Art. -Nr.: HY-158113

CBPD-409

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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).

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Reinheit: 98.29%
CAS. Nr.: 3037549-86-0
Formel: C₄₆H₅₂F₂N₁₀O₅
Molecular Weight:862.97

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

CBPD-409 Chemical Structure

CAS. Nr.: 3037549-86-0

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Histone Acetyltransferase Isoform-spezifische Produkte anzeigen :

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CWR22R	IC₅₀	1.2 nM Compound: 25; CBPD-409	Antiproliferative activity against AR positive human 22Rv1 cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay Antiproliferative activity against AR positive human 22Rv1 cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay	[PMID: 38530938]
LNCaP	IC₅₀	1.6 nM Compound: 25; CBPD-409	Antiproliferative activity against AR positive human LNCaP cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay Antiproliferative activity against AR positive human LNCaP cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay	[PMID: 38530938]
VCaP	IC₅₀	2 nM Compound: 25; CBPD-409	Antiproliferative activity against AR positive human VCaP cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay Antiproliferative activity against AR positive human VCaP cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay	[PMID: 38530938]

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.

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 T_1/2 of 2.8 h (i.v.) and 2.6 h (p.o.), an oral exposure C_max 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.

Chemical Information

CAS. Nr. 3037549-86-0
Appearance Solid
Molecular Weight 862.97
Formel C₄₆H₅₂F₂N₁₀O₅
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.1588 mL

5.7939 mL

11.5879 mL

5 mM

0.2318 mL

1.1588 mL

2.3176 mL

10 mM

0.1159 mL

0.5794 mL

1.1588 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Chen Z, et al., Discovery of CBPD-409 as a Highly Potent, Selective, and Orally Efficacious CBP/p300 PROTAC Degrader for the Treatment of Advanced Prostate Cancer. J Med Chem. 2024 Mar 26. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

PROTAC Library

MCE Bioactive Compound Library

Alle Histone Acetyltransferase Isoform-spezifische Produkte anzeigen

Alle PROTACs Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CBPD-409

PROTAC Library

MCE Bioactive Compound Library

Alle Histone Acetyltransferase Isoform-spezifische Produkte anzeigen

Alle PROTACs Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CBPD-409 Related Classifications

HY-158113 Related Classifications