Art. -Nr.: HY-168555

YJ1206

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YJ1206 is an orally active selective CDK12/CDK13 PROTAC degrader. YJ1206 induces DNA damage and genomic instability, activates the AKT pathway, and triggers apoptosis. YJ1206 reduces tumor cell viability, inhibits tumor growth, and attenuates tumor cell dissemination. YJ1206 is applicable to research related to prostate cancer and high-grade serous tubo-ovarian cancer.
(Pink: CDK12 and CDK13 ligand (HY-168658); Blue: Cereblon E3 ligase ligand; Black: linker).

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Reinheit: 97.26%
CAS. Nr.: 3053716-98-3
Formel: C₄₉H₅₂FN₁₁O₅
Molecular Weight:894.01

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

YJ1206 Chemical Structure

CAS. Nr.: 3053716-98-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

YJ1206 is an orally active selective CDK12/CDK13 PROTAC degrader. YJ1206 induces DNA damage and genomic instability, activates the AKT pathway, and triggers apoptosis. YJ1206 reduces tumor cell viability, inhibits tumor growth, and attenuates tumor cell dissemination. YJ1206 is applicable to research related to prostate cancer and high-grade serous tubo-ovarian cancer^[1]^[2]. (Pink: CDK12 and CDK13 ligand (HY-168658); Blue: Cereblon E3 ligase ligand; Black: linker).

IC₅₀ & Target^[1]

CDK12

CDK13

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle CDK Isoform-spezifische Produkte anzeigen :

Alle Akt Isoform-spezifische Produkte anzeigen :

Alle mTOR Isoform-spezifische Produkte anzeigen :

In Vitro

YJ1206 (0.2-100 nM; 4 h) potently and dose-dependently degrades CDK12 and CDK13 proteins in VCaP prostate cancer cells^[1].
YJ1206 (for 5 days) inhibits the viability of VCaP prostate cancer cells, with an IC₅₀ of 12.55 nM^[1].
YJ1206 (500 nM; 8 h) selectively degrades CDK12, CDK13 and CCNK in 22Rv1 prostate cancer cells, with extremely weak off-target protein degradation activity^[1].
YJ1206 induces gene length-dependent transcription elongation defects in VCaP prostate cancer cells, specifically manifesting as inhibition of long gene expression, alteration of DDR and AKT-mTOR pathway activities, and induction of DNA damage-related changes in gene expression^[1].
YJ1206 (500 nM; 15 h) activates the AKT pathway in VCaP and 22Rv1 prostate cancer cells by increasing the phosphorylation levels of AKT^S473, PRAS40 and S6^[1].
YJ1206 (0.030-30 μM; 5 days) potently reduces the viability of 6227_KO PRN;Cdk12^KO and 6137_J PRN;Cdk12^HET mouse ovarian cancer cells, with an IC₅₀ value of approximately 212 nM; whereas it shows weaker efficacy against 15973_WT PRN cells, with an IC₅₀ value of 3337 nM^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

VCaP prostate cancer cells
Concentration:

0.2, 1, 5, 20, 100 nM
Incubation Time:

4 h
Result:

Degraded CDK12 and CDK13 proteins in a dose-dependent manner, with significant reduction observed at concentrations starting from 0.2 nM.

Cell Viability Assay^[2]

Cell Line:

15973_WT PRN, 6227_KO PRN;Cdk12KO, 6137_J PRN;Cdk12HET
Concentration:

0.030, 0.060, 0.12, 0.24, 0.48, 0.96, 1.9, 3.8, 7.6, 15, 30 μM
Incubation Time:

5 days
Result:

Reduced cell viability in a dose-dependent manner across all three cell lines, with significantly greater potency in CDK12-deficient lines.
Exhibited an IC50 value of 3337 nM in 15973_WT PRN cells.
Exhibited IC50 values of 214.8 nM and 211.9 nM in 6227_KO PRN;Cdk12KO and 6137_J PRN;Cdk12HET cells, respectively.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-t	AUC_0-∞	Bioavailability	CL
Mice^[1]	2.5 mg/kg	i.v.	2.95 h	0.08 h	2686.40 ng/mL	7029.51 ng·h/mL	7047.89 ng·h/mL	59.31 %	364.67 mL/h/kg
Mice^[1]	10 mg/kg	p.o.	3.40 h	1.33 h	1601.34 ng/mL	16677.07 ng·h/mL	16812.99 ng·h/mL	59.31 %	/

In Vivo

YJ1206 (100 mg/kg; p.o.; three times per week; for a total of 5 days) completely degrades CDK12, CDK13 and CCNK in castrated VCaP xenograft mice, induces robust apoptosis as detected by PARP cleavage and TUNEL staining, and moderately inhibits tumor growth^[1].
YJ1206 (100 mg/kg; p.o.; three times per week) significantly inhibits tumor growth in the WA74 PDX prostate cancer mouse model, induces regression in 19% of tumors, and causes no significant body weight loss^[1].
YJ1206 (100 mg/kg; p.o.; three times per week; for 4 consecutive weeks) moderately inhibits tumor growth in castrated 22Rv1 xenograft mouse models^[1].
YJ1206 (50-100 mg/kg; p.o.; three times per week) significantly inhibits the growth of CDK12-deficient ovarian cancer subcutaneous allografts in C57BL/6J mice, with a more pronounced therapeutic effect observed at the 100 mg/kg dose^[2].
Oral administration of YJ1206 at a dose of 100 mg/kg three times per week significantly inhibits the growth of subcutaneous xenografts of human CDK12-knockout ovarian cancer in NSG mice^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

