Art. -Nr.: HY-168201

MJP6412

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MJP6412 is a p300 and CBP PROTAC degrader that potently degrades p300 and CBP in 22Rv1 cells with DC₅₀ values of 1.6 nM and 1.2 nM, respectively. MJP6412 downregulates the expression of AR-FL, AR-V7 and c-MYC, as well as androgen receptor target genes (KLK3, FKBP5, TMPRSS2). MJP6412 completely abolishes p300/CBP-dependent histone acetylation (H3K27Ac and H2BNTAC) and induces G₁ cell cycle arrest. MJP6412 inhibits cancer cell proliferation and tumor growth. MJP6412 can be used in prostate cancer-related research.
(Pink: CBP/p300 ligand (HY-111784); Blue: Cereblon ligand (HY-W087383); Black: linker (HY-W102095)).

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Reinheit: 95.90%
CAS. Nr.: 3105406-14-9
Formel: C₅₅H₅₄F₂N₈O₉
Molecular Weight:1009.06

Speicherung:

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

MJP6412 Chemical Structure

CAS. Nr.: 3105406-14-9

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

MJP6412 is a p300 and CBP PROTAC degrader that potently degrades p300 and CBP in 22Rv1 cells with DC₅₀ values of 1.6 nM and 1.2 nM, respectively. MJP6412 downregulates the expression of AR-FL, AR-V7 and c-MYC, as well as androgen receptor target genes (KLK3, FKBP5, TMPRSS2). MJP6412 completely abolishes p300/CBP-dependent histone acetylation (H3K27Ac and H2BNTAC) and induces G₁ cell cycle arrest. MJP6412 inhibits cancer cell proliferation and tumor growth. MJP6412 can be used in prostate cancer-related research^[1]. (Pink: CBP/p300 ligand (HY-111784); Blue: Cereblon ligand (HY-W087383); Black: linker (HY-W102095)).

IC₅₀ & Target^[1]

p300

CBP

AR-FL

AR-V7

KLK3

FKBP5

TMPRSS2

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Histone Acetyltransferase Isoform-spezifische Produkte anzeigen :

In Vitro

MJP6412 (0.1-1000 nM; 24 h) potently degrades p300 (DC₅₀ = 1.6 nM, D_max = 96%) and CBP (DC₅₀ = 1.2 nM, D_max = 89%) in 22Rv1 human castration-resistant prostate cancer cells after 24 h of treatment^[1].
MJP6412 (5 days) potently inhibits the growth of 22Rv1 human castration-resistant prostate cancer cells with an IC₅₀ of 37.6 nM and I_max of 91% after 5 days of treatment^[1].
MJP6412 (0.1-1000 nM; 24 h) potently degrades p300 (DC₅₀ = 3.4 nM, D_max = 94%) and CBP (DC₅₀ = 3.7 nM, D_max = 82%) in LNCaP human prostate cancer cells after 24 h of treatment^[1].
MJP6412 (0.1-1000 nM; 24 h) potently degrades p300 (DC₅₀ = 1.6 nM, D_max = 97%) and CBP (DC₅₀ = 1.4 nM, D_max = 89%) in VCaP human prostate cancer cells after 24 h of treatment^[1].
MJP6412 (10 nM; 12 h) degrades p300 and CBP in 22Rv1 human castration-resistant prostate cancer cells via a ubiquitin-proteasome-dependent PROTAC mechanism that requires CRBN recruitment and binding to p300/CBP^[1].
MJP6412 (100 nM; 6 h) acts as a highly selective p300/CBP degrader in 22Rv1 human castration-resistant prostate cancer cells, with no reduction in known CRBN neo-substrates after 6 h of treatment with 100 nM^[1].
MJP6412 (5 days) potently inhibits the growth of VCaP human prostate cancer cells with an IC₅₀ of 7.9 nM and I_max of 98% after 5 days of treatment^[1].
MJP6412 (5 days) potently inhibits the growth of LNCaP human prostate cancer cells with an IC₅₀ of 21.4 nM and I_max of 89% after 5 days of treatment^[1].
MJP6412 (5 days) potently inhibits the growth of enzalutamide-resistant VCaP-ENR human prostate cancer cells with an IC₅₀ of 5.2 nM and I_max of 98% after 5 days of treatment^[1].
MJP6412 (5 days) potently inhibits the growth of enzalutamide-resistant LNCaP-ENR human prostate cancer cells with an IC₅₀ of 138.1 nM and I_max of 72% after 5 days of treatment^[1].
MJP6412 (10-100 nM; 24-48 h) downregulates AR and c-MYC signaling in 22Rv1 human castration-resistant prostate cancer cells, reducing AR-FL, AR-V7, and c-MYC protein and mRNA levels, as well as AR-regulated gene mRNA levels, after 24−48 h of treatment with 10−100 nM^[1].
MJP6412 (10-100 nM; 12 h) completely extinguishes p300/CBP-dependent histone acetylation (H3K27Ac, H2BK5Ac, H2BK20Ac) in 22Rv1 human castration-resistant prostate cancer cells after 12 h of treatment with 100 nM^[1].
MJP6412 (10 nM; 0.25-96 h) induces long-lasting degradation of p300 and CBP in 22Rv1 human castration-resistant prostate cancer cells, with maximum degradation starting at 12 h and lasting through 48 h after treatment with 10 nM^[1].
MJP6412 (1-100 nM; 48 h) induces dose-dependent G1 cell cycle arrest in VCaP human prostate cancer cells, with significant arrest occurring after 48 h of treatment with 100 nM^[1].

