1. PROTAC Cell Cycle/DNA Damage
  2. PROTACs CDK
  3. 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).

For research use only. We do not sell to patients.

DN1679

DN1679 Chemical Structure

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Description

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[1]. (Pink: CDK12 and CDK13 ligand (HY-181036); Blue: Cereblon ligand (HY-W093272); Black: linker).

IC50 & Target[1]

CDK12

8.8 nM (DC50)

CDK13

9.8 nM (DC50)

Cereblon

 

In Vitro

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.

Parmacokinetics
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
Molecular Weight

1068.10

Formula

C52H53F4N11O8S

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
DN1679
Cat. No.:
HY-181035
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