PROTAC BTK Degrader-1
Based on 1 Customer Validation
PROTAC BTK Degrader-1 is a selective, orally active BTK PROTAC degrader with a DC50 of 5.8 nM. PROTAC BTK Degrader-1 induces ubiquitination and degradation of wild-type and mutant (C481S, T316) BTK proteins via the CRBN-mediated pathway. PROTAC BTK Degrader-1 exhibits anticancer activity against diffuse large B-cell lymphoma. PROTAC BTK Degrader-1 can be used in lymphoma-related research.
(Pink: Btk ligand (HY-150885); Blue: Cereblon ligand (HY-138793); Black: linker).
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity : 99.92%
- CAS No.: 2801715-13-7
- 화학식: C43H43N9O4
- 분자량:749.86
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보관:
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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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
제품 설명
IC50 & Target
[1]|
Cereblon |
Cellular Effect
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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] |
In Vitro
PROTAC BTK Degrader-1 (Compound C13) (0.1-1000 nM; 24 h) potently degrades BTK protein in Mino cells with a DC50 of 5.8 nM and 96% maximal degradation after 24 h of treatment[1].
PROTAC BTK Degrader-1 (1-1000 nM) dose-dependently degrades the Ibrutinib (HY-10997)-resistant BTKT316A mutant protein in transfected HEK293 cells[1].
PROTAC BTK Degrader-1 (3-7 days) potently inhibits the growth of OCI-ly10 (IC50 = 5.9 nM) and TMD8 (IC50 = 4.7 nM) hematologic cancer cells, with minimal activity against MM.1S cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
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Cell Line:Mino human lymphoma cells
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Concentration:0.1-1000 nM
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Incubation Time:24 h
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Result:Dose-dependently degraded BTK protein with a half-maximal degradation concentration (DC50) of 5.8 nM and a maximal degradation (Dₘₐₓ) of 96% after 24 h.
Showed a hook effect at higher concentrations (500 and 1000 nM), where degradation efficacy decreased.
Parmacokinetics
In Vivo
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, 30 mg/kg
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Administration:p.o., twice daily for 17 days
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Result:Strongly and dose-dependently
decreased BTK protein levels.
Effectively penetrate and function in tumor tissue.
Inhibited tumor growth by 50.9% (10 mg/kg) and 96.9% (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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분자량 749.86
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
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)
용액&용해도
In Vitro:
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)
순도&문서
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Data Sheet (288 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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