KTX-951
Based on 1 Customer Validation
KTX-951 is an orally active PROTAC degrader of IRAK4 and IMiD (Ikaros/Aiolos) substrates (Kd = 3.5 nM). KTX-951 induces IRAK4 degradation, and the degradation efficiency is independent of IRAK4 binding affinity. The DC50 values of KTX-951 for IRAK4, Ikaros and Aiolos are 18 nM, 14 nM and 13 nM, respectively. The IC50 of KTX-951 against OCl-Ly10 CTG is 35 nM. KTX-951 exhibits antitumor activity.
(Pink: IRAK4 ligand (HY-48932); Blue: Cereblon ligand (HY-10984); Black: linker (HY-W382009)).
For research use only. We do not sell to patients.
- Purity: 99.60%
- CAS No.: 2573298-36-7
- Formula: C46H52F2N8O6
- Molecular Weight:850.95
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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 PROTACs Isoforms
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Biological Activity
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IRAK4 3.5 nM (Kd) |
IRAK4 18 nM (DC50) |
KTX-951 binds to recombinant IRAK4 with a Kd of 3.5 nM[1].
KTX-951 degrades IRAK4, Ikaros, and Aiolos in OCI-Ly10 cells with DC50 values of 18 nM, 14 nM, and 13 nM, respectively, and inhibits OCI-Ly10 cell proliferation with an IC50 of 35 nM[1].
KTX-951 exhibits favorable in vitro metabolic stability, permeability, solubility, and human plasma protein binding properties, including HLM clearance of 2 μL/min/mg, MDCK permeability of 1.1×10-6 cm/s, FaSSIF solubility of 21 μM, and human plasma free fraction of 0.12[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2573298-36-7
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Appearance Solid
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Molecular Weight 850.95
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Formula C46H52F2N8O6
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Color Light yellow to yellow
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SMILES
FC(F)(C)C1=CC=CC(C(NC(C(OC)=CC2=N3)=CC2=CN3[C@H]4CC[C@@H](CC4)CN5CCC6(CC(CCNC7=C(C8=O)C(C(N8C(C(N9)=O)CCC9=O)=O)=CC=C7)C6)CC5)=O)=N1
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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 : 50 mg/mL (58.76 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, 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)
Purity & Documentation
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Data Sheet (272 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 | 1.1752 mL | 5.8758 mL | 11.7516 mL | 29.3789 mL |
| 5 mM | 0.2350 mL | 1.1752 mL | 2.3503 mL | 5.8758 mL | |
| 10 mM | 0.1175 mL | 0.5876 mL | 1.1752 mL | 2.9379 mL | |
| 15 mM | 0.0783 mL | 0.3917 mL | 0.7834 mL | 1.9586 mL | |
| 20 mM | 0.0588 mL | 0.2938 mL | 0.5876 mL | 1.4689 mL | |
| 25 mM | 0.0470 mL | 0.2350 mL | 0.4701 mL | 1.1752 mL | |
| 30 mM | 0.0392 mL | 0.1959 mL | 0.3917 mL | 0.9793 mL | |
| 40 mM | 0.0294 mL | 0.1469 mL | 0.2938 mL | 0.7345 mL | |
| 50 mM | 0.0235 mL | 0.1175 mL | 0.2350 mL | 0.5876 mL |
KTX-951 Related Classifications
HY-148290 Related Classifications
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