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

Cell Cycle Analysis^[1]

Cell Line:

VCaP human prostate cancer cells
Concentration:

1, 10 and 100 nM
Incubation Time:

48 h
Result:

Induced G1 cell cycle arrest in a dose-dependent manner.
Induced detectable G1 arrest at 1 nM.
Significantly induced G1 arrest at 100 nM.

Western Blot Analysis^[1]

Cell Line:

VCaP cells
Concentration:

0.1, 1, 10 and 100 nM
Incubation Time:

24 h (for AR-FL, AR-V7, and c-MYC protein expression); 12 h (for H2BK5Ac, H2BK20Ac, and H3K27Ac protein expression)
Result:

Treatment with 0.1, 1, 10, and 100 nM for 24 h resulted in a dose-dependent decrease in AR-FL, AR-V7, and c-MYC protein expression.
At 10 nM, the expression of AR-FL and AR-V7 was significantly reduced, and at 100 nM, a >80% reduction in AR-FL and AR-V7 proteins was observed.
For c-MYC, 10 nM significantly reduced its expression, and 100 nM almost completely depleted it.
In the acetylation assay, treatment with 10 nM for 12 h significantly decreased the levels of H3K27Ac, H2BK5Ac, and H2BK20Ac, and these acetylation marks were almost completely abolished at 100 nM.

Parmacokinetics

Species	Dose	Route	T_1/2	AUC_0-t	V_z	CL	MRT_0-t
Mice^[1]	5 mg/kg	i.v.	4.27 h	2407 ng/mL·h	12500 mL/kg	2058 mL/h/kg	2.75 h

In Vivo

MJP6412 (10 mg/kg; i.p.; single dose) efficiently reduces p300 protein levels in 22Rv1 prostate cancer xenograft tumors in ICR mice^[1].
MJP6412 (3-15 mg/kg; i.v.; every other day; 24 days) exhibits significant antitumor activity with a 42% TGI in VCaP prostate cancer xenograft tumors in BALB/c-Nude mice, with excellent biosafety^[1].

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

Animal Model:

ICR mice 22Rv1 prostate cancer xenograft^[1]
Dosage:

10 mg/kg
Administration:

i.p.; single dose
Result:

Reduced p300 protein levels in 22Rv1 xenograft tumor tissue at 6 hours post-treatment.

Animal Model:

Male BALB/c-Nude mice, 6 weeks old, were maintained in a standard SPF mouse room. VCaP cells (1 × 10⁷ cells in Matrigel (Corning Life Sciences), 0.2 mL/mouse) were injected subcutaneously into the right side of the induced cell-derived xenograft tumor and allowed to grow to the indicated size. When the average volume of the tumors reached approximately 200 mm³, treatment can start.
^[1]
Dosage:

3 mg/kg; 15 mg/kg
Administration:

i.v.; every other day; 24 days
Result:

Achieved a tumor growth inhibition (TGI) value of 42% at 15 mg/kg, comparable to positive control CCS1477.
Was well tolerated, with no significant mouse weight loss observed over the 24-day treatment period.

Chemical Information

CAS. Nr. 3105406-14-9
Appearance Solid
Molecular Weight 1009.06
Formel C₅₅H₅₄F₂N₈O₉
Color Light yellow to yellow
SMILES

O=C(CCC1N(C(C2=C3C=CC(N4CCC(CC4)OC5=CC=C(C=C5)NC(CO[C@H]6CC[C@H](N7C([C@H]8N(C9=CC(F)=C(F)C=C9)C(CCC8)=O)=NC%10=CC(C%11=C(C)ON=C%11C)=CC=C7%10)CC6)=O)=C2)=O)C3=O)NC1=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 (99.10 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

0.9910 mL

4.9551 mL

9.9102 mL

5 mM

0.1982 mL

0.9910 mL

1.9820 mL

10 mM

0.0991 mL

0.4955 mL

0.9910 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 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (2.48 mM); Suspended solution

This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (2.48 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, 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 (282 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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]. Ma M, et al. Discovery of a Highly Potent PROTAC Degrader of p300/CBP Proteins for the Treatment of Enzalutamide-Resistant Prostate Cancer. Journal of medicinal chemistry. 2024 Sep 29. [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	0.9910 mL	4.9551 mL	9.9102 mL	24.7755 mL
	5 mM	0.1982 mL	0.9910 mL	1.9820 mL	4.9551 mL
	10 mM	0.0991 mL	0.4955 mL	0.9910 mL	2.4776 mL
	15 mM	0.0661 mL	0.3303 mL	0.6607 mL	1.6517 mL
	20 mM	0.0496 mL	0.2478 mL	0.4955 mL	1.2388 mL
	25 mM	0.0396 mL	0.1982 mL	0.3964 mL	0.9910 mL
	30 mM	0.0330 mL	0.1652 mL	0.3303 mL	0.8259 mL
	40 mM	0.0248 mL	0.1239 mL	0.2478 mL	0.6194 mL
	50 mM	0.0198 mL	0.0991 mL	0.1982 mL	0.4955 mL
	60 mM	0.0165 mL	0.0826 mL	0.1652 mL	0.4129 mL
	80 mM	0.0124 mL	0.0619 mL	0.1239 mL	0.3097 mL

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MJP6412

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Histone Acetyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MJP6412 Related Classifications

HY-168201 Related Classifications