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CBPD-268 is an effective orally active CBP/p300 PROTAC degrader, with a DC50 value of ≤ 0.03 nM. It induces degradation of CBP/p300 and inhibits cell growth, exhibiting antitumor activity. Additionally, CBPD-268 shows potential for research in AR-positive prostate cancer.
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| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| Description | CBPD-268 is an effective orally active CBP/p300 PROTAC degrader, with a DC50 value of ≤ 0.03 nM. It induces degradation of CBP/p300 and inhibits cell growth, exhibiting antitumor activity. Additionally, CBPD-268 shows potential for research in AR-positive prostate cancer. |
| In vitro | CBPD-268 demonstrates high degradation efficiency on CBP and p300 proteins in 22Rv1 cells with DC50 values of 0.01 and 0.03 nM, respectively, after 4 hours. The compound achieves degradation by binding to CBP/p300 and CRBN proteins. Additionally, CBPD-268 (0-1000 nM; 4 days) inhibits cell growth with IC50 values of 3.7, 10.3, and 4.6 nM in 22Rv1, LNCaP, and VCaP cells, respectively. |
| In vivo | CBPD-268, administered orally at doses of 0.3, 1, 3, to 10, and 30 mg/kg as a single dose, induces degradation of CBP and p300 proteins in tumor tissues. When given at 1 mg/kg twice a week or 3 mg/kg weekly for 4 weeks, CBPD-268 shows antitumor activity. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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