WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H123936
CAS#: N/A
Description: SP27 is a selective PLK4 proteolysis targeting chimera (PROTAC) degrader. SP27 exhibited effective PLK4 degradation, more potent inhibition of cell growth, and more efficient precision-therapeutic effect in the TRIM37-amplified MCF-7 cell line than conventional inhibitor CZS-035. Moreover, SP27 showed 149% bioavailability after intraperitoneal administration in PK studies and potent antitumor efficacy in vivo. The discovery of SP27 demonstrated the practicality and importance of PLK4 PROTAC and paved the way for studying PLK4-dependent biological functions and treat TRIM37-amplified breast cancer.
Hodoodo Cat#: H123936
Name: SP27
CAS#: N/A
Chemical Formula: C40H40F2N12O5
Exact Mass: 806.32
Molecular Weight: 806.840
Elemental Analysis: C, 59.55; H, 5.00; F, 4.71; N, 20.83; O, 9.91
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Synonym: SP27; SP 27; SP-27
IUPAC/Chemical Name: 5-(4-(4-(6-((2,4-difluorobenzyl)amino)-4-((5-methyl-1H-pyrazol-3-yl)amino)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carbonyl)piperidin-1-yl)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione
InChi Key: NTSTTXFDEIQUET-UHFFFAOYSA-N
InChi Code: InChI=1S/C40H40F2N12O5/c1-21-16-32(50-49-21)45-34-29-20-44-54(35(29)48-40(47-34)43-19-23-2-3-24(41)17-30(23)42)25-10-14-52(15-11-25)37(57)22-8-12-51(13-9-22)26-4-5-27-28(18-26)39(59)53(38(27)58)31-6-7-33(55)46-36(31)56/h2-5,16-18,20,22,25,31H,6-15,19H2,1H3,(H,46,55,56)(H3,43,45,47,48,49,50)
SMILES Code: FC1=CC=C(CNC2=NC(N(C3CCN(C(C4CCN(C5=CC6=C(C(N(C7C(NC(CC7)=O)=O)C6=O)=O)C=C5)CC4)=O)CC3)N=C8)=C8C(NC9=NNC(C)=C9)=N2)C(F)=C1
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:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 806.84 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: |
Sun Y, Xue Y, Sun P, Mu S, Liu H, Sun Y, Wang L, Wang J, Wu T, Yin W, Qin Q, Sun Y, Liu N, Wang H, Yang H, Zhao D, Cheng M. Discovery of the First Potent, Selective, and In Vivo Efficacious Polo-like Kinase 4 Proteolysis Targeting Chimera Degrader for the Treatment of TRIM37-Amplified Breast Cancer. J Med Chem. 2023 Jun 6. doi: 10.1021/acs.jmedchem.3c00505. Epub ahead of print. PMID: 37279162.