DN1679
DN1679 is a potent, selective and orally active CRBN-dependent CDK12/13 PROTAC dual degrader. DN1679 shows DC50 of 8.8/9.8 nM (MDA-MB-231), 5.1/6.4 nM (MDA-MB-157) and 17.2/15.8 nM (MDA-MB-468) for CDK12/13. DN1679 can downregulate DNA damage response gene mRNA levels, such as ATM, ATR, BRCA1 and RAD51. DN1679 demonstrates a potent synergistic anti-tumor effect companied with Olaparib (HY-10162). DN1679 can be used for research of triple-negative breast cance.
(Pink: CDK12 and CDK13 ligand (HY-181036); Blue: Cereblon ligand (HY-W093272); Black: linker).
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- Formule: C52H53F4N11O8S
- Masse moléculaire:1068.10
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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CDK12 8.8 nM (DC50) |
CDK13 9.8 nM (DC50) |
Cereblon |
DN1679 inhibits MDA-MB-231, MDA-MB-157 and MDA-MB-468 cells proliferation with IC50 values of 31.7, 49.1 and 121.4 nM. DN1679 has low cytotoxicity to normal human cell lines (MCF10A and NCM460) (IC50 of 236.9 and 378.5 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Tmax | Cmax | T1/2 | AUC0-t | CL |
|---|---|---|---|---|---|---|---|
| Mice[1] | 20 mg/kg | p.o. | 2.0 h | 3617 ng/mL | 4.1 h | 15730 ng·h/mL | 1309 mL/h/kg |
Chemical Information
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Masse moléculaire 1068.10
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Formule C52H53F4N11O8S
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SMILES
CC(N([C@@H]1CC[C@H](CC1)NC2=NC(C3=CN=CC(S(C)(=O)=O)=C3)=C(C=N2)C(F)(F)F)C4=CC=C(C=C4)C5=CN=C(N=C5)O[C@H]6CN(CC6)CC7CCN(CC7)C8=CC(C(N9C%10CCC(NC%10=O)=O)=O)=C(C=C8F)C9=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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