PDGFRA/CAIX/XII-IN-1
Based on 1 Customer Validation
PDGFRA/CAIX/XII-IN-1 is an inhibitor of PDGFRA, CA IX and CA XII, with an IC50 of 20 nM against PDGFRA, a Ki of 93.3 nM against CA IX, and a Ki of 80.0 nM against CA XII. PDGFRA/CAIX/XII-IN-1 binds to the ATP-binding pocket of PDGFRA and blocks the downstream STAT3, AKT and ERK1/2 signaling pathways. PDGFRA/CAIX/XII-IN-1 induces G0/G1 cell cycle arrest and endogenous apoptosis (Apoptosis), including cleavage of PARP-1, caspase-9 and caspase-3, activation of caspase 3/7, and down-regulation of Mcl-1. PDGFRA/CAIX/XII-IN-1 exhibits antiproliferative activity in eosinophilic leukemia cells. PDGFRA/CAIX/XII-IN-1 can be used for the research of leukemia.
For research use only. We do not sell to patients.
- Purity: 98.10%
- Formula: C25H25N5O5S
- Molecular Weight:507.56
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
All Caspase Isoforms
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Biological Activity
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CA IX 93.3 nM (Ki) |
CA XII 80 nM (Ki) |
STAT3 |
ERK1 |
ERK2 |
Caspase-9 |
Caspase 3 |
PDGFRA/CAIX/XII-IN-1 (Compound 9d) potently inhibits recombinant PDGFRA protein, with an IC50 of 20 nM[1].
PDGFRA/CAIX/XII-IN-1 (1 μM) exerts targeted inhibitory effects on specific RTK subfamilies, and exhibits potent activity against PDGFRα and closely related class III RTKs[1].
PDGFRA/CAIX/XII-IN-1 inhibits recombinant human cancer-associated CA IX (Ki = 93.3 nM) and CA XII (Ki = 80.0 nM) with moderate potency, while exhibiting only weak activity against normal CA I/II isoforms[1].
PDGFRA/CAIX/XII-IN-1 (72 h) potently inhibits the proliferation of FIP1L1-PDGFRA-driven EOL-1 eosinophilic leukemia cells (GI50 = 2 nM), also exhibits significant cytotoxicity against MV4-11 cells (GI50 = 0.263 μM), and shows weak cytotoxicity against Kasumi-1 and RS4-11 cells with GI50 values of 2.081 μM and 4.599 μM, respectively[1].
PDGFRA/CAIX/XII-IN-1 (0-2500 nM; 1 h) dose-dependently inhibits the phosphorylation of FIP1L1-PDGFRA and its downstream STAT3, AKT and ERK1/2 signaling pathways in EOL-1 cells; after treatment at a concentration of 100 nM for 1 h, the inhibitory effect on PDGFRA is nearly complete[1].
PDGFRA/CAIX/XII-IN-1 (0-2500 nM; 24 h) induces apoptosis in EOL-1 eosinophilic leukemia cells by activating the intrinsic apoptotic pathway. The effect is detectable at a concentration of 0.8 nM, and the pathway is potently activated at subnanomolar concentrations, while no pro-apoptotic effect is observed on THP-1 cells[1].
PDGFRA/CAIX/XII-IN-1 (0.16-100 nM; 24 h) induces dose-dependent G0/G1 cell cycle arrest in EOL-1 eosinophilic leukemia cells, with a significant arrest effect observed at 0.8 nM; additionally, after 24 h of treatment, concentrations of 4 nM and above induce apoptotic cell death (characterized by a sub-G1 cell population)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:EOL-1 cells
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Concentration:0, 4, 20, 100, 500, 2500 nM
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Incubation Time:1 h
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Result:Induced a dose-dependent inhibition of FIP1L1-PDGFRA phosphorylation (p-PDGFRA/B Y849/857), with substantial reduction at 20 nM and near-complete dephosphorylation at 100 nM.
Reduced phosphorylation of downstream signaling molecules STAT3 (p-STAT3 Y705) from 20 nM upward, AKT (p-AKT S473) with substantial inhibition at 100 nM and above, and ERK1/2 (p-ERK1/2 T202/Y204) with strong inhibition from 100 nM.
Maintained unchanged total protein levels of PDGFRA, STAT3, AKT, and ERK1/2.
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Cell Line:EOL-1 cells, THP-1 cells
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Concentration:0.032, 0.16, 0.8, 4, 20, 100, 500 2500 nM (caspase 3/7 activity, Western blot); 0.16, 4, 100 nM (Annexin V/PI staining)
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Incubation Time:24 h
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Result:In EOL-1 cells: induced dose-dependent cleavage of PARP-1 (detectable at 0.8 nM, accumulating at 4 nM and higher), reduced antiapoptotic Mcl-1 expression (substantial reduction at 4 nM, near-complete depletion at 20 nM), activated caspase 9 (cleavage detected at 4 nM and higher) and caspase 3 (cleavage detected at 4 nM and higher).
Caused a robust, dose-dependent increase in caspase 3/7 activity (significant activation at 0.032 nM, ~7-fold increase at 0.8 nM).
Induced a concentration-dependent shift from viable cells to early and late apoptotic populations via Annexin V/PI staining.
In THP-1 cells: showed no significant signs of apoptosis or caspase 3/7 activation at tested concentrations.
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Cell Line:EOL-1 cells
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Concentration:0.16, 0.8, 4, 20, 100 nM
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Incubation Time:24 h
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Result:Caused a dose-dependent accumulation of cells in the G0/G1 phase, accompanied by a decrease in S and G2/M populations.
Induced modest G0/G1 arrest at 0.16 nM, significant arrest at 0.8 nM and higher.
Triggered a sub-G1 apoptotic population from 4 nM onward, which expanded markedly at 20 and 100 nM.
Chemical Information
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Appearance Solid
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Molecular Weight 507.56
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Formula C25H25N5O5S
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Color Light yellow to light brown
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SMILES
O=C(NC1=CC(S(=O)(N)=O)=C(C=C1)C)NC2=CC=C(C=C2)NC3=C4C=C(C(OC)=CC4=NC=C3)OC
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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 6 months -20°C 1 month
Solvent & Solubility
DMSO : 8.33 mg/mL (16.41 mM; ultrasonic and warming and heat to 60°C; 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 0.83 mg/mL (1.64 mM); Clear solution
This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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: ≥ 0.83 mg/mL (1.64 mM); Clear solution
This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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 (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9702 mL | 9.8511 mL | 19.7021 mL | 49.2553 mL |
| 5 mM | 0.3940 mL | 1.9702 mL | 3.9404 mL | 9.8511 mL | |
| 10 mM | 0.1970 mL | 0.9851 mL | 1.9702 mL | 4.9255 mL | |
| 15 mM | 0.1313 mL | 0.6567 mL | 1.3135 mL | 3.2837 mL |
PDGFRA/CAIX/XII-IN-1 Related Classifications
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