phosphorylation in Jurkat cells and inhibits migration of Jurkat cells in response to CXCL12[1].
PF-06465469 (1 µM) significantly decreases CD69, PD-1 and LAG-3 expression in CAR-T cells cocultured with MEC1 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1407966-77-1
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Appearance Solid
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Molecular Weight 523.63
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Formula C30H33N7O2
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Color White to off-white
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SMILES
O=C(NC1=CC=C(C(C)C)C(C)=C1)C2=CC=CC(C3=NN([C@H]4CN(C(C=C)=O)CCC4)C5=NC=NC(N)=C53)=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Cancer Lett
Interleukin-2-inducible T-cell kinase inhibition to block NF-κB signaling exerts anti-tumor effects and enhances chemotherapy in NK/T-cell lymphoma. [Abstract]2025 May 28:618:217602. PMID: 40054659 -
PLoS One
A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]2024 Nov 1;19(11):e0308647. PMID: 39485774
Solvent & Solubility
DMSO : 11 mg/mL (21.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 1.1 mg/mL (2.10 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1.1 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (11.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.1 mg/mL (2.10 mM); Clear solution
This protocol yields a clear solution of ≥ 1.1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (11.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Mamand S, et al. Comparison of interleukin-2-inducible kinase (ITK) inhibitors and potential for combination therapies for T-cell lymphoma. Sci Rep. 2018 Sep 21;8(1):14216. [Content Brief]
[2]. Fu Z, et al. IL-2-inducible T cell kinase deficiency sustains chimeric antigen receptor T cell therapy against tumor cells. J Clin Invest. 2024 Nov 26;135(4):e178558. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9097 mL | 9.5487 mL | 19.0975 mL | 47.7436 mL |
| 5 mM | 0.3819 mL | 1.9097 mL | 3.8195 mL | 9.5487 mL | |
| 10 mM | 0.1910 mL | 0.9549 mL | 1.9097 mL | 4.7744 mL | |
| 15 mM | 0.1273 mL | 0.6366 mL | 1.2732 mL | 3.1829 mL | |
| 20 mM | 0.0955 mL | 0.4774 mL | 0.9549 mL | 2.3872 mL |
PF-06465469 Related Classifications
HY-108691 Related Classifications
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