1H-Isoindole-1,3(2H)-dione, 2-(2,6-dioxo-3-piperidinyl)-4-[[2-[3-[4-[6-[6-[(2R)-2-(3-fluorophenyl)-1-pyrrolidinyl]imidazo[1,2-b]pyridazin-3-yl]-2-pyridinyl]-1-piperazinyl]-3-oxopropoxy]ethyl]amino]- manufacturers
- CG 428
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- $178.00
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2026-09-10
- CAS:2412055-93-5
- Purity: 99.86%
- Supply Ability: 10g
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| | 1H-Isoindole-1,3(2H)-dione, 2-(2,6-dioxo-3-piperidinyl)-4-[[2-[3-[4-[6-[6-[(2R)-2-(3-fluorophenyl)-1-pyrrolidinyl]imidazo[1,2-b]pyridazin-3-yl]-2-pyridinyl]-1-piperazinyl]-3-oxopropoxy]ethyl]amino]- Basic information |
| Product Name: | 1H-Isoindole-1,3(2H)-dione, 2-(2,6-dioxo-3-piperidinyl)-4-[[2-[3-[4-[6-[6-[(2R)-2-(3-fluorophenyl)-1-pyrrolidinyl]imidazo[1,2-b]pyridazin-3-yl]-2-pyridinyl]-1-piperazinyl]-3-oxopropoxy]ethyl]amino]- | | Synonyms: | 1H-Isoindole-1,3(2H)-dione, 2-(2,6-dioxo-3-piperidinyl)-4-[[2-[3-[4-[6-[6-[(2R)-2-(3-fluorophenyl)-1-pyrrolidinyl]imidazo[1,2-b]pyridazin-3-yl]-2-pyridinyl]-1-piperazinyl]-3-oxopropoxy]ethyl]amino]-;CG 428;CG 428, 10 mM in DMSO;2-(2,6-Dioxo-3-piperidinyl)-4-[[2-[3-[4-[6-[6-[(2R)-2-(3-fluorophenyl)-1-pyrrolidinyl]imidazo[1,2-b]pyridazin-3-yl]-2-pyridinyl]-1-piperazinyl]-3-oxopropoxy]ethyl]amino]-1H-isoindole-1,3(2H)-dione | | CAS: | 2412055-93-5 | | MF: | C43H43FN10O6 | | MW: | 814.86 | | EINECS: | | | Product Categories: | | | Mol File: | 2412055-93-5.mol | ![1H-Isoindole-1,3(2H)-dione, 2-(2,6-dioxo-3-piperidinyl)-4-[[2-[3-[4-[6-[6-[(2R)-2-(3-fluorophenyl)-1-pyrrolidinyl]imidazo[1,2-b]pyridazin-3-yl]-2-pyridinyl]-1-piperazinyl]-3-oxopropoxy]ethyl]amino]- Structure](CAS/20210305/GIF/2412055-93-5.gif) |
| | 1H-Isoindole-1,3(2H)-dione, 2-(2,6-dioxo-3-piperidinyl)-4-[[2-[3-[4-[6-[6-[(2R)-2-(3-fluorophenyl)-1-pyrrolidinyl]imidazo[1,2-b]pyridazin-3-yl]-2-pyridinyl]-1-piperazinyl]-3-oxopropoxy]ethyl]amino]- Chemical Properties |
| density | 1.51±0.1 g/cm3(Predicted) | | solubility | Soluble to 100 mM in DMSO | | pka | 10.74±0.40(Predicted) |
| | 1H-Isoindole-1,3(2H)-dione, 2-(2,6-dioxo-3-piperidinyl)-4-[[2-[3-[4-[6-[6-[(2R)-2-(3-fluorophenyl)-1-pyrrolidinyl]imidazo[1,2-b]pyridazin-3-yl]-2-pyridinyl]-1-piperazinyl]-3-oxopropoxy]ethyl]amino]- Usage And Synthesis |
| Description | CG428 is a tropomyosin receptor kinase (TRK) degrader that targets the intracellular kinase domain of TRK. CG428 reduced levels of the tropomyosin 3 (TPM3)-TRKA fusion protein in KM12 colorectal carcinoma cells and inhibited downstream PLCγ1 signaling at sub-nanomolar concentrations. CG428 also degraded human wild-type TRKA. | | Uses | 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 (Kd = 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)) | | storage | Store at -20°C | | 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. DOI:10.1021/acs.jmedchem.0c01342 |
| | 1H-Isoindole-1,3(2H)-dione, 2-(2,6-dioxo-3-piperidinyl)-4-[[2-[3-[4-[6-[6-[(2R)-2-(3-fluorophenyl)-1-pyrrolidinyl]imidazo[1,2-b]pyridazin-3-yl]-2-pyridinyl]-1-piperazinyl]-3-oxopropoxy]ethyl]amino]- Preparation Products And Raw materials |
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