| CAS |
No.1362850-20-1 |
| 英文名称 |
Seletalisib |
| 分子式 |
C23H14ClF3N6O |
| 分子量 |
482.85 |
| 溶解性 |
Soluble in DMSO ≥8mg/mL |
| 纯度 |
≥98% |
| 外观(性状) |
White to off-white Solid |
| 储存条件 |
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| SMILES |
C1=CC2=CC(=C(N=C2C(=C1)Cl)C3=C[N+](=CC=C3)[O-])C(C(F)(F)F)NC4=NC=NC5=C4N=CC=C5 |
| InChIKey |
LNLJHGXOFYUARS-OAQYLSRUSA-N |
| InChI |
InChI=1S/C23H14ClF3N6O/c24-16-6-1-4-13-10-15(18(31-19(13)16)14-5-3-9-33(34)11-14)21(23(25，26)27)32-22-20-17(29-12-30-22)7-2-8-28-20/h1-12，21H，(H，29，30，32)/t21-/m1/s1 |
| PubChem CID |
56928390 |
| 靶点 |
PI3K |
| 通路 |
Cell Cycle;DNA Damage/DNA Repair; Epigenetics;PI3K/Akt/mTOR |
| 背景说明 |
Seletalisib是有效选择性的PI3Kδ抑制剂。 |
| 生物活性 |
Seletalisib (UCB5857) is potent and selective PI3Kδ inhibitor with an IC50 of 12 nM.[1] |
| IC50 |
IC50:PI3Kδ 12 nM[1] |
| In Vitro |
Seletalisib is a potent， ATP-competitive and highly selective PI3Kδ inhibitor able to block AKT phosphorylation following activation of the BCR in a B-cell line. Seletalisib inhibits N-formyl peptides (fMLP)-stimulated but not phorbol myristate acetate (PMA)-stimulated superoxide release from human neutrophils consistent with a PI3Kδ-specific activity. No indications of cytotoxicity are observed in PBMCs or other cell types treated with seletalisib. seletalisib blocks human T-cell production of several cytokines from activated T-cells. Seletalisib inhibits T-cell differentiation to Th1， Th2， and Th17 subtypes. Additionally， seletalisib inhibits B-cell proliferation and cytokine release. In human whole blood assays， seletalisib inhibits CD69 expression upon B-cell activation and anti-IgE-mediated basophil degranulation[1]. |
| In Vivo |
Seletalisib significantly inhibits IL-2 release following TCR stimulation in the rat. The inhibition is observed at all tested doses of seletalisib with almost complete inhibition reached at dose levels ≥1 mg/kg. Seletalisib has potent in vivo effects with an estimated IC50 value of [1]. |
| 动物实验 |
Rats: Rats are dosed with seletalisib (0.1-10 mg/kg in 500 μL volume) or vehicle via oral gavage 30 min prior to i.v. administration of anti- CD3 antibody administered in a 200 μL dose volume. The vehicle is methylcellulose or saline for oral and i.v. administration， respectively. Seletalisib levels and IL-2 levels are measured[1]. |
| 激酶实验 |
Seletalisib is dissolved 1 mM solution in DMSO， and tested in a concentration response (seletalisib)， to explore the effects of PI3Kδ-specific inhibition compared with complete inhibition of class I PI3K signaling. In addition， seletalisib is tested in the BioMap BT cell system at concentrations of 1000， 100， 10， and 1 nM. An activity profile is generated based on the effect of the compounds on the levels of cellular readouts， including cytokines， growth factors， adhesion molecules， and proliferation endpoints[1]. |
| 数据来源文献 |
[1]. Allen RA， et al. Seletalisib: Characterization of a Novel， Potent， and Selective Inhibitor of PI3Kδ. J Pharmacol Exp Ther. 2017 Apr 25. pii: jpet.116.237347. |
| 规格 |
1mg 5mg 10mg 25mg 50mg |
| 单位 |
瓶 |
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