MD-224
- Product Name
- MD-224
- CAS No.
- 2136247-12-4
- Chemical Name
- MD-224
- Synonyms
- MD-224;MD-224, 10 mM in DMSO;11,E1/E2/E3 Enzyme,leukemia,PROTACs,E2 conjugating enzyme,MD 224;MD224,inhibit,PROTAC,Ubiquitin activating enzyme,Ubiquitin ligase,Inhibitor,MDM-2/p53,cancer,MD-224,E1 activating enzyme,Ubiquitin conjugating enzyme,E3 ligating enzyme,RS4;(3'R,4'S,5'R)-6''-Chloro-4'-(3-chloro-2-fluorophenyl)-N-(4-((5-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)pent-4-yn-1-yl)carbamoyl)phenyl)-2''-oxodispiro[cyclohexane-1,2'-pyrrolidine-3',3''-indoline]-5'-carboxamide;(3'R,4'S,5'R)-6''-Chloro-4'-(3-chloro-2-fluorophenyl)-N-(4-((5-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)pent-4-yn-1-yl)carbamoyl)phenyl)-2''-oxodispiro[cyclohexane-1,2'-pyrrolidine-3',3''-indoline]-5'-carboxamide;(3'R,4'S,5'R)-6''-Chloro-4'-(3-chloro-2-fluorophenyl)-N-(4-((5-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)pent-4-yn-1-yl)carbamoyl)phenyl)-2''-oxodispiro[cyclohexane-1,2'-pyrrolidine-3',3''-indoline]-5'-carboxamide , MD-224;(3'R,4'S,5'R)-6''-Chloro-4'-(3-chloro-2-fluorophenyl)-N-[4-[[[5-[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1-oxo-1H-isoindol-4-yl]-4-pentyn-1-yl]amino]carbonyl]phenyl]-1'',2''-dihydro-2''-oxodispiro[cyclohexane-1,2'-pyrrolidine-3',3''-[3H]indole]-5'-carboxamide;Dispiro[cyclohexane-1,2'-pyrrolidine-3',3''-[3H]indole]-5'-carboxamide, 6''-chloro-4'-(3-chloro-2-fluorophenyl)-N-[4-[[[5-[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1-oxo-1H-isoindol-4-yl]-4-pentyn-1-yl]amino]carbonyl]phenyl]-1'',2''-dihydro-2''-oxo-, (3'R,4'S,5'R)-
- CBNumber
- CB25821231
- Molecular Formula
- C48H43Cl2FN6O6
- Formula Weight
- 889.81
- MOL File
- 2136247-12-4.mol
MD-224 Property
- Density
- 1.49±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:100.0(Max Conc. mg/mL);112.38(Max Conc. mM)
- form
- Solid
- pka
- 10.67±0.40(Predicted)
- color
- Light yellow to yellow
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- CS-0082057
- Product name
- MD-224
- Purity
- 99.74%
- Packaging
- 5mg
- Price
- $190
- Updated
- 2021/12/16
- Product number
- CS-0082057
- Product name
- MD-224
- Purity
- 99.74%
- Packaging
- 10mg
- Price
- $350
- Updated
- 2021/12/16
- Product number
- CS-0082057
- Product name
- MD-224
- Purity
- 99.74%
- Packaging
- 25mg
- Price
- $650
- Updated
- 2021/12/16
- Product number
- CS-0082057
- Product name
- MD-224
- Purity
- 99.74%
- Packaging
- 50mg
- Price
- $950
- Updated
- 2021/12/16
- Product number
- CS-0082057
- Product name
- MD-224
- Purity
- 99.74%
- Packaging
- 100mg
- Price
- $1750
- Updated
- 2021/12/16
MD-224 Chemical Properties,Usage,Production
Uses
MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 consists of ligands for Cereblon and MDM2. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent[1]. MD-224 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
IC 50
MDM2: 1 nM (IC50)
References
[1] Li Y, et al. Discovery of MD-224 as a First-in-Class, Highly Potent, and Efficacious Proteolysis TargetingChimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable TumorRegression. J Med Chem. 2019 Jan 24;62(2):448-466 DOI:10.1021/acs.jmedchem.8b00909
MD-224 Preparation Products And Raw materials
Raw materials
Preparation Products
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