2. PROTAC Cell Cycle/DNA Damage Apoptosis PI3K/Akt/mTOR
  3. PROTACs CDK Apoptosis Akt mTOR
  4. YJ1206

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).

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

YJ1206

YJ1206 Chemical Structure

CAS No. : 3053716-98-3

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10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

YJ1206 Related Antibodies

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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Akt Akt1 Akt2 Akt3

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mTOR mTORC1 mTORC2

  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

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

 

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 AKTS473, PRAS40 and S6[1].
YJ1206 (0.030-30 μM; 5 days) potently reduces the viability of 6227_KO PRN;Cdk12KO and 6137_J PRN;Cdk12HET 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.

YJ1206 Related Antibodies

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 T1/2 Tmax Cmax AUC0-t AUC0-∞ 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.
Molecular Weight

894.01

Formula

C49H52FN11O5
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.1186 mL 5.5928 mL 11.1856 mL
5 mM 0.2237 mL 1.1186 mL 2.2371 mL
View the 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.

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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Working solution concentration: mg/mL
Purity & Documentation

Purity: 96.92%

SDS (251 KB)

COA (245 KB) HNMR (352 KB) RP-HPLC (259 KB) LCMS (98 KB)

Handling Instructions (2659 KB)
References

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 1.1186 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 Related Classifications

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  • 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.

Keywords:

YJ12063053716-98-3YJ 1206YJ-1206PROTACsCDKApoptosisAktmTORCyclin dependent kinasePKBProtein kinase BMammalian target of Rapamycin22Rv1 prostate cancer cellsprostate cancertubo-ovarian high-grade serous carcinomaAKT pathwayapoptosisDNA damageCCNKCDK13CDK12VCaP prostate cancer cellsInhibitorinhibitorinhibit

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