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  2. Epigenetic Reader Domain
  3. Inobrodib

Inobrodib (CCS1477) is an orally active, potent, and selective inhibitor of the p300/CBP bromodomain. Inobrodib binds to p300 and CBP with Kd values of 1.3 and 1.7 nM, respectively, and with 170/130-fold selectivity compared with BRD4 with a Kd of 222 nM. CCS1477 inhibits cell proliferation in prostate cancer cell lines and decreases androgen receptor (AR)- and C-MYC-regulated gene expression.

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Inobrodib Chemical Structure

Inobrodib Chemical Structure

CAS No. : 2222941-37-7

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10 mM * 1 mL in DMSO
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10 mg USD 340 In-stock
25 mg USD 720 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Inobrodib (CCS1477) is an orally active, potent, and selective inhibitor of the p300/CBP bromodomain. Inobrodib binds to p300 and CBP with Kd values of 1.3 and 1.7 nM, respectively, and with 170/130-fold selectivity compared with BRD4 with a Kd of 222 nM. CCS1477 inhibits cell proliferation in prostate cancer cell lines and decreases androgen receptor (AR)- and C-MYC-regulated gene expression[1].

IC50 & Target

p300/CBP[1]

In Vitro

Inobrodib binding to cellular histones in an in-cell BRET assay gives an IC50 of 19 nM for p300 and 1060 nM for BRD4. Inobrodib shows potent growth-inhibitory activity in VCaP, 22Rv1, and LNCaP95 (all IC50 < 100 nM) that express both AR-FL and AR-V7[1].
? Inobrodib (0-3000 nM; 48 hours) reduces expression of AR-regulated genes (KLK2, KLK3, and TMPRSS2) in both 22Rv1 and LNCaP95 cells. Inobrodib also reduces C-MYC protein expression in both 22Rv1 and LNCaP95 cells and AR-V7 protein expression in 22Rv1 cells, without clear impact on AR-FL protein expression in 22Rv1 and LNCaP95 cells. Inobrodib reduces C-MYC mRNA and downstream AR and C-MYC signaling in 22Rv1 and C4-2 cells at 16 hours. Inobrodib regulates AR signaling by affecting the recruitment of CBP, p300, and AR-FL to known AR binding sites, and has the potential to abrogate persistent AR signaling in CRPC[1].

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

In Vivo

Inobrodib (10-30 mg/kg; oral gavage; 10 or 20 mg/kg daily (QD) or 30 mg/kg every other day (QOD) for 28 days) suppresses growth of a 22Rv1 mouse xenograft model with associated reduction in AR signaling[1].
? Inobrodib (20 mg/kg; oral gavage; daily for 8 days) decreases AR and AR-V7 signaling and inhibits growth in a patient- derived model of lethal prostate cancer (NOD/SCID gamma (NSG) male castrated mice)[1].

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

Animal Model: Noncastrated male athymic nude mice[1]
Dosage: 10-30 mg/kg
Administration: Oral gavage; at 10 or 20 mg/kg daily (QD) or at 30 mg/kg every other day (QOD) for 28 days
Result: Affected tumor growth at 10 mg/kg daily, 20 mg/kg daily, and 30 mg/kg every other day.
Clinical Trial
Molecular Weight

534.60

Formula

C30H32F2N4O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1N(C2=CC=C(F)C(F)=C2)[C@H](C3=NC4=CC(C5=C(C)ON=C5C)=CC=C4N3[C@H]6CC[C@H](OC)CC6)CCC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (187.06 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 1.8706 mL 9.3528 mL 18.7056 mL
5 mM 0.3741 mL 1.8706 mL 3.7411 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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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: ≥ 5.25 mg/mL (9.82 mM); Clear solution

    This protocol yields a clear solution of ≥ 5.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (52.5 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% Corn Oil

    Solubility: ≥ 5.25 mg/mL (9.82 mM); Clear solution

    This protocol yields a clear solution of ≥ 5.25 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 (52.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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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 +
+
%
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%
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

Purity: 99.53% ee.: 97.03%

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8706 mL 9.3528 mL 18.7056 mL 46.7639 mL
5 mM 0.3741 mL 1.8706 mL 3.7411 mL 9.3528 mL
10 mM 0.1871 mL 0.9353 mL 1.8706 mL 4.6764 mL
15 mM 0.1247 mL 0.6235 mL 1.2470 mL 3.1176 mL
20 mM 0.0935 mL 0.4676 mL 0.9353 mL 2.3382 mL
25 mM 0.0748 mL 0.3741 mL 0.7482 mL 1.8706 mL
30 mM 0.0624 mL 0.3118 mL 0.6235 mL 1.5588 mL
40 mM 0.0468 mL 0.2338 mL 0.4676 mL 1.1691 mL
50 mM 0.0374 mL 0.1871 mL 0.3741 mL 0.9353 mL
60 mM 0.0312 mL 0.1559 mL 0.3118 mL 0.7794 mL
80 mM 0.0234 mL 0.1169 mL 0.2338 mL 0.5845 mL
100 mM 0.0187 mL 0.0935 mL 0.1871 mL 0.4676 mL
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Inobrodib 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.

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Inobrodib
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