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
Unlabeled Cas

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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