CG428

Cat. No.: HY-137465: FAQs
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CG428 is a potent and selective 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 PLCγ1phosphorylation (IC₅₀ = 0.33 nM). CG428 has a higher binding affinity for TRKA than TRKB and TRKC (K_d = 1 nM, 28 nM and 4.2 nM, respectively). In addition, CG428 effectively inhibits KM12 cell growth (IC₅₀ = 2.9 nM).(Pink: TRK inhibitor (HY-118271); Black: linker (HY-W067489); Blue: CRBN Ligand (HY-41547))

For research use only. We do not sell to patients.

CG428 Chemical Structure

CAS No. : 2412055-93-5

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TrkA TrkB TrkC Trk

Biological Activity
Purity & Documentation
References
Customer Review

Description

CG428 is a potent and selective 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 PLCγ1phosphorylation (IC₅₀ = 0.33 nM). CG428 has a higher binding affinity for TRKA than TRKB and TRKC (K_d = 1 nM, 28 nM and 4.2 nM, respectively). In addition, CG428 effectively inhibits KM12 cell growth (IC₅₀ = 2.9 nM)^[1].(Pink: TRK inhibitor (HY-118271); Black: linker (HY-W067489); Blue: CRBN Ligand (HY-41547))

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]

Molecular Weight

814.86

Formula

C₄₃H₄₃FN₁₀O₆

CAS No.

2412055-93-5

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

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

CG428 Related Classifications

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Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CG4282412055-93-5CG 428CG-428PROTACsTrk ReceptorTropomyosin related kinase receptorTPM3-TRKATRK degraderKM12pPLCγ1TRKATRKBTRKCanti-tumorInhibitorinhibitorinhibit

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