PROTAC BTK Degrader-1
Based on 1 Customer Validation
PROTAC BTK Degrader-1 is a potent, selective and orally active PROTAC BTK degrader with an IC50 value of 34.51 nM and 64.56 nM for BTK WT and BTK-481S, respectively. PROTAC BTK Degrader-1 effectively reduces BTK protein levels and suppresses tumor growth.
(Pink: Btk ligand (HY-150885); Blue: Cereblon ligand (HY-138793); Black: linker).
For research use only. We do not sell to patients.
- Purity: 99.92%
- CAS No.: 2801715-13-7
- Formula: C43H43N9O4
- Molecular Weight:749.86
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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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Biological Activity
IC50: 34.51 nM (BTK WT), 64.56 nM (BTK-481S)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| JeKo-1 | IC50 |
104.69 nM
Compound: C13
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Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay
Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay
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[PMID: 35671249] |
| JeKo-1 | IC50 |
708.2 nM
Compound: C13
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Antiproliferative activity against CRBN knockout human JeKo-1 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay
Antiproliferative activity against CRBN knockout human JeKo-1 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay
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[PMID: 35671249] |
| OCI-Ly10 | IC50 |
5.9 nM
Compound: C13
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Antiproliferative activity against human OCILY10 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay
Antiproliferative activity against human OCILY10 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay
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[PMID: 35671249] |
| TMD8 | IC50 |
4.7 nM
Compound: C13
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Antiproliferative activity against human TMD8 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay
Antiproliferative activity against human TMD8 cells assessed as inhibition of cell growth incubated for 3 to 7 days by MTS assay
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[PMID: 35671249] |
Pharmacokinetic Parameters of PROTAC BTK Degrader-1 in ICR mice[1].
| PO (100 mg/kg) | IV (2 mg/kg) | |
| Tmax (h) | 1.00 | |
| T1/2 (h) | 8.3 | 3.7 |
| Cmax (ng/mL) | 3089 | |
| AUC0-t (ng/mL·h) | 16,894 | 2827 |
| AUC0-∞ (ng/mL·h) | 17,070 | 2845 |
| VdSS (L/kg) | 3.1 | |
| CL (mL/min/kg) | 11.7 | |
| MRT (h) | 4.5 | |
| F (%) | 12 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:OCI-ly10 xenograft mouse model[1]
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Dosage:10 and 30 mg/kg
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Administration:PO, bid, for 17 days
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Result:Inhibited tumor growth by 50.9 and 96.9% at 10 and 30 mg/kg, respectively.
Chemical Information
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CAS No. 2801715-13-7
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Appearance Solid
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Molecular Weight 749.86
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Formula C43H43N9O4
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Color White to off-white
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SMILES
O=C(N1)C(CCC1=O)N(C2=O)CC3=C2C=CC(C#CCN4CCC(CC4)N5CCC(CC5)N6N=C(C7=C(N=CN=C76)N)C8=CC=C(C=C8)OC9=CC=CC=C9)=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : 100 mg/mL (133.36 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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). 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 (276 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 (sealed storage, away from moisture and light). 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 | 1.3336 mL | 6.6679 mL | 13.3358 mL | 33.3396 mL |
| 5 mM | 0.2667 mL | 1.3336 mL | 2.6672 mL | 6.6679 mL | |
| 10 mM | 0.1334 mL | 0.6668 mL | 1.3336 mL | 3.3340 mL | |
| 15 mM | 0.0889 mL | 0.4445 mL | 0.8891 mL | 2.2226 mL | |
| 20 mM | 0.0667 mL | 0.3334 mL | 0.6668 mL | 1.6670 mL | |
| 25 mM | 0.0533 mL | 0.2667 mL | 0.5334 mL | 1.3336 mL | |
| 30 mM | 0.0445 mL | 0.2223 mL | 0.4445 mL | 1.1113 mL | |
| 40 mM | 0.0333 mL | 0.1667 mL | 0.3334 mL | 0.8335 mL | |
| 50 mM | 0.0267 mL | 0.1334 mL | 0.2667 mL | 0.6668 mL | |
| 60 mM | 0.0222 mL | 0.1111 mL | 0.2223 mL | 0.5557 mL | |
| 80 mM | 0.0167 mL | 0.0833 mL | 0.1667 mL | 0.4167 mL | |
| 100 mM | 0.0133 mL | 0.0667 mL | 0.1334 mL | 0.3334 mL |
PROTAC BTK Degrader-1 Related Classifications
HY-147943 Related Classifications
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