PROTAC BTK Degrader-16
Based on 1 Customer Validation
PROTAC BTK Degrader-16 is a BTK PROTAC degrader with a DC50 of 0.0006 nM in TMD8 cells. PROTAC BTK Degrader-16 recruits E3 ligase CRBN to tag BTK for degradation, leading to loss of BTK signaling. PROTAC BTK Degrader-16 induces degradation of BTK, leading to inhibition of cell growth in ABC-DLBCL cells. PROTAC BTK Degrader-16 can be used for the research of activated b-cell-like diffuse large b-cell lymphoma (ABC-DLBCL).
(Pink: Target protein ligand; Blue: E3 ligase ligand; Black: linker).
For research use only. We do not sell to patients.
- Purity: 98.72%
- CAS No.: 2377645-56-0
- Formula: C52H54F2N8O6
- Molecular Weight:925.03
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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
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| TMD8 | GI50 |
0.290 nM
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Growth inhibition against human ABC-DLBCL TMD8 cells assessed as reduction in total cell growth incubated for 120 hrs by Cell Titer-Glo (CTG) assay.
Growth inhibition against human ABC-DLBCL TMD8 cells assessed as reduction in total cell growth incubated for 120 hrs by Cell Titer-Glo (CTG) assay.
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38265691 |
| TMD8 | DC50 |
0.022 nM
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Half-maximal degradation of BTK-eGFP fusion protein in engineered human ABC-DLBCL TMD8 cells incubated for 48 hrs by fluorescence-activated cell sorting (FACS) assay.
Half-maximal degradation of BTK-eGFP fusion protein in engineered human ABC-DLBCL TMD8 cells incubated for 48 hrs by fluorescence-activated cell sorting (FACS) assay.
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38265691 |
| TMD8 | DC50 |
0.0006 nM
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Half-maximal degradation of endogenous BTK protein in human ABC-DLBCL TMD8 cells incubated for 48 hrs by Meso Scale Discovery (MSD) assay.
Half-maximal degradation of endogenous BTK protein in human ABC-DLBCL TMD8 cells incubated for 48 hrs by Meso Scale Discovery (MSD) assay.
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38265691 |
In Vitro
PROTAC BTK Degrader-16 (compound 1) (120 h) potently inhibits the growth of TMD8 cells with a GI50 of 0.290 nM[1].
PROTAC BTK Degrader-16 (48 h) mediates half-maximal degradation of BTK-eGFP in engineered TMD8 cells with a DC50 of 0.022 nM[1].
PROTAC BTK Degrader-16 (48 h) potently degrades endogenous BTK in TMD8 cells with a DC50 of 0.0006 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | Cmax |
|---|---|---|---|
| Mice[1] | 20 mg/kg | i.v. | 13 μM |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2377645-56-0
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Appearance Solid
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Molecular Weight 925.03
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Formula C52H54F2N8O6
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Color White to off-white
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SMILES
O=C(C1=CC=C(C(C)(C)O)C=C1F)NC2=CC(F)=CC(C3=C4C=C(C5=CC=C(CCN6CCC7(CC6)CCN(CC7)C(C8=CC=C(C(N9C(NC(CC9)=O)=O)=C8)OC)=O)C=C5)NC4=NC=N3)=C2C
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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
Purity & Documentation
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Data Sheet (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC BTK Degrader-16 Related Classifications
HY-163295 Related Classifications
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