| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C44H45FN10O6 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
CG428-NEG is the negative control of the PROTAC CG428. It binds TRKA, TRKB and TRKC with high affinity, showing Kd values of 0.88 nM, 4.8 nM and 59.8 nM, respectively. The compound inhibits the growth of cancer cells and reduces the level of TPM3-TRKA fusion protein in cancer cells, and it can be used in colorectal cancer research[1]. It is supplied as a light yellow to yellow solid (C44H45FN10O6, MW 828.89) at 97.6% purity.
Physical & Chemical Properties
| CAS Number | 2714560-39-9 |
|---|---|
| Molecular Formula | C44H45FN10O6 |
| Molecular Weight | 828.89 g/mol |
| Purity | 97.6% |
| Appearance | Solid |
| 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 |
| Target | TrkA, TrkB, TrkC |
| Signaling Pathway | PROTAC; Protein Tyrosine Kinase/RTK; Neuronal Signaling |
| Storage | Powder: -20°C, 3 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
TrkA 0.88 nM (Kd) |
TrkB 4.8 nM (Kd) |
TrkC 59.8 nM (Kd) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
CG428-NEG (1 μM) binds human TRKA with high affinity, human TRKC with moderate affinity, and human TRKB with lower affinity, with Kd values of 0.88 nM, 4.8 nM, and 59.8 nM, respectively[1]. In KM12 cells, CG428-NEG (30 nM; 6 h) lowers the level of TPM3-TRKA fusion protein[1]. CG428-NEG (3 days) inhibits KM12 cell growth with an IC50 of 28 nM[1].
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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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