GNE-987 |
Catalog No.GC60883
One-Click Copy Product Info
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GNE-987은 von Hippel-Lindau 및 BRD4에 대한 리간드로 연결된 PROTAC입니다. GNE-987은 피코몰 세포 BRD4 분해 활성을 나타낸다(EOL-1 AML 세포주의 경우 DC50=0.03 nM). GNE-987은 낮은 나노몰 친화도로 BRD4의 BD1 및 BD2 브로모도메인에 동등하게 결합합니다(각각 IC50=4.7 및 4.4nM). GNE-987은 강력한 BET 결합제/억제제, VHL 결합 단편 및 10개의 메틸렌 스페이서 부분을 통합합니다. GNE-987은 PROTAC-항체 접합체(PAC)에 사용할 수 있습니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2417371-71-0
Sample solution is provided at 25 µL, 10mM.
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GNE-987 is a highly active chimeric BET degrader. GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50=0.03 nM for EOL-1 AML cell line). GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC50=4.7 and 4.4 nM, respectively). GNE-987 incorporates a potent BET binder/inhibitor, a VHL-binding fragment, and a ten methylene spacer moiety. GNE-987 can be used in PROTAC-Antibody Conjugate (PAC)[1].
GNE-987 inhibits EOL-1 and HL-60 cell viability with IC50s of 0.02 and 0.03 nM, respectively, and inhibits MYC expression with an IC50 of 0.03 nM[1]. GNE-987 (0.1-10 nM; 5 hours) degrades the BRD2 and BRD3 BET family proteins[1]. Western Blot Analysis[1] Cell Line: EOL-1 cells
[1]. Pillow TH, et al. Antibody Conjugation of a Chimeric BET Degrader Enables in vivo Activity. ChemMedChem. 2019 Oct 31.
| Cas No. | 2417371-71-0 | SDF | |
| Canonical SMILES | O=C([C@H](C[C@@H](O)C1)N1C([C@@H](NC(CCCCCCCCCCNC(C2=C(CS(=O)(C)=O)C=C(C(N(C3=NC=C(F)C=C3F)C4)=C2)C5=CN(C)C(C6=C5C4=CN6)=O)=O)=O)C(C)(C)C)=O)NCC7=CC=C(C(SC=N8)=C8C)C=C7 | ||
| Formula | C56H67F2N9O8S2 | M.Wt | 1096.31 |
| Solubility | DMSO: 150 mg/mL (136.82 mM) | Storage | 4°C, stored under nitroge |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 912.2 μL | 4.5608 mL | 9.1215 mL |
| 5 mM | 182.4 μL | 912.2 μL | 1.8243 mL |
| 10 mM | 91.2 μL | 456.1 μL | 912.2 μL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 36 reference(s) in Google Scholar.)