MedKoo Biosciences, Inc.
Tel:   +1-919-636-5577    Fax:   +1-919-980-4831    Email:   sales@medkoo.com
Search
Login Register
Search
MedKoo Cat#: 576218 | Name: Siremadlin succinate

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Siremadlin (HDM201) is a potent and selective MDM2 antagonist designed to reactivate p53 signaling in tumors with wild-type TP53. It binds to MDM2 with high affinity (IC₅₀ ≈ 2.1 nM), disrupting the MDM2–p53 interaction and leading to p53 stabilization, upregulation of p53 target genes (such as p21 and PUMA), and induction of cell cycle arrest and apoptosis in cancer cells. In vitro studies demonstrate antiproliferative activity across a range of wild-type TP53 tumor cell lines, with GI₅₀ values typically in the low nanomolar range. In vivo, Siremadlin has shown robust tumor growth inhibition and regression in xenograft models, including acute myeloid leukemia (AML) and solid tumors like liposarcoma and neuroblastoma.

Chemical Structure

Siremadlin succinate
Siremadlin succinate
CAS#1638193-48-2 (succinate)

Theoretical Analysis

MedKoo Cat#: 576218

Name: Siremadlin succinate

CAS#: 1638193-48-2 (succinate)

Chemical Formula: C30H30Cl2N6O8

Exact Mass: 672.1502

Molecular Weight: 673.50

Elemental Analysis: C, 53.50; H, 4.49; Cl, 10.53; N, 12.48; O, 19.00

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
Bulk Inquiry
Related CAS #
1638193-48-2 (succinate) 1448867-41-1 (free base)
Synonym
Siremadlin succinate; HDM201; HDM-201; HDM 201;
IUPAC/Chemical Name
Butanedioic acid, compd. with (6S)-5-(5-chloro-1,2-dihydro-1-methyl-2-oxo-3-pyridinyl)-6-(4-chlorophenyl)-2-(2,4-dimethoxy-5-pyrimidinyl)-5,6-dihydro-1-(1-methylethyl)pyrrolo(3,4-d)imidazol-4(1H)-one (1:1)
InChi Key
WOEIHDWLQDGIAG-BDQAORGHSA-N
InChi Code
InChI=1S/C26H24Cl2N6O4.C4H6O4/c1-13(2)33-21-19(30-22(33)17-11-29-26(38-5)31-23(17)37-4)25(36)34(18-10-16(28)12-32(3)24(18)35)20(21)14-6-8-15(27)9-7-14;5-3(6)1-2-4(7)8/h6-13,20H,1-5H3;1-2H2,(H,5,6)(H,7,8)/t20-;/m0./s1
SMILES Code
COc1ncc(c(OC)n1)c2nc3C(=O)N([C@@H](c4ccc(Cl)cc4)c3n2C(C)C)C5=CC(=CN(C)C5=O)Cl.OC(=O)CCC(=O)O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 673.50 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Wu CE, Esfandiari A, Ho YH, Wang N, Mahdi AK, Aptullahoglu E, Lovat P, Lunec J. Targeting negative regulation of p53 by MDM2 and WIP1 as a therapeutic strategy in cutaneous melanoma. Br J Cancer. 2017 Dec 12. doi: 10.1038/bjc.2017.433. [Epub ahead of print] PubMed PMID: 29235570. 2: Holzer P. Discovery of Potent and Selective p53-MDM2 Protein-Protein Interaction Inhibitors as Anticancer Drugs. Chimia (Aarau). 2017 Oct 25;71(10):716-721. doi: 10.2533/chimia.2017.716. PubMed PMID: 29070416. 3: Chapeau EA, Gembarska A, Durand EY, Mandon E, Estadieu C, Romanet V, Wiesmann M, Tiedt R, Lehar J, de Weck A, Rad R, Barys L, Jeay S, Ferretti S, Kauffmann A, Sutter E, Grevot A, Moulin P, Murakami M, Sellers WR, Hofmann F, Jensen MR. 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. doi: 10.1073/pnas.1620262114. Epub 2017 Mar 6. PubMed PMID: 28265066; PubMed Central PMCID: PMC5373361. 4: Furet P, Masuya K, Kallen J, Stachyra-Valat T, Ruetz S, Guagnano V, Holzer P, Mah R, Stutz S, Vaupel A, Chène P, Jeay S, Schlapbach A. 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):4837-4841. doi: 10.1016/j.bmcl.2016.08.010. Epub 2016 Aug 9. PubMed PMID: 27542305.