CPS2
Based on 1 publication(s) in Google Scholar
CPS2 is a first-in-class, highly potent, selective and irreversible PROTAC CDK2 degrader (IC50= 24 nM). CPS2 can be used for the research of acute myeloid leukemia.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.33%
- CAS. Nr.: 2756741-90-7
- Formel: C38H42N12O10S2
- Molecular Weight:890.94
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Publications Citing Use of MedChemExpress (MCE) CPS2
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Biologische Aktivität
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CDK2 24 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HL-60 | IC50 |
>1000 nM
Compound: CPS2
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Antiproliferative activity against human HL-60 cells measured after 1 to 3 days by CCK-8 assay
Antiproliferative activity against human HL-60 cells measured after 1 to 3 days by CCK-8 assay
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[PMID: 38878515] |
CPS2 (5-333 nM; 12 hours; Ramos cells) stands out as the most potent degrader[1].
CPS2 (0.5-2 μM; HSCs) inhibits the proliferation of HSCs without inducing cytotoxicity. CPS2 (1-10000 nM; 48 hours; NB4 cells) induces potent CDK2 degradation. CPS2 (250 nM; 0-6 hours; Ramos and NB4 cells) rapidly induces the degradation of CDK2. CPS2 (10-500 nM; 6 hours; Ramos cells) induces only CDK2 degradation and does not directly perturb the other CDK proteins under subnanomolar concentration conditions. CPS2 (250 nM; 6 hours; NB4 cells) stands out as the most downregulated protein in cells treated for 6 hours with CPS2, confirming the selectivity of CPS2 for CDK2. CPS2 (0-250 nM; NB4 cells) makes the levels of CDK2 obviously decreased. CPS2 (2 μM; 3 days; HL60 cells) obviously promotes ATRA-induced CD11b upregulation[1].
The antileukemic effects of CPS2 are mediated by CDK2 degradation. CPS2 also induces granulocytic differentiation of HSCs, as assessed by cell morphological analysis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Ramos cells
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Concentration:5~333 nM
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Incubation Time:12 hours
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Result:Stood out as the most potent degrader.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 2756741-90-7
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Appearance Solid
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Molecular Weight 890.94
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Formel C38H42N12O10S2
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Color Yellow to green
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SMILES
O=C(N1)CCC(N2C(C3=CC=CC(NCCOCCOCCN4N=NC(COCCNS(C5=CC=C(C=C5)NC6=NN(C(N)=N6)C(C7=C(C=CS7)C)=O)(=O)=O)=C4)=C3C2=O)=O)C1=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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bioRxiv
MYBL2 drives prostate cancer plasticity and identifies CDK2 as a therapeutic vulnerability in RB1-loss and neuroendocrine prostate cancer. [Abstract]2024 Feb 2:2024.01.31.578216. PMID: 38352340
Lösungsmittel & Löslichkeit
DMSO : 32.5 mg/mL (36.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (271 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.1224 mL | 5.6121 mL | 11.2241 mL | 28.0603 mL |
| 5 mM | 0.2245 mL | 1.1224 mL | 2.2448 mL | 5.6121 mL | |
| 10 mM | 0.1122 mL | 0.5612 mL | 1.1224 mL | 2.8060 mL | |
| 15 mM | 0.0748 mL | 0.3741 mL | 0.7483 mL | 1.8707 mL | |
| 20 mM | 0.0561 mL | 0.2806 mL | 0.5612 mL | 1.4030 mL | |
| 25 mM | 0.0449 mL | 0.2245 mL | 0.4490 mL | 1.1224 mL | |
| 30 mM | 0.0374 mL | 0.1871 mL | 0.3741 mL | 0.9353 mL |
CPS2 Related Classifications
HY-141680 Related Classifications
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