WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H123552
CAS#: 2488892-09-5
Description: TMX-2172 is a heterobifunctional CDK2 degrader with degradation selectivity for CDK2 and CDK5 over not only CDK1, but transcriptional CDKs (CDK7 and CDK9) and cell cycle CDKs (CDK4 and CDK6) as well. Antiproliferative activity in ovarian cancer cells (OVCAR8) depends on CDK2 degradation and correlates with high expression of cyclin E1 (CCNE1), which functions as a regulatory subunit of CDK2. TMX-2172 represents a lead for further development and that CDK2 degradation is a potentially valuable therapeutic strategy in ovarian and other cancers that overexpress CCNE1.
Hodoodo Cat#: H123552
Name: TMX-2172
CAS#: 2488892-09-5
Chemical Formula: C41H45BrFN9O11S
Exact Mass: 969.21
Molecular Weight: 970.830
Elemental Analysis: C, 50.72; H, 4.67; Br, 8.23; F, 1.96; N, 12.99; O, 18.13; S, 3.30
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Synonym: TMX-2172; TMX 2172; TMX2172;
IUPAC/Chemical Name: 2-((5-bromo-2-((4-(N-(14-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)-3,6,9,12-tetraoxatetradecyl)sulfamoyl)-2-methylphenyl)amino)pyrimidin-4-yl)amino)-6-fluorobenzamide
InChi Key: ZOJWMCDSTRTTOW-UHFFFAOYSA-N
InChi Code: InChI=1S/C41H45BrFN9O11S/c1-24-22-25(8-9-29(24)49-41-46-23-27(42)37(51-41)48-31-7-3-5-28(43)35(31)36(44)54)64(58,59)47-13-15-61-17-19-63-21-20-62-18-16-60-14-12-45-30-6-2-4-26-34(30)40(57)52(39(26)56)32-10-11-33(53)50-38(32)55/h2-9,22-23,32,45,47H,10-21H2,1H3,(H2,44,54)(H,50,53,55)(H2,46,48,49,51)
SMILES Code: O=C(N(C1CCC(NC1=O)=O)C2=O)C3=C2C(NCCOCCOCCOCCOCCNS(C4=CC(C)=C(NC5=NC(NC6=C(C(N)=O)C(F)=CC=C6)=C(Br)C=N5)C=C4)(=O)=O)=CC=C3
Appearance: To be determined
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: Cyclin-dependent kinase 2 (CDK2) is a potential therapeutic target for the treatment of cancer. Development of CDK2 inhibitors has been extremely challenging as its ATP-binding site shares high similarity with CDK1, a related kinase whose inhibition causes toxic effects.
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The following data is based on the product molecular weight 970.83 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.
| 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 |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
Teng M, Jiang J, He Z, Kwiatkowski NP, Donovan KA, Mills CE, Victor C, Hatcher JM, Fischer ES, Sorger PK, Zhang T, Gray NS. Development of CDK2 and CDK5 Dual Degrader TMX-2172. Angew Chem Int Ed Engl. 2020 Aug 10;59(33):13865-13870. doi: 10.1002/anie.202004087. Epub 2020 Jun 3. PMID: 32415712; PMCID: PMC7703486.
