Cart summary

You have no items in your shopping cart.

YJ1206

SKU: orb2695706

Description

YJ1206 is an orally bioavailable, low-toxicity PROTAC that potently and selectively degrades CDK12/13 (IC50=12.55 nM). It disrupts transcription elongation, induces DNA damage and cell-cycle arrest, and inhibits prostate cancer cell proliferation, showing synergistic potential with AKT inhibitors in preclinical research.

Research Area

Cell Biology, Pharmacology & Drug Discovery

Images & Validation

Key Properties

CAS Number3053716-98-3
MW894.01
Purity97.14%
FormulaC49H52FN11O5
SMILESO=C1C=2C(C(=O)N1C3C(=O)NC(=O)CC3)=CC(F)=C(C2)N4CCC(CC4)N5CCN(CC5)C6=CC=C(N(C(NCC7=CC=CC=C7)=O)[C@@H]8CC[C@@H](NC9=NC%10=C(C=N9)C=CC=C%10)CC8)C=N6
TargetApoptosis,CDK,PROTACs
SolubilityDMSO:50 mg/mL (55.93 mM)

Bioactivity

Target IC50
CDK12/13 (VCaP prostate cancer cells):12.55  nM
In Vivo
In CD-1 immunocompetent mice bearing VCaP-CRPC, WA74 PDX, or PC310 PDX prostate tumor xenografts, YJ1206 was administered orally at 100 mg/kg, 3 times per week, for up to 21 days. Tumor samples were analyzed by Western blot, H&E staining, IHC, and TUNEL assays. YJ1206 significantly suppressed tumor growth with minimal observed toxicity.
In Vitro
VCaP and 22Rv1 prostate cancer cells were treated with YJ1206 at concentrations ranging from 0 to 500 nM for 4 to 15 hours. Experiments included Western blot, RNA-seq, proteomics, and qPCR to evaluate degradation of CDK12/13 and downstream effects. YJ1206 showed an IC₅₀ of 12.55 nM in VCaP cells and exhibited potent antiproliferative activity.

Storage & Handling

Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

YJ 1206

Similar Products

Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at support@biorbyt.com.

Key Properties

No computed properties available.

Documents Download

Datasheet
Product Information
Download

Request a Document

Protocol Information

YJ1206 (orb2695706)

  • Star
  • Star
  • Star
  • Star
  • Star
  • 0.0
Based on 0 reviews

Participating in our Biorbyt product reviews program enables you to support fellow scientists by sharing your firsthand experience with our products.

Login to Submit a Review

No reviews yet

Step 1: Enter information below

(Recommended: An additional animal making an allowance for loss during the experiment)

Step 2: Enter the in vivo formulation

(This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

1 mg
$ 90.00
5 mg
$ 140.00
10 mg
$ 180.00
25 mg
$ 270.00
50 mg
$ 440.00
100 mg
$ 710.00
DispatchUsually dispatched within 5-10 working days
Bulk Enquiry