PI3Kdelta-IN-8 biochemical

PI3Kdelta-IN-8

Cat. Num. AAA228122

• Purity: 98%
• Synonyms: PI3Kdelta-IN-8; N/A; PI3Kdelta-IN-8 biochemical

• Purity/Purification: 98%

• CAS: 2101518-75-4
• Targets&IC50: PI3Kgamma:17.9 nM (IC50), PI3Kalpha:377.2 nM (IC50), PI3Kbeta:241.6 nM (IC50), PI3Kdelta:3.3 nM (IC50)
• Solubility: <1mg/ml refers to the product slightly soluble or insoluble
• In vitro: PI3Kdelta-IN-8 (1-30 mg/kg; p.o. once daily for 24 d) significantly reduces the tumor volume and tumor weight in a dose-dependent manner in mice[1]. PI3Kdelta-IN-8 (1 mg/kg; i.v.) displays a suitable half-life (1 h), C max (2.3 uM) and low clearance (5.6 mL/min/kg) in mice[1]. PI3Kdelta-IN-8 (10 mg/kg; p.o.) displays moderate oral bioavailability (39%), C max (7.5 uM), and AUC last (22 uM/h) in mice[1]. Animal Model: Female NOD scid mice were injected OCI-Ly10 cells[1]. Dosage: 1, 3, 10, 30 mg/kg. Administration: P.o. once daily for 24 days. Result: Reduced the tumor volume, with an ED 50 of 6.47 mg/kg. Tumor growth inhibition of 81.95% was seen with a highly significant reduction in both tumor volume and tumor weight. Animal Model: Male BALB/c mice[1]. Dosage: 1 mg/kg for i.v.; 10 mg/kg for p.o. (Pharmacokinetic Analysis). Administration: Intravenous administration and oral administration. Result: I.v.: t 1/2 =1 h, C max =2.3 uM, CL=5.6 mL/min/kg. P.o.: F=39%, C max =7.5 uM, AUC last =22uM/h.
• Preparation and Storage: Powder: -20 degree C for 3 years; In solvent: -80 degree C for 2 years

Structure

(TLR8 agonist 2, CAS 2412937-64-3)

Structure

(TLR8 agonist 2, CAS 2412937-64-3)

Related Product Information for PI3Kdelta-IN-8 biochemical

PI3Kdelta-IN-8 is a potent, selective and orally active PI3Kdelta inhibitor, with an IC 50 of 3.3 nM. PI3Kdelta-IN-8 shows selectivity for PI3Kdelta over PI3Kalpha, PI3Kbeta, and PI3Kgamma (IC 50 =377.2, 241.6, 17.9 nM, respectively). PI3Kdelta-IN-8 has anti-tumor activity.

References

1. Zhe Cai, et al. Tlr8 agonist. WO2020057604A1.