2. PROTAC Epigenetics
  3. PROTACs Histone Acetyltransferase
  4. CBPD-268

CBPD-268 is a potent and orally active CBP/p300 PROTAC degrader with an DC50 value of ≤ 0.03 nM. CBPD-268 induces CBP/p300 degradation and inhibits cell growth. CBPD-268 shows antitumor activity. CBPD-268 has the potential for the research of AR-positive prostate cancer (Srtucture Note: Red, Androgen receptor degrader (HY-W248665A); Blue, CBP/p300 ligand (HY-161483); Black, Linker).

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

CBPD-268 Chemical Structure

CBPD-268 Chemical Structure

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CBPD-268 Related Antibodies

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Description

CBPD-268 is a potent and orally active CBP/p300 PROTAC degrader with an DC50 value of ≤ 0.03 nM. CBPD-268 induces CBP/p300 degradation and inhibits cell growth. CBPD-268 shows antitumor activity. CBPD-268 has the potential for the research of AR-positive prostate cancer (Srtucture Note: Red, Androgen receptor degrader (HY-W248665A); Blue, CBP/p300 ligand (HY-161483); Black, Linker)[1].

In Vitro

CBPD-268 (4, 24 h) shows high degradation efficiency for CBP and p300 protein with DC50s of 0.01, 0.03 nM at 4 h in 22Rv1 cells[1].
CBPD-268 shows degradation by binding to both CBP/p300 and CRBN protein[1].
CBPD-268 (0-1000 nM; 4 days) inhibits cell growth with IC50s of 3.7, 10.3, 4.6 nM for 22Rv1, LNCaP, VCaP cells, respectively[1].

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

CBPD-268 Related Antibodies
In Vivo

CBPD-268 (0.3, 1, 3, 10, 30 mg/kg; p.o.; once) induces depletion of both CBP and p300 proteins in tumor tissues with a single oral administration at 0.3-3 mg/kg[1].
CBPD-268 (1, 3 mg/kg; p.o.; twice a week for 1 mg/kg or 3 mg/kg weekly for 4-weeks) shows antitumor activity[1].
Pharmacokinetic Parameters[1].

Species IV (mg/kg) T1/2 (h) V1/2(L/kg) CL (mL/min/kg) PO(mg/kg) T1/2 (h) Cmax (ng/ml) AUC(h*ng/mL) F(%)
Rats 1 1.9 4.9 34.6 3 1.3 220.6 936.9 67
Mice 1 3.4 1.6 6.0 3 3.1 724.7 4190.4 60

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

Animal Model: male CB17 SCID mice (VCaP xenograft tumor)[1]
Dosage: 0.3, 1, 3, 10, 30 mg/kg
Administration: P.o.; once
Result: Induced depletion of both CBP and p300 proteins in the VCaP tumor tissue in a dose-dependent manner.
Animal Model: male CB17 SCID mice (VCaP xenograft tumor model)[1]
Dosage: 1, 3 mg/kg
Administration: P.o.; twice a week for 1 mg/kg or 3 mg/kg weekly for 4-weeks
Result: Inhibited tumor growth and shows little effect on animal body weight.
Animal Model: female BALB/c mice[1]
Dosage: 3, 10, 30 mg/kg
Administration: P.o.; twice weekly for 5-6 weeks
Result: Induced no weight loss or other signs of toxicity at both 3 and 10 mg/kg dose-levels in both male and female mice.
Animal Model: Female Sprague–Dawley (SD) rats[1]
Dosage: 1-10 mg/kg
Administration: P.o.; twice a week for 5 weeks
Result: Did not cause animal body weight loss during the entire experiment and did not induce any signs of toxicity during the entire experiment.
Molecular Weight

819.90

Formula

C44H47F2N9O5
SMILES

CC(N1CC2=C(CC1)N([C@@H]3CC[C@H](CC3)CN4CC(C=C(C(N(C5CCC(NC5=O)=O)C6=O)=O)C6=C7)=C7C4)N=C2N8CCCC9=C8C=C(C(F)F)C(C%10=CN(N=C%10)C)=C9)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CBPD-268 Related Classifications

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Help & FAQs
  • 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:

CBPD-268CBPD268CBPD 268PROTACsHistone AcetyltransferaseHATsHATorally activeprostate cancer22Rv1LNCaPVCaP cellsInhibitorinhibitorinhibit

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