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  3. Inobrodib

Inobrodib (Synonyms: CCS1477)

Cat. No.: HY-111784 Purity: 99.42%
Handling Instructions

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.

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

Inobrodib Chemical Structure

Inobrodib Chemical Structure

CAS No. : 2222941-37-7

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Solution
10 mM * 1 mL in DMSO USD 223 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
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5 mg USD 190 In-stock
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10 mg USD 340 In-stock
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25 mg USD 720 In-stock
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50 mg USD 1020 In-stock
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Based on 1 publication(s) in Google Scholar

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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 1,060 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].

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].

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.
SMILES

O=C1N(C2=CC=C(F)C(F)=C2)[[email protected]](C3=NC4=CC(C5=C(C)ON=C5C)=CC=C4N3[[email protected]]6CC[[email protected]](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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (187.06 mM; Need ultrasonic)

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
10 mM 0.1871 mL 0.9353 mL 1.8706 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

  • 3.

    Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 2.5 mg/mL (4.68 mM); Clear solution

  • 4.

    Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.68 mM); Clear solution

*All of the co-solvents are available by MCE.
References

Purity: 99.53% ee.: 97.03%

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Inobrodib
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HY-111784
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