PROTAC BRD9 Degrader-7
Based on 1 Customer Validation
PROTAC BRD9 Degrader-7 is an orally active, selective BRD9 PROTAC degrader (DC50 = 1.02 nM). PROTAC BRD9 Degrader-7 mediates BRD9 degradation via the ubiquitin-proteasome system. PROTAC BRD9 Degrader-7 exhibits proliferation inhibitory activity in the MV4-11 cells. PROTAC BRD9 Degrader-7 can be used in the research of acute myeloid leukemia and other related malignancies.
(Pink: BRD9 ligand (HY-123616); Blue: Cereblon ligand (HY-W023573); Black: linker).
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity : 99.24%
- CAS No.: 3056013-04-5
- 화학식: C36H35N5O7
- 분자량:649.69
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보관:Powder -20°C, 3 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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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
All PROTACs Isoforms
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Biological Activity
제품 설명
IC50 & Target
[1]|
Cereblon |
BRD9 1.02 nM (DC50) |
In Vitro
PROTAC BRD9 Degrader-7 (Compound C6) (1-100 nM) exhibits potent BRD9 degradation activity in MV4-11 cells, with degradation rates of 93% at 10 nM and 99% at 100 nM[1].
PROTAC BRD9 Degrader-7 (0.0045-10 nM, 0-24 h) degrades BRD9 in a dose- and time-dependent manner in MV4-11 cells[1].
PROTAC BRD9 Degrader-7 (7 days) shows cytotoxicity against MV4-11, MOLM-13 cells, with IC50s of 3.69, 21.03 nM, has no cytotoxicity against HEL, K562, HL-60 cells[1].
PROTAC BRD9 Degrader-7 (0.1-100 nM) does not induce degradation of BRD4 and BRD7 proteins in MV4-11 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:MV4-11 cells
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Concentration:0.0045, 0.013, 0.041, 0.12, 0.33, 0.37, 1.11, 3.33, 10 nM
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Incubation Time:0, 0.5, 1, 2, 4, 6, 9, 12, 24 h
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Result:Degraded BRD9 in a dose- and time-dependent manner, effectively reduced BRD9 protein levels at 2 h, achieving a degradation rate of 91.32% after 4 h, completely degraded BRD9 protein at 0.33 nM for 24 h.
Parmacokinetics
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC0-t |
|---|---|---|---|---|---|---|
| Mice[1] | 20 mg/kg | i.g. | 8.8 h | 2 h | 3436.95 ng/mL | 17749.45 ng·h/mL |
Chemical Information
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CAS No. 3056013-04-5
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Appearance Solid
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분자량 649.69
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화학식 C36H35N5O7
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Color Light yellow to yellow
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SMILES
O=C(N(C)C=C1C2=CC(OC)=C(CN3CCN(C4=CC=C5C(C(N(C6C(NC(CC6)=O)=O)C5=O)=O)=C4)CC3)C(OC)=C2)C7=C1C=CC=C7
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 70 mg/mL (107.74 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)
Protocol
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
순도&문서
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Data Sheet (271 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
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 | 1.5392 mL | 7.6960 mL | 15.3920 mL | 38.4799 mL |
| 5 mM | 0.3078 mL | 1.5392 mL | 3.0784 mL | 7.6960 mL | |
| 10 mM | 0.1539 mL | 0.7696 mL | 1.5392 mL | 3.8480 mL | |
| 15 mM | 0.1026 mL | 0.5131 mL | 1.0261 mL | 2.5653 mL | |
| 20 mM | 0.0770 mL | 0.3848 mL | 0.7696 mL | 1.9240 mL | |
| 25 mM | 0.0616 mL | 0.3078 mL | 0.6157 mL | 1.5392 mL | |
| 30 mM | 0.0513 mL | 0.2565 mL | 0.5131 mL | 1.2827 mL | |
| 40 mM | 0.0385 mL | 0.1924 mL | 0.3848 mL | 0.9620 mL | |
| 50 mM | 0.0308 mL | 0.1539 mL | 0.3078 mL | 0.7696 mL | |
| 60 mM | 0.0257 mL | 0.1283 mL | 0.2565 mL | 0.6413 mL | |
| 80 mM | 0.0192 mL | 0.0962 mL | 0.1924 mL | 0.4810 mL | |
| 100 mM | 0.0154 mL | 0.0770 mL | 0.1539 mL | 0.3848 mL |
PROTAC BRD9 Degrader-7 Related Classifications
HY-155361 Related Classifications
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