ChemicalBook > CAS DataBase List > GEN272
GEN272
- Product Name
- GEN272
- CAS No.
- 1936428-93-1
- Chemical Name
- GEN272
- Synonyms
- GEN272;GNE-272;GNE272;GNE 272;(S)-1-(3-((2-FLUORO-4-(1-METHYL-1H-PYRAZOL-4-YL)PHENYL)AMINO)-1-(TETRAHYDROFURAN-3-YL)-1,4,6,7-TETRAHYDRO-5H-PYRAZOLO[4,3-C]PYRIDIN-5-YL)ETHAN-1-ONE;Ethanone, 1-[3-[[2-fluoro-4-(1-methyl-1H-pyrazol-4-yl)phenyl]amino]-1,4,6,7-tetrahydro-1-[(3S)-tetrahydro-3-furanyl]-5H-pyrazolo[4,3-c]pyridin-5-yl]-
- CBNumber
- CB93339885
- Molecular Formula
- C22H25FN6O2
- Formula Weight
- 424.47
- MOL File
- 1936428-93-1.mol
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GEN272 Property
- Boiling point:
- 645.3±55.0 °C(Predicted)
- Density
- 1.43±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : ≥ 150 mg/mL (353.38 mM)
- form
- Solid
- pka
- 1.98±0.20(Predicted)
- color
- White to off-white
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N-Bromosuccinimide Price
ChemScene
- Product number
- CS-7493
- Product name
- GNE-272
- Purity
- 99.74%
- Packaging
- 2mg
- Price
- $132
- Updated
- 2021/12/16
ChemScene
- Product number
- CS-7493
- Product name
- GNE-272
- Purity
- 99.74%
- Packaging
- 5mg
- Price
- $228
- Updated
- 2021/12/16
ChemScene
- Product number
- CS-7493
- Product name
- GNE-272
- Purity
- 99.74%
- Packaging
- 10mg
- Price
- $360
- Updated
- 2021/12/16
ChemScene
- Product number
- CS-7493
- Product name
- GNE-272
- Purity
- 99.74%
- Packaging
- 50mg
- Price
- $1140
- Updated
- 2021/12/16
Alichem
- Product number
- 1936428931
- Product name
- (S)-1-(3-((2-fluoro-4-(1-methyl-1h-pyrazol-4-yl)phenyl)amino)-1-(tetrahydrofuran-3-yl)-1,4,6,7-tetrahydro-5h-pyrazolo[4,3-c]pyridin-5-yl)ethan-1-one
- Packaging
- 250mg
- Price
- $540.75
- Updated
- 2021/12/16
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GEN272 Chemical Properties,Usage,Production
Uses
GNE-272 is a potent and selective CBP/EP300 inhibitor with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively. GNE-272 is also a selective in vivo probe for CBP/EP300[1].
in vivo
GNE-272 demonstrates low clearance following a 1 mg/ kg intravenous dose in a mouse PK experiment and good oral bioavailability when dosed at 100 mg/kg, reaching an unbound Cmax of 26 μM. GNE-272 shows a marked antiproliferative effect in hematologic cancer cell lines and modulates MYC expression in vivo that corresponds with antitumor activity in an AML tumor model[1].
IC 50
CBP/p300
References
[1] Crawford TD, et al. Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300. J Med Chem. 2016 Dec 8;59(23):10549-10563. DOI:10.1021/acs.jmedchem.6b01022
GEN272 Preparation Products And Raw materials
Raw materials
Preparation Products
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