| Identification | Back Directory | [Name]
YH239-EE | [CAS]
1364488-67-4 | [Synonyms]
CS-1286
YH239-EE
YH239-EE USP/EP/BP
YH 239-EE;YH 239 EE
Ethyl 3-[2-(tert-Butylamino)-1-[N-(4-chlorobenzyl)formamido]-2-oxoet
Ethyl 3-(2-(tert-butylamino)-1-(N-(4-chlorobenzyl)formamido)-2-oxoethyl)-6-chloro-1H-indole-2-
Ethyl 3-(2-(tert-butylamino)-1-(N-(4-chlorobenzyl)formamido)-2-oxoethyl)-6-chloro-1H-indole-2-carboxylate
ethyl 3-[2-(tert-butylamino)-1-[(4-chlorophenyl)methyl-formylamino]-2-oxoethyl]-6-chloro-1H-indole-2-carboxylate
1H-Indole-2-carboxylic acid, 6-chloro-3-[1-[[(4-chlorophenyl)methyl]formylamino]-2-[(1,1-dimethylethyl)amino]-2-oxoethyl]-, ethyl ester
YH239-EE ethyl 3-[2-(tert-butylamino)-1-[(4-chlorophenyl)methyl-formylamino]-2-oxoethyl]-6-chloro-1H-indole-2-carboxylate
YH239-EE 6-Chloro-3-[1-[[(4-chlorophenyl)methyl]formylamino]-2-[(1,1-dimethylethyl)amino]-2-oxoethyl]-1H-indole-2-carboxylic acid Ethyl Ester | [Molecular Formula]
C25H27Cl2N3O4 | [MDL Number]
MFCD28099816 | [MOL File]
1364488-67-4.mol | [Molecular Weight]
504.42 |
| Chemical Properties | Back Directory | [Boiling point ]
763.3±60.0 °C(Predicted) | [density ]
1.313±0.06 g/cm3(Predicted) | [storage temp. ]
Desiccate at -20°C | [solubility ]
≥50.4 mg/mL in DMSO; insoluble in H2O; ≥4.26 mg/mL in EtOH with ultrasonic | [form ]
solid | [pka]
13.20±0.30(Predicted) |
| Hazard Information | Back Directory | [Uses]
YH239-EE, the ethyl ester of YH239, is a potent p53-MDM2 antagonist and an apoptosis inducer. | [Biological Activity]
yh239-ee is a potent antagonist of p53-mdm2 [1].p53 is a transcription factor and functions as a tumor suppressor. mdm2 is a negative regulator of p53. the interaction of p53 and mdm2 has emerged as a novel target for anticancer drugs [1].yh239-ee is a potent p53-mdm2 antagonist. in oci-aml-3 cells, yh239-ee potently inhibited cell proliferation. in aml cell lines, yh239-ee induced a cell cycle arrest and cell accumulation in the sub-g1 phase. yh239-ee induced apoptosis by 11.8-fold, 5.6-fold and 13.1-fold in oci-aml-3, molm-13 and nb4 aml cell lines, respectively. in molm-13 cells, yh239 exhibited almost no apoptotic effect. however, yh239-ee significantly induced apoptosis. in molm-13 cells, (+)-yh239-ee and (?)-yh239-ee inhibited metabolic activity with ec50 values of 7.5 μm and 25.2 μm and induced apoptosis with 13.7% and 51.5% viable cells, respectively. (+)-yh239-ee (20 μm) induced p53 and significantly activated caspase 3 and 7 [1]. | [target]
p53-MDM2 | [storage]
Store at -20°C | [References]
[1]. huang y, wolf s, beck b, et al. discovery of highly potent p53-mdm2 antagonists and structural basis for anti-acute myeloid leukemia activities. acs chem biol, 2014, 9(3): 802-811. |
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| Company Name: |
SPIRO PHARMA
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| Tel: |
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| Website: |
www.spiropharma.com.cn |
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