PROTAC CBP/P300 Degrader-1

Name: PROTAC CBP/P300 Degrader-1
Brand: MedChemExpress
SKU: HY-138536
Rating: 4.5 (1 reviews)

Cat. No.: HY-138536 Purity: 99.18%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

PROTAC CBP/P300 Degrader-1 is a potent PROTAC CBP/P300 degrader. PROTAC CBP/P300 Degrader-1 potently inhibited cell viability of multiple cancer cell lines.

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

PROTAC CBP/P300 Degrader-1 Chemical Structure

CAS No. : 2484739-48-0

Size	Price	Stock	Quantity
1 mg	USD 477	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 1050	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 1650	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 3300	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 5300	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 8500	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

Description

PROTAC CBP/P300 Degrader-1 is a potent PROTAC CBP/P300 degrader. PROTAC CBP/P300 Degrader-1 potently inhibited cell viability of multiple cancer cell lines^[1].

IC₅₀ & Target^[1]

Cereblon

In Vitro

PROTAC CBP/P300 Degrader-1 shows LNCaP prostate cancer cell viability inhibition (IC₅₀=0.4 nM). PROTAC CBP/P300 Degrader-1 (10 nM) induces degradation of P300 (≥ 80%)^[1].
PROTAC CBP/P300 Degrader-1 potently inhibited cell viability of multiple cancel cell lines (IC₅₀s ranging from 0.1-141.4 nM for HEL, NOMO-1, MOLM-13, HL-60, MEG-01, MM.IS, MM.1R, NCL-H929, RPM-8226, AMO-1, WSU-DLCL2, Karpas-422, Pfeiffer, SU-DHL-1, LNCap clone FGC, VCap; 22RV1, NCI-H520, NCI-H703, LK-2, MCE-7, and SK-BR-3 cells)^[1].

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

Molecular Weight

893.98

Formula

C₄₆H₅₃F₂N₁₁O₆

CAS No.

2484739-48-0

Appearance

Solid

Color

Light yellow to green yellow

SMILES

O=C(N1CC2=C(CC1)N(C(CC3)CCN3C(CCCCCNC4=C(C(N5C(CCC6=O)C(N6)=O)=O)C(C5=O)=CC=C4)=O)N=C2N7C8=CC(C(F)F)=C(C(C=N9)=CN9C)C=C8CCC7)NC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility

In Vitro:

DMSO : 173.33 mg/mL (193.89 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	1.1186 mL	5.5930 mL	11.1859 mL
5 mM	0.2237 mL	1.1186 mL	2.2372 mL
10 mM	0.1119 mL	0.5593 mL	1.1186 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 (sealed storage, away from moisture and light). 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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: 6.5 mg/mL (7.27 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 6.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (65.0 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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

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

Purity: 99.18%

Select Batch:

Data Sheet (274 KB) SDS (252 KB)

COA (253 KB) HNMR (253 KB) LCMS (110 KB)

Handling Instructions (2659 KB)

References

[1]. Jing Liu, et al. Cyclic-amp response element binding protein (cbp) and/or adenoviral e1a binding protein of 300 kda (p300) degradation compounds and methods of use. WO2020173440A1.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.1186 mL	5.5930 mL	11.1859 mL	27.9648 mL
	5 mM	0.2237 mL	1.1186 mL	2.2372 mL	5.5930 mL
	10 mM	0.1119 mL	0.5593 mL	1.1186 mL	2.7965 mL
	15 mM	0.0746 mL	0.3729 mL	0.7457 mL	1.8643 mL
	20 mM	0.0559 mL	0.2796 mL	0.5593 mL	1.3982 mL
	25 mM	0.0447 mL	0.2237 mL	0.4474 mL	1.1186 mL
	30 mM	0.0373 mL	0.1864 mL	0.3729 mL	0.9322 mL
	40 mM	0.0280 mL	0.1398 mL	0.2796 mL	0.6991 mL
	50 mM	0.0224 mL	0.1119 mL	0.2237 mL	0.5593 mL
	60 mM	0.0186 mL	0.0932 mL	0.1864 mL	0.4661 mL
	80 mM	0.0140 mL	0.0699 mL	0.1398 mL	0.3496 mL
	100 mM	0.0112 mL	0.0559 mL	0.1119 mL	0.2796 mL