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 (Structure Note: Red, Androgen receptor degrader (HY-W248665A); Blue, CBP/p300 ligand (HY-161483); Black, Linker).

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CBPD-268

CBPD-268 Chemical Structure

CAS No. : 2832961-58-5

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Based on 1 publication(s) in Google Scholar

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 (Structure 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
CAS No.
Appearance

Solid

Color

White to light yellow

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
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (121.97 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 1.2197 mL 6.0983 mL 12.1966 mL
5 mM 0.2439 mL 1.2197 mL 2.4393 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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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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

Purity: 99.23%

SDS (251 KB)

COA (252 KB) HNMR (427 KB) RP-HPLC (254 KB) LCMS (95 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 1.2197 mL 6.0983 mL 12.1966 mL 30.4915 mL
5 mM 0.2439 mL 1.2197 mL 2.4393 mL 6.0983 mL
10 mM 0.1220 mL 0.6098 mL 1.2197 mL 3.0492 mL
15 mM 0.0813 mL 0.4066 mL 0.8131 mL 2.0328 mL
20 mM 0.0610 mL 0.3049 mL 0.6098 mL 1.5246 mL
25 mM 0.0488 mL 0.2439 mL 0.4879 mL 1.2197 mL
30 mM 0.0407 mL 0.2033 mL 0.4066 mL 1.0164 mL
40 mM 0.0305 mL 0.1525 mL 0.3049 mL 0.7623 mL
50 mM 0.0244 mL 0.1220 mL 0.2439 mL 0.6098 mL
60 mM 0.0203 mL 0.1016 mL 0.2033 mL 0.5082 mL
80 mM 0.0152 mL 0.0762 mL 0.1525 mL 0.3811 mL
100 mM 0.0122 mL 0.0610 mL 0.1220 mL 0.3049 mL
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CBPD-268 Related Classifications

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-2682832961-58-5CBPD268CBPD 268PROTACsHistone AcetyltransferaseHATsHATorally activeprostate cancer22Rv1LNCaPVCaP cellsInhibitorinhibitorinhibit

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