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Referencia número: HY-181035

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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).

Para uso exclusivo en investigación. No vendemos a pacientes.

Fòrmula: C₅₂H₅₃F₄N₁₁O₈S
Peso molecular:1068.10

Almacenamiento:

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

Data Sheet (267 KB)

DN1679 Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
Chemical Information
Pureza y Documentación
Referencias
Calculators
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

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

Ver todos los productos específicos de isoformas PROTACs :

Ver todos los productos específicos de isoformas CDK :

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	T_max	C_max	T_1/2	AUC_0-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

Peso molecular 1068.10
Fòrmula 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
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (267 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Chen D, et al. Discovery of DN1679 as a Potent, Orally Bioavailable, and Highly Selective CDK12/13 Dual Degrader for the Treatment of Triple-Negative Breast Cancer. J Med Chem. 2026 Jan 22;69(2):1033-1048. [Content Brief]

Calculators

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
Chemical Information
Pureza y Documentación
Referencias

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DN1679

Ver todos los productos específicos de isoformas PROTACs

Ver todos los productos específicos de isoformas CDK