Pentanamide, N-[[4-[3-[2,6-difluoro-3-[(propylsulfonyl)amino]benzoyl]-1H-pyrrolo[2,3-b]pyridin-5-yl]phenyl]methyl]-5-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]amino]-
- CAS No.
- 2417296-82-1
- Chemical Name:
- Pentanamide, N-[[4-[3-[2,6-difluoro-3-[(propylsulfonyl)amino]benzoyl]-1H-pyrrolo[2,3-b]pyridin-5-yl]phenyl]methyl]-5-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]amino]-
- Synonyms
- CG 858;PROTAC BRAF-V600E degrader-2;Pentanamide, N-[[4-[3-[2,6-difluoro-3-[(propylsulfonyl)amino]benzoyl]-1H-pyrrolo[2,3-b]pyridin-5-yl]phenyl]methyl]-5-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]amino]-
- CBNumber:
- CB111475616
- Molecular Formula:
- C42H39F2N7O8S
- Molecular Weight:
- 839.86
- MDL Number:
- MOL File:
- 2417296-82-1.mol
- MSDS File:
- SDS
- TDS File:
- TDS
Pentanamide, N-[[4-[3-[2,6-difluoro-3-[(propylsulfonyl)amino]benzoyl]-1H-pyrrolo[2,3-b]pyridin-5-yl]phenyl]methyl]-5-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]amino]- Properties
| Density | 1.470±0.06 g/cm3(Predicted) |
|---|---|
| solubility | DMSO:83.99(Max Conc. mg/mL);100.0(Max Conc. mM) |
| pka | 6.27±0.10(Predicted) |
Pentanamide, N-[[4-[3-[2,6-difluoro-3-[(propylsulfonyl)amino]benzoyl]-1H-pyrrolo[2,3-b]pyridin-5-yl]phenyl]methyl]-5-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]amino]- price
Pentanamide, N-[[4-[3-[2,6-difluoro-3-[(propylsulfonyl)amino]benzoyl]-1H-pyrrolo[2,3-b]pyridin-5-yl]phenyl]methyl]-5-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]amino]- Chemical Properties, Uses, Production
Description
CG 858 is a selective BRAF-V600E protein Degrader (uSMITETM). CG 858 comprises the BRAF kinase inhibitor vemurafenib linked to the E3 ligase ligand Thalidomide. CG 858 dose-dependently degrades BRAF-V600E but not wild type BRAF, and reduces cell viability and colony formation in HT-29 and A375 cells (DC50 values are 124 nM and 500 nM, respectively). It exhibits 88% degradation at 500 nM. CG 858 also impairs melanoma cell growth.
Uses
PROTAC BRAF-V600E degrader-2 (compound 12) is a potent BRAF-V600E degrader with Kds of 14.4 nM and 9.5 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-2 selectively degraded the kinase domain of BRAF-V600E but not the wild-type BRAF. PROTAC BRAF-V600E degrader-2 inhibits melanoma cell growth[1].
IC 50
BRAF-V600E: 9.5 nM (Kd); Braf: 14.4 nM (Kd); Cereblon
storage
Store at -20°C
References
[1] Xiao-Ran Han, 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
Pentanamide, N-[[4-[3-[2,6-difluoro-3-[(propylsulfonyl)amino]benzoyl]-1H-pyrrolo[2,3-b]pyridin-5-yl]phenyl]methyl]-5-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]amino]- Preparation Products And Raw materials
Raw materials
Preparation Products
Pentanamide, N-[[4-[3-[2,6-difluoro-3-[(propylsulfonyl)amino]benzoyl]-1H-pyrrolo[2,3-b]pyridin-5-yl]phenyl]methyl]-5-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]amino]- Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 29874 | 58 |
| Supplier | Advantage |
|---|---|
| TargetMol Chemicals Inc. | 58 |




