1887237-54-8
1887237-54-8 structure
- Name: I-BET567
- Chemical Name: I-BET567
- CAS Number: 1887237-54-8
- Molecular Formula: C17H18ClN5O2
- Molecular Weight: 359.81
- Catalog: Signaling Pathways Epigenetics Epigenetic Reader Domain
- Create Date: 2022-03-07 13:05:21
- Modify Date: 2024-01-14 15:03:44
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I-BET567 is a potent and oral active inhibitor of pan-BET candidate with pIC50s of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. I-BET567 has been demonstrated efficacy in mouse models of oncology and inflammation[1].
| Name | I-BET567 |
|---|
| Description | I-BET567 is a potent and oral active inhibitor of pan-BET candidate with pIC50s of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. I-BET567 has been demonstrated efficacy in mouse models of oncology and inflammation[1]. |
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| Related Catalog | |
| Target |
BRD4 (BD1):6.9 (pIC50) BRD2:7.2 (pIC50) |
| In Vitro | I-BET567 (compound 27) (72 hours; 1.5 nM-30 μM) effectively inhibites the proliferation of human NMC cell line 11060 in vitro with a mean gpIC50 6.2 (0.63 μM)[1]. Cell Viability Assay[1] Cell Line: NMC line 11060 cells Concentration: 1.5 nM-30 μM Incubation Time: 72 hours Result: Significantly reduced cell growth. |
| In Vivo | I-BET567 (compound 27) (3, 10, and 30 mg/kg; p.o.; once daily for 20 days) leads to a significant reduction in tumor growth compared with vehicle controls at both 10 and 30 mg/kg[1]. Assessment of Pharmacokinetics (PK) profile of I-BET567 following intravenous infusion and oral administration in male wistar han rat and beagle doga[1]. species dose ivb/poc (mg/kg) CLb (mL/min/kg) CLb,u (mL/min/kg) CLrenal (mL/min/kg) Vss (L/kg) Vss,u (L/kg) t1/2 (h) Fpo (%) fub rat 1.3/3 25 109 7 2.4 10.4 1.6 99d 0.23 dog 1.0/3 8.1 20 6.9 1.2 2.9 1.8 98 0.41 a: Values are mean, n=3 unless otherwise stated. b: IV dose 1h infusion in DMSO and (10%, w/v) Kleptose HPB in saline (2%: 98% (v/v)). c: PO dose vehicle: 1%(w/v) methycellulose (400 cps) (aq). d: Mean n = 2. Animal Model: NMC 11060 xenograft mouse model (NOD/SCID mouse; bearing NMC 11060 cells) [1] Dosage: 3, 10, and 30 mg/kg Administration: p.o. (once daily for 20 days Result: Led to a significant reduction in tumor growth compared to vehicle controls at both 10 and 30 mg/kg. |
| References |
| Molecular Formula | C17H18ClN5O2 |
|---|---|
| Molecular Weight | 359.81 |