GSK1324726A (I-BET726)
- Product Name
- GSK1324726A (I-BET726)
- CAS No.
- 1300031-52-0
- Chemical Name
- GSK1324726A (I-BET726)
- Synonyms
- GSK1324726A;CS-1736;I-BET726;I-BET726; I-BET 726;GSK1324726A (I-BET726);I-BET726 (GSK1324726A);BET Inhibitor, I-BET726;GSK1324726A, 10 mM in DMSO;GSK1324726A (I-BET726) USP/EP/BP;GSK-1324726A,Apoptosis,GSK1324726A,Inhibitor,Epigenetic Reader Domain,inhibit
- CBNumber
- CB62677051
- Molecular Formula
- C25H23ClN2O3
- Formula Weight
- 434.91
- MOL File
- 1300031-52-0.mol
GSK1324726A (I-BET726) Property
- Boiling point:
- 707.3±60.0 °C(Predicted)
- Density
- 1.304±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- insoluble in H2O; ≥1.87 mg/mL in EtOH with gentle warming and ultrasonic; ≥17.7 mg/mL in DMSO
- form
- Powder
- pka
- 4.20±0.10(Predicted)
- color
- White to light yellow
- InChI
- InChI=1S/C25H23ClN2O3/c1-15-13-23(27-21-10-8-20(26)9-11-21)22-14-19(7-12-24(22)28(15)16(2)29)17-3-5-18(6-4-17)25(30)31/h3-12,14-15,23,27H,13H2,1-2H3,(H,30,31)/t15-,23+/m0/s1
- InChIKey
- FAWSUKOIROHXAP-NPMXOYFQSA-N
- SMILES
- C(O)(=O)C1=CC=C(C2C=CC3=C(C=2)[C@H](NC2=CC=C(Cl)C=C2)C[C@H](C)N3C(C)=O)C=C1
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
- Precautionary statements
-
P280Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 16872
- Product name
- I-BET726
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $41
- Updated
- 2024/03/01
- Product number
- 16872
- Product name
- I-BET726
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $142
- Updated
- 2024/03/01
- Product number
- 16872
- Product name
- I-BET726
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $263
- Updated
- 2024/03/01
- Product number
- 16872
- Product name
- I-BET726
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $601
- Updated
- 2024/03/01
- Product number
- B1013
- Product name
- GSK1324726A
- Packaging
- 1unit
- Price
- $28
- Updated
- 2021/12/16
GSK1324726A (I-BET726) Chemical Properties,Usage,Production
Description
I-BET726 is an inhibitor of BET family proteins that binds BRD2, BRD3, and BRD4 with high affinity (IC50s = 41, 31, and 22 nM, respectively) and competes with tetra-acetylated histone 4 peptides for binding to the bromodomains of these proteins. It exhibits >1,000-fold selectivity for these proteins over other bromodomain-containing homologs. I-BET726 inhibits cell growth and induces cytotoxicity in neuroblastoma cell lines by modulating the expression of genes involved in apoptosis and Myc signaling. I-BET726 can be administered orally to animals, and it reduces tumor growth in mouse xenograft models of human neuroblastoma.
Uses
GSK1324726A is a novel, potent, and selective inhibitor of BET proteins with high affinity to BRD2 (IC50=41 nM), BRD3 (IC50=31 nM), and BRD4 (IC50=22 nM).
in vivo
GSK1324726A (I-BET726) inhibits neuroblastoma tumor growth. In the SK-N-AS model, mice in the vehicle group are euthanized on day 14 due to large tumor size. While there is no significant difference in tumor growth between the vehicle and GSK1324726A (5 mg/kg) group, 58% tumor growth inhibition (TGI) is observed in the GSK1324726A (15 mg/kg) group on day 14 of the study (n=9; p=0.006). Mice in the GSK1324726A (15 mg/kg) group are treated for an additional 7 days before tumor volume reaches a level comparable to that observed in the vehicle group, at which point the study is terminated. Tumors in the CHP-212 model grow much more slowly. After 42 days, tumors in vehicle-treated mice are only half the size those in the SK-N-AS model at the end of the study (Day 14). In the CHP-212 model, treatment with 5 mg/kg GSK1324726A results in TGI equal to 50% (n=8; p=0.1816), and mice in the 15 mg/kg group exhibits a TGI of 82% at the end of the study (n=5; p=0.0488)[1].
target
BRD2
References
[1] wyce a, ganji g, smitheman kn, chung cw, korenchuk s, bai y, barbash o, le b, craggs pd, mccabe mt, kennedy-wilson km, sanchez lv, gosmini rl, parr n, mchugh cf, dhanak d, prinjha rk, auger kr, tummino pj. bet inhibition silences expression of mycn and bcl2 and induces cytotoxicity in neuroblastoma tumor models. plos one. 2013 aug 23;8(8):e72967.
GSK1324726A (I-BET726) Preparation Products And Raw materials
Raw materials
Preparation Products
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