TargetMol

Siremadlin

Product Code:
 
TAR-T5555
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
1 / 1
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CodeSizePrice
TAR-T5555-1mg1mg£119.00
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TAR-T5555-5mg5mg£177.00
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TAR-T5555-1mL1 mL * 10 mM (in DMSO)£203.00
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TAR-T5555-10mg10mg£229.00
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TAR-T5555-25mg25mg£361.00
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TAR-T5555-50mg50mg£547.00
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This product comes from: United States.
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Further Information

Bioactivity:
Siremadlin is a potent, orally bioavailable and highly specific p53-MDM2 interaction inhibitor.
CAS:
1448867-41-1
Formula:
C26H24Cl2N6O4
Molecular Weight:
555.42
Pathway:
Ubiquitination
Purity:
0.98
SMILES:
COc1ncc(-c2nc3C(=O)N([C@H](c3n2C(C)C)c2ccc(Cl)cc2)c2cc(Cl)cn(C)c2=O)c(OC)n1
Target:
E1/E2/E3 Enzyme

References

St?phane F, et al. Abstract 1224: Insights into the mechanism of action of NVP-HDM201, a differentiated and versatile Next-Generation small-molecule inhibitor of Mdm2, under evaluation in phase I clinical trials. Insights into the mechanism of action of NVP-HDM201, a differentiated and versatile Next-Generation small-molecule inhibitor of Mdm2, under evaluation in phase I clinical trials. [abstract]. In: Proceedings of the 107th Annual Meeting of the American Association for Cancer Research; 2016 Apr 16-20; New Orleans, LA. Philadelphia (PA): AACR; Cancer Res 2016;76(14 Suppl):Abstract nr 1224. Furet P, et al. Discovery of a novel class of highly potent inhibitors of the p53-MDM2 interaction by structure-based design starting from a conformational argument. Bioorg Med Chem Lett. 2016 Oct 1;26(19):4837-41. Chapeau EA, et al. Resistance mechanisms to TP53-MDM2 inhibition identified by in vivo piggyBac transposon mutagenesis screen in an Arf-/- mouse model. Proc Natl Acad Sci U S A. 2017 Mar 21;114(12):3151-3156.