DS-5272

Cat. No.: HY-120667: FAQs
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DS-5272 is an orally acitve inhibitor for p53-MDM2 with an IC₅₀ of 20 nM. DS-5272 inhibits the proliferation of SJSA-1 (wildtype p53, IC₅₀=0.17 μM) and DLD-1 (mutant p53). DS-5272 arrest the cell cycle, and induces apoptosis in SJSA-1. DS-5272 exhibits antitumor efficacy in mice.

For research use only. We do not sell to patients.

DS-5272 Chemical Structure

CAS No. : 1235575-97-9

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Description

IC₅₀ & Target

IC₅₀: 20 nM (p53-MDM2 interaction)

Cellular Effect

Cell Line	Type	Value	Description	References
DLD-1	GI₅₀	> 50 μM Compound: 8, DS-5272	Antiproliferative activity against human DLD1 cells expressing mutant p53 after 3 days by luminescent cell viability assay Antiproliferative activity against human DLD1 cells expressing mutant p53 after 3 days by luminescent cell viability assay	[PMID: 25882531]
SJSA-1	GI₅₀	0.17 μM Compound: 8, DS-5272	Antiproliferative activity against human SJSA1 cells expressing wildtype p53 after 3 days by luminescent cell viability assay Antiproliferative activity against human SJSA1 cells expressing wildtype p53 after 3 days by luminescent cell viability assay	[PMID: 25882531]

Molecular Weight

703.67

Formula

C₃₄H₃₈Cl₂F₂N₆O₂S

CAS No.

1235575-97-9

SMILES

O=C([C@H]1N(C(C2=C(C(C)C)N3C(S2)=N[C@@](C)(C4=CC=C(Cl)N=C4)[C@H]3C5=CC=C(Cl)C(F)=C5)=O)C[C@H](F)C1)N(C6)[C@H](CC)CNC76CC7

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Miyazaki M, et al., Discovery of DS-5272 as a promising candidate: A potent and orally active p53-MDM2 interaction inhibitor. Bioorg Med Chem. 2015 May 15;23(10):2360-7. [Content Brief]

DS-5272 Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DS-52721235575-97-9DS5272DS 5272MDM-2/p53ApoptosisSJSA-1DLD-1,BALB/c mouseorally activeInhibitorinhibitorinhibit

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