product name PI-3065
Description: PI-3065 is a selective p110δ inhibitor with IC50 of 15 nM, and >70-fold selectivity over other PI3K family members. PI-3065 has been reported to selectively inhibit p110δkinase with Ki values of 15nM, 110nM, 130nM and 940nM, IC50 values of 5nM, 91nM, 600nM and >10000nM for p110δ, p110α, p110β and p110γ, respectively. In addition, PI-3065 has been revealed to inhibit 4T1 tumour growth and metastasis. PI-3065 has also noted to prolong survival and reduce the incidence of macroscopic metastases and other disease-associated pathologies.
References: Nature. 2014 Jun 19;510(7505):407-11.
506.64
Formula
C27H31FN6OS
CAS No.
955977-50-1
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 50 mg/mL warming (98.7 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Chemical Name
4-(6-((4-(cyclopropylmethyl)piperazin-1-yl)methyl)-2-(5-fluoro-1H-indol-4-yl)thieno[3,2-d]pyrimidin-4-yl)morpholine
other peoduct :
| In Vitro | Kinase Assay:
Cell Assay: Proliferation of 4T1 cells is assayed following a 4-h treatment with the indicated p110δ inhibitors, then washing and MTS staining are carried out after 48 h culture. PI-3065 shows no inhibition on the growth of 4T1 cells, which do not expressing detectable levels of p110δ |
|---|---|
| In Vivo | In mouse model, PI-3065 (75 mg/kg, p.o.) also suppresses 4T1 tumor growth and metastasis via inactivation of p110δ. In the LSL.KrasG12D/+; p53R172H/+; PdxCretg/+ (or KPC) model of pancreatic ductal adenocarcinoma, PI-3065 prolongs survival and reduces the incidence of macroscopic metastases and other disease-associated pathologies. |
| Animal model | Female WT BALB/c mice bearing 4T1 tumors |
| Formulation & Dosage | Dissolved in 0.5% methylcellulose with 0.2% Tween 80; 75 mg/kg; Oral administration |
| References | [1] Ali K, et al. Nature. 2014, 510(7505), 407-411. |
