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

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

CBPD-409 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

View All Isoforms

  • 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
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

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

CBPD-409 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
CBPD-409
Cat. No.:
HY-158113
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.