| Identification | Back Directory | [Name]
1-Propanesulfonamide, N-[3-[5-[[1-[3-[2-[2-[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]ethoxy]ethoxy]ethoxy]-1-oxopropyl]-4-piperidinyl]methylamino]-3-(5-pyrimidinyl)-1H-pyrrolo[3,2-b]pyridin-1-yl]-2,4-difluorophenyl]- | [CAS]
2417296-84-3 | [Synonyms]
Inhibitor,Raf,A375,HT-29,Compound 23,inhibit,BRAF-V600E,ubiquitin-proteasome system,anticancer,melanoma,Raf kinases,PROTACs
1-Propanesulfonamide, N-[3-[5-[[1-[3-[2-[2-[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]ethoxy]ethoxy]ethoxy]-1-oxopropyl]-4-piperidinyl]methylamino]-3-(5-pyrimidinyl)-1H-pyrrolo[3,2-b]pyridin-1-yl]-2,4-difluorophenyl]- | [Molecular Formula]
C48H54F2N10O10S | [MOL File]
2417296-84-3.mol | [Molecular Weight]
1001.08 |
| Chemical Properties | Back Directory | [density ]
1.48±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [form ]
Solid | [pka]
5.48±0.10(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
PROTAC BRAF-V600E degrader-1 (compound 23) is a potent PROTAC BRAF-V600E degrader whlie no degradation activity against BRAF-WT. PROTAC BRAF-V600E degrader-1 exhibits Kd values of 2.4 nM and 2 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-1 degrades BRAF-V600E via the ubiquitin-proteasome system (UPS) and inhibits the growth of melanoma cells[1]. (In the molecular structure, target protein ligand: BI-882370 (HY-107779), red part; E3 ubiquitin enzyme ligand: Pomalidomide (HY-10984), blue part; PROTAC linker: G007-LK (HY-12438), black part. | [IC 50]
BRAF-V600E: 2 nM (Kd); Braf: 2.4 nM (Kd) | [References]
[1] Han XR, et al. Discovery of Selective Small Molecule Degraders of BRAF-V600E. J Med Chem. 2020 Apr 23;63(8):4069-4080. DOI:10.1021/acs.jmedchem.9b02083 |
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NewCan Biotech Limited
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+86-0571-86912261 +86-15658003402 |
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https://www.newcanbio.com/ |
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