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| Size | Price | Stock |
|---|---|---|
| 100mg | $1250 | Check With Us |
| 250mg | $1850 | Check With Us |
| 500mg | $2775 | Check With Us |
: Cat #: V31532 CAS #: 2222941-37-7 Purity ≥ 99%
Description: Inobrodib (CCS1477; BP-IN-1; CCS-1477) is a novel, potent and selective p300/CBP bromodomain inhibitor with anticancer activity.
References: Rasool RU, et al. Toppling the HAT to Treat Lethal Prostate Cancer. Cancer Discov. 2021;11(5):1011-1013.
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- Protocol
- Related Biological Data
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| Molecular Weight (MW) | 534.60 |
|---|---|
| Molecular Formula | C30H32F2N4O3 |
| CAS No. | 2222941-37-7 |
| SMILES Code | 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 |
| Synonyms | CBP-IN 1; CCS-1477; CCS 1477; CCS147; CBP-IN-1; CBP IN-1; Inobrodib; |
| Protocol | In Vitro | 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. 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. |
|---|---|---|
| In Vivo | 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). 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. |
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 1.8706 mL | 9.3528 mL | 18.7056 mL | 37.4111 mL |
| 5mM | 0.3741 mL | 1.8706 mL | 3.7411 mL | 7.4822 mL |
| 10mM | 0.1871 mL | 0.9353 mL | 1.8706 mL | 3.7411 mL |
| 20mM | 0.0935 mL | 0.4676 mL | 0.9353 mL | 1.8706 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.