CB17SCID (male, 6 weeks old)^[1]
Dosage:

100 mg/kg
Administration:

p.o.; 3x/week; 5 days/31 days
Result:

Completely abrogated CDK12, CDK13, and CCNK protein levels in tumors.
Increased levels of cleaved PARP and γ-H2AX.
Significantly elevated cleaved PARP and TUNEL staining scores compared to vehicle controls.
Exhibited moderate anti-tumor efficacy: 80% of tumors showed progressive disease, 15% showed stable disease, and 5% showed partial response.
Significantly reduced mean tumor volume and weight compared to vehicle controls.

Animal Model:

CB17SCID (male, 6 weeks old)^[1]
Dosage:

100 mg/kg
Administration:

p.o.; 3x/week
Result:

Significantly suppressed tumor growth, resulting in drastically reduced mean tumor volume and weight compared to vehicle controls.
Induced partial response (regression) in 19% of treated tumors.
Caused no significant changes in animal body weights.
Induced tumor regression characterized by hyalinization, remnant tumor nodules, and degenerative cells via histopathological analysis.\nExhibited mild to moderate anti-tumor efficacy, with all treated tumors showing progressive disease but significantly reduced mean tumor volume and weight compared to vehicle controls.

Animal Model:

C57BL/6J mice (female)^[2]
Dosage:

50 mg/kg; 100 mg/kg
Administration:

p.o.; 3 times/wk
Result:

Reduced tumor volume to ~150 mm³ by day 20 (50 mg/kg dose) compared to ~320 mm³ in vehicle controls.
Reduced tumor volume to ~100 mm³ by day 20 (100 mg/kg dose) compared to ~320 mm³ in vehicle controls, with p<0.001 for both doses vs. vehicle.
Showed no obvious toxicity as measured by percent change in body weight.

Animal Model:

NSG mice^[2]
Dosage:

100 mg/kg
Administration:

p.o.; 3 times/wk
Result:

Reduced tumor volume to ~150 mm³ by day 20 compared to ~300 mm³ in vehicle controls, with p<0.001.

Chemical Information

CAS. Nr. 3053716-98-3
Appearance Solid
Molecular Weight 894.01
Formel C₄₉H₅₂FN₁₁O₅
Color Light yellow to yellow
SMILES

O=C(NCC1=CC=CC=C1)N(C2=CN=C(N3CCN(C4CCN(C5=C(F)C=C(C(N(C6CCC(NC6=O)=O)C7=O)=O)C7=C5)CC4)CC3)C=C2)[C@H](CC8)CC[C@@H]8NC9=NC=C%10C(C=CC=C%10)=N9
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 66.67 mg/mL (74.57 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.1186 mL

5.5928 mL

11.1856 mL

5 mM

0.2237 mL

1.1186 mL

2.2371 mL

10 mM

0.1119 mL

0.5593 mL

1.1186 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 1 mg/mL (1.12 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 1 mg/mL (1.12 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 1 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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)
Handling Instructions (2659 KB)

Verweise

[1]. Chang Y, et al. Development of an orally bioavailable CDK12/13 degrader and induction of synthetic lethality with AKT pathway inhibition. Cell Rep Med. 2024;5(10):101752. [Content Brief]

[2]. Tien JC, et al. Defining CDK12 as a tumor suppressor and therapeutic target in mouse models of tubo-ovarian high-grade serous carcinoma. Proc Natl Acad Sci U S A. 2025;122(24):e2426909122. [Content Brief]

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.

Complete Stock Solution Preparation Table

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	1.1186 mL	5.5928 mL	11.1856 mL	27.9639 mL
	5 mM	0.2237 mL	1.1186 mL	2.2371 mL	5.5928 mL
	10 mM	0.1119 mL	0.5593 mL	1.1186 mL	2.7964 mL
	15 mM	0.0746 mL	0.3729 mL	0.7457 mL	1.8643 mL
	20 mM	0.0559 mL	0.2796 mL	0.5593 mL	1.3982 mL
	25 mM	0.0447 mL	0.2237 mL	0.4474 mL	1.1186 mL
	30 mM	0.0373 mL	0.1864 mL	0.3729 mL	0.9321 mL
	40 mM	0.0280 mL	0.1398 mL	0.2796 mL	0.6991 mL
	50 mM	0.0224 mL	0.1119 mL	0.2237 mL	0.5593 mL
	60 mM	0.0186 mL	0.0932 mL	0.1864 mL	0.4661 mL

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YJ1206

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

PI3K/Akt/mTOR Compound Library

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Mitochondrial Protection Compound Library

PROTAC Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle CDK Isoform-spezifische Produkte anzeigen

Alle Akt Isoform-spezifische Produkte anzeigen

Alle mTOR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

YJ1206 Related Classifications

HY-168555 Related Classifications