Serdemetan structure
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Common Name | Serdemetan | ||
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CAS Number | 881202-45-5 | Molecular Weight | 328.410 | |
Density | 1.3±0.1 g/cm3 | Boiling Point | 615.1±50.0 °C at 760 mmHg | |
Molecular Formula | C21H20N4 | Melting Point | N/A | |
MSDS | N/A | Flash Point | 325.8±30.1 °C |
Use of SerdemetanSerdemetan(JNJ-26854165) acts as a HDM2 ubiquitin ligase antagonist and also induces early apoptosis in p53 wild-type cells, inhibits cellular proliferation followed by delayed apoptosis in the absence of functional p53.IC50 value: HDM2 ubiquitin ligaseTarget: in vitro: JNJ 26854165 is a novel tryptamine derivative which activates p53 and acts as a HDM2 ubiquitin ligase antagonist. JNJ 26854165 inhibits cell growth and induces apoptosis in leukemia cell lines with IC50 values of 0.24, 0.33, 0.32 and 0.44 μM at 72 hours for OCI-AML-3, MOLM-13, NALM-6 and REH cells, respectively. In addition, JNJ 26854165 accelerates proteasome-mediated degradation of p21 and antagonizes the transcriptional induction of p21 by p53. It also induces S-phase delay and upregulates E2F1 expression in p53 mutant cells, resulting in preferential apoptosis of S-phase cells. JNJ 26854165 is an oral Mdm2 inhibitor which can inhibit the interaction of Mdm2-p53 complex with the proteasome and increase p53 levels by binding to RING domain of Mdm2. A recent study shows that JNJ 26854165 inhibits clonogenic survival in four human cancer cell lines: H460, A549, p53-WT-HCT116, and p53-null-HCT116.in vivo:JNJ 26854165 leads to significant differences in EFS distribution in 17 of the 36 (47%) evaluable solid tumor xenografts and in 5 of 7 (71%) of the evaluable ALL xenografts using a dose of 20 mg/kg administered via oral gavage daily for 5 days, repeated for 6 weeks. |
Name | N1-(2-(1H-Indol-3-yl)ethyl)-N4-(pyridin-4-yl)benzene-1,4-diamine |
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Synonym | More Synonyms |
Description | Serdemetan(JNJ-26854165) acts as a HDM2 ubiquitin ligase antagonist and also induces early apoptosis in p53 wild-type cells, inhibits cellular proliferation followed by delayed apoptosis in the absence of functional p53.IC50 value: HDM2 ubiquitin ligaseTarget: in vitro: JNJ 26854165 is a novel tryptamine derivative which activates p53 and acts as a HDM2 ubiquitin ligase antagonist. JNJ 26854165 inhibits cell growth and induces apoptosis in leukemia cell lines with IC50 values of 0.24, 0.33, 0.32 and 0.44 μM at 72 hours for OCI-AML-3, MOLM-13, NALM-6 and REH cells, respectively. In addition, JNJ 26854165 accelerates proteasome-mediated degradation of p21 and antagonizes the transcriptional induction of p21 by p53. It also induces S-phase delay and upregulates E2F1 expression in p53 mutant cells, resulting in preferential apoptosis of S-phase cells. JNJ 26854165 is an oral Mdm2 inhibitor which can inhibit the interaction of Mdm2-p53 complex with the proteasome and increase p53 levels by binding to RING domain of Mdm2. A recent study shows that JNJ 26854165 inhibits clonogenic survival in four human cancer cell lines: H460, A549, p53-WT-HCT116, and p53-null-HCT116.in vivo:JNJ 26854165 leads to significant differences in EFS distribution in 17 of the 36 (47%) evaluable solid tumor xenografts and in 5 of 7 (71%) of the evaluable ALL xenografts using a dose of 20 mg/kg administered via oral gavage daily for 5 days, repeated for 6 weeks. |
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Related Catalog | |
References |
Density | 1.3±0.1 g/cm3 |
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Boiling Point | 615.1±50.0 °C at 760 mmHg |
Molecular Formula | C21H20N4 |
Molecular Weight | 328.410 |
Flash Point | 325.8±30.1 °C |
Exact Mass | 328.168793 |
PSA | 52.74000 |
LogP | 3.45 |
Appearance of Characters | brown solid |
Vapour Pressure | 0.0±1.8 mmHg at 25°C |
Index of Refraction | 1.747 |
Storage condition | -20℃ |
HS Code | 2933990090 |
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HS Code | 2933990090 |
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Summary | 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
1,4-Benzenediamine, N-[2-(1H-indol-3-yl)ethyl]-N-4-pyridinyl- |
1-N-[2-(1H-indol-3-yl)ethyl]-4-N-pyridin-4-ylbenzene-1,4-diamine |
Serdemetan |
N-[2-(1H-Indol-3-yl)ethyl]-N'-(4-pyridinyl)-1,4-benzenediamine |
JNJ 26854165 |