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Art. -Nr.: HY-137465

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CG428

Name: CG428
Brand: MedChemExpress
SKU: HY-137465
Price: 215.00 USD
Availability: InStock
Rating: 5 (1 reviews)

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CG428 is a potent and selective CRBN-dependent tropomyosin receptor kinase (TRK) PROTAC degrader that has anti-tumor activity. CG428 reduces levels of the tropomyosin 3 TPM3-TRKA fusion protein in KM12 colorectal carcinoma cells (DC₅₀ = 0.36 nM) and inhibits downstream PLCγ1 phosphorylation (IC₅₀ = 0.33 nM). CG428 has a higher binding affinity for TRKA than TRKB and TRKC (Kd = 1 nM, 28 nM and 4.2 nM, respectively). CG428 can be used for the research of colorectal carcinoma.
(Pink: Trk Receptor ligand (HY-118271); Blue: Cereblon ligand (HY-41547); Black: linker (HY-W067489)).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit : 98.18%
CAS. Nr.: 2412055-93-5
Formel: C₄₃H₄₃FN₁₀O₆
Molecular Weight:814.86

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

CG428 Chemical Structure

CAS. Nr.: 2412055-93-5

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Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

CG428 is a potent and selective CRBN-dependent tropomyosin receptor kinase (TRK) PROTAC degrader that has anti-tumor activity. CG428 reduces levels of the tropomyosin 3 TPM3-TRKA fusion protein in KM12 colorectal carcinoma cells (DC₅₀ = 0.36 nM) and inhibits downstream PLCγ1 phosphorylation (IC₅₀ = 0.33 nM). CG428 has a higher binding affinity for TRKA than TRKB and TRKC (Kd = 1 nM, 28 nM and 4.2 nM, respectively). CG428 can be used for the research of colorectal carcinoma^[1]. (Pink: Trk Receptor ligand (HY-118271); Blue: Cereblon ligand (HY-41547); Black: linker (HY-W067489)).

IC₅₀ & Target

^[1]

TrkA

1 nM (Kd)

TrkC

4.2 nM (Kd)

TrkB

28 nM (Kd)

Cereblon

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Trk Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
KM12	IC₅₀	52 nM Compound: 6; CG428	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 binds with high affinity to recombinant TRKA, TRKB, and TRKC kinases, with K_d values of 1.0, 28.0 and 4.2 nM^[1].
CG428 degrades endogenous TPM3-TRKA fusion protein (DC50 = 0.36 nM) and inhibits PLCγ1 phosphorylation (IC₅₀ = 0.33 nM) in KM12 cells^[1].
CG428 potently degrades endogenous wild-type TRKA in HEL cells with a DC₅₀ of 2.23 nM^[1].
CG428 (0.7-500 nM; 6 h) exhibits reduced potency for degradation of ectopically expressed AGBL4-TRKB and ETV6-TRKC fusion protein in KM12 cells, with a hook effect at high concentrations^[1].
CG428 potently inhibits the growth of KM12 cells with an IC₅₀ of 2.9 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
Concentration:

0.04, 0.12, 0.4, 1.1, 3.3, 10, 30 nM
Incubation Time:

6 h
Result:

Induced potent degradation of TPM3-TRKA with a DC₅₀ of 0.36 ± 0.06 nM.
Inhibited downstream PLCγ1 phosphorylation with an IC₅₀ of 0.33 ± 0.06 nM.
Caused 96 ± 3% TPM3-TRKA degradation at 10 nM.
Caused 82 ± 2% TPM3-TRKA degradation at 1 nM.
Caused 46 ± 6% TPM3-TRKA degradation at 0.1 nM.

Parmacokinetics

Species	Dose	Route	C_max	T_max	T_1/2
Mice^[1]	10 mg/kg	i.p.	1640 nM	1 h	0.9 h

In Vivo

CG428 (10 mg/kg; i.p.; single dose) demonstrates good plasma exposure in male ICR mice following a single 10 mg/kg intraperitoneal administration, with concentrations remaining well above its in vitro DC₅₀ up to 8 h post dosing^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

ICR (male)^[1]
Dosage:

10 mg/kg
Administration:

i.p.; single dose
Result:

Reached a maximum plasma concentration of 1640 ± 120 nM at 1 h post dosing.
Plasma concentration was 12.4 ± 13.6 nM at 8 h post dosing.
Exhibited a half-life of 0.9 h.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 2412055-93-5
Appearance Solid
Molecular Weight 814.86
Formel C₄₃H₄₃FN₁₀O₆
Color Light yellow to yellow
SMILES

O=C1N(C(CC2)C(NC2=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
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (122.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.2272 mL

6.1360 mL

12.2720 mL

5 mM

0.2454 mL

1.2272 mL

2.4544 mL

10 mM

0.1227 mL

0.6136 mL

1.2272 mL

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.

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)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
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)
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. J Med Chem. 2020;63(23):14562-14575. [Content Brief]

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.

Complete Stock Solution Preparation Table

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	1.2272 mL	6.1360 mL	12.2720 mL	30.6801 mL
	5 mM	0.2454 mL	1.2272 mL	2.4544 mL	6.1360 mL
	10 mM	0.1227 mL	0.6136 mL	1.2272 mL	3.0680 mL
	15 mM	0.0818 mL	0.4091 mL	0.8181 mL	2.0453 mL
	20 mM	0.0614 mL	0.3068 mL	0.6136 mL	1.5340 mL
	25 mM	0.0491 mL	0.2454 mL	0.4909 mL	1.2272 mL
	30 mM	0.0409 mL	0.2045 mL	0.4091 mL	1.0227 mL
	40 mM	0.0307 mL	0.1534 mL	0.3068 mL	0.7670 mL
	50 mM	0.0245 mL	0.1227 mL	0.2454 mL	0.6136 mL
	60 mM	0.0205 mL	0.1023 mL	0.2045 mL	0.5113 mL
	80 mM	0.0153 mL	0.0767 mL	0.1534 mL	0.3835 mL
	100 mM	0.0123 mL	0.0614 mL	0.1227 mL	0.3068 mL

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise

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Art. -Nr.:
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CG428

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Trk Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Beschreibung

IC50 & Target

Cellular Effect

In Vitro

Parmacokinetics

In Vivo

Clinical Trial

Chemical Information

Lösungsmittel & Löslichkeit

In Vitro:

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CG428 Related Classifications

HY-137465 Related Classifications

Bioz

Keywords

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