2. Epigenetics PROTAC
  3. Histone Acetyltransferase PROTACs
  4. CBPD-409

CBPD-409 is an orally active PROTAC degrader for CBP/p300, with DC50 of 0.2–0.4 nM. CBPD-409 exhibits antiproliferative effects in AR+ prostate cancer cell lines VCaP, LNCaP and 22Rv1, with IC50s of 1.2–2.0 nM. CBPD-409 exhibits antitumor efficacy (Red: CBP inhibitor GNE049 (HY-108435); Blue: CRBN/cullin 4A Thalidomide (HY-14658); Black: Linker).

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

CBPD-409 Chemical Structure

CBPD-409 Chemical Structure

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Customer Review

Based on 1 publication(s) in Google Scholar

CBPD-409 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

CBPD-409 is an orally active PROTAC degrader for CBP/p300, with DC50 of 0.2–0.4 nM. CBPD-409 exhibits antiproliferative effects in AR+ prostate cancer cell lines VCaP, LNCaP and 22Rv1, with IC50s of 1.2–2.0 nM. CBPD-409 exhibits antitumor efficacy (Red: CBP inhibitor GNE049 (HY-108435); Blue: CRBN/cullin 4A Thalidomide (HY-14658); Black: Linker)[1].

In Vitro

CBPD-409 (0.01-10 nM) suppresses the AR signaling and c-Myc expression in prostate cancer cells VCaP, LNCaP and 22Rv1[1].

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

CBPD-409 Related Antibodies

RT-PCR[1]

Cell Line: VCaP, LNCaP and 22Rv1
Concentration: 0.01-10 nM
Incubation Time: 6 h
Result: Reduced mRNA levels of KLK3, AR and c-Myc.
In Vivo

CBPD-409 (1 mg/kg, iv; 3 mg/kg, po) exhibits pharmacokinetic profiles in ICR mice, with a low clearance CL of 1.7 mL/min/kg, a half-life with T1/2 of 2.8 h (i.v.) and 2.6 h (p.o.), an oral exposure Cmax of 2494 ng/mL and an oral bioavailability with F=50%[1].
CBPD-409 (0.3-1 mg/kg, po, once daily for 5 weeks) exhibits antitumor efficacy against VCaP prostate cancer with tumor growth inhibition TGI of 73-87%, without significant toxicity in VCaP xenograft mice model[1].

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

Animal Model: VCaP xenograft CB17 SCID mice model[1]
Dosage: 0.3-1 mg/kg
Administration: p.o., once a day for 5 weeks
Result: Inhibited tumor growth with TGI of 73% (0.3 mg/kg) and 87% (1 mg/kg), without significant body weight loss.
Molecular Weight

862.97

Formula

C46H52F2N10O5
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(N1C2C(NC(CC2)=O)=O)C3=CC(N4CCN(C[C@@H]5CC[C@@H](N6C7=C(CN(C(C)=O)CC7)C(N8C9=C(CCC8)C=C(C(C(F)F)=C9)C%10=CN(C)N=C%10)=N6)CC5)CC4)=CC=C3C1=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (115.88 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 1.1588 mL 5.7939 mL 11.5879 mL
5 mM 0.2318 mL 1.1588 mL 2.3176 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (2.90 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (2.90 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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 1.1588 mL 5.7939 mL 11.5879 mL 28.9697 mL
5 mM 0.2318 mL 1.1588 mL 2.3176 mL 5.7939 mL
10 mM 0.1159 mL 0.5794 mL 1.1588 mL 2.8970 mL
15 mM 0.0773 mL 0.3863 mL 0.7725 mL 1.9313 mL
20 mM 0.0579 mL 0.2897 mL 0.5794 mL 1.4485 mL
25 mM 0.0464 mL 0.2318 mL 0.4635 mL 1.1588 mL
30 mM 0.0386 mL 0.1931 mL 0.3863 mL 0.9657 mL
40 mM 0.0290 mL 0.1448 mL 0.2897 mL 0.7242 mL
50 mM 0.0232 mL 0.1159 mL 0.2318 mL 0.5794 mL
60 mM 0.0193 mL 0.0966 mL 0.1931 mL 0.4828 mL
80 mM 0.0145 mL 0.0724 mL 0.1448 mL 0.3621 mL
100 mM 0.0116 mL 0.0579 mL 0.1159 mL 0.2897 mL
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CBPD-409 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-409CBPD409CBPD 409Histone AcetyltransferasePROTACsHATsHATVCaPLNCaP22Rv1CB17 SCID miceICR miceorally activeInhibitorinhibitorinhibit

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