CG428-NEG
Based on 1 Customer Validation
CG428-NEG is the negative control of PROTAC CG428 (HY-137465). CG428-NEG binds to TRKA, TRKB and TRKC with high affinity, with Kd values of 0.88 nM, 4.8 nM and 59.8 nM, respectively. CG428-NEG inhibits the growth of cancer cells and reduces the level of TPM3-TRKA fusion protein in cancer cells. CG428-NEG can be used in the research of colorectal cancer.
(Pink: Trk Receptor Target protein ligand; Blue: Cereblon ligand (HY-W586822); Black: linker).
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 97.6%
- CAS No.: 2714560-39-9
- Formule: C44H45FN10O6
- Masse moléculaire:828.89
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Stockage: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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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
TrkA 0.88 nM (Kd) |
TrkB 4.8 nM (Kd) |
TrkC 59.8 nM (Kd) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| KM12 | IC50 |
28 nM
Compound: 26
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Antiproliferative activity against human KM12 cells assessed as reduction in cell viability measured after 3 days by Celltiter-Glo assay
Antiproliferative activity against human KM12 cells assessed as reduction in cell viability measured after 3 days by Celltiter-Glo assay
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[PMID: 33058680] |
In Vitro
CG428-NEG (Compound 26) (1 μM) exhibits high-affinity binding activity to human TRKA, moderate affinity to human TRKC, and lower affinity to human TRKB, with corresponding Kd values of 0.88 nM, 4.8 nM, and 59.8 nM[1].
CG428-NEG (30 nM; 6 h) reduces the level of TPM3-TRKA fusion protein in KM12 cells[1].
CG428-NEG (3 days) inhibits the growth of KM12 cells with an IC50 of 28 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:KM12 human colorectal carcinoma cells (harboring endogenous TPM3-TRKA fusion protein)
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Concentration:30 nM
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Incubation Time:6 h
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Result:Reduced TPM3-TRKA protein levels at 30 nM.
Did not affect total PLCγ1 or GSPT1 protein levels.
Chemical Information
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CAS No. 2714560-39-9
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Appearance Solid
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Masse moléculaire 828.89
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Formule C44H45FN10O6
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Color Light yellow to yellow
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SMILES
O=C1N(C(CC2)C(N(C)C2=O)=O)C(C3=C1C=CC=C3NCCOCCC(N4CCN(C5=NC(C6=CN=C7C=CC(N8[C@@H](C9=CC=CC(F)=C9)CCC8)=NN76)=CC=C5)CC4)=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Pureté et documentation
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Fiche technique (269 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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Instruction de manipulation (2659 KB)
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CG428-NEG Related Classifications
HY-157542 Related Classifications
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