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Art. -Nr.: HY-157542

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CG428-NEG

Name: CG428-NEG
Brand: MedChemExpress
SKU: HY-157542
Price: 522.00 USD
Availability: InStock
Rating: 5 (1 reviews)

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CG428-NEG is the negative control of PROTAC CG428 (HY-137465). CG428-NEG binds to TRKA, TRKB and TRKC with high affinity, with K_d 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).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit : 97.6%
CAS. Nr.: 2714560-39-9
Formel: C₄₄H₄₅FN₁₀O₆
Molecular Weight:828.89

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

CG428-NEG Chemical Structure

CAS. Nr.: 2714560-39-9

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

CG428-NEG is the negative control of PROTAC CG428 (HY-137465). CG428-NEG binds to TRKA, TRKB and TRKC with high affinity, with K_d 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^[1]. (Pink: Trk Receptor Target protein ligand; Blue: Cereblon ligand (HY-W586822); Black: linker).

IC₅₀ & Target

^[1]

TrkA

0.88 nM (Kd)

TrkB

4.8 nM (Kd)

TrkC

59.8 nM (Kd)

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Trk Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
KM12	IC₅₀	28 nM Compound: 26	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	[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 K_d 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.

Western Blot Analysis^[1]

Cell Line:

KM12 human colorectal carcinoma cells (harboring endogenous TPM3-TRKA fusion protein)
Concentration:

30 nM
Incubation Time:

6 h
Result:

Reduced TPM3-TRKA protein levels at 30 nM.
Did not affect total PLCγ1 or GSPT1 protein levels.

Chemical Information

CAS. Nr. 2714560-39-9
Appearance Solid
Molecular Weight 828.89
Formel C₄₄H₄₅FN₁₀O₆
Color Light yellow to yellow
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (269 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Chen L, et al. Discovery of First-In-Class Potent and Selective Tropomyosin Receptor Kinase Degraders. Journal of medicinal chemistry. 2020 Dec 10;63(23):14562-14575. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise

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CG428-NEG

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Trk Receptor Isoform-spezifische Produkte anzeigen