PI 3065
Modify Date: 2024-01-02 16:33:31
PI 3065 structure
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Common Name | PI 3065 | ||
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| CAS Number | 955977-50-1 | Molecular Weight | 506.638 | |
| Density | 1.4±0.1 g/cm3 | Boiling Point | N/A | |
| Molecular Formula | C27H31FN6OS | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of PI 3065PI-3065 is a potent inhibitor of PI3K p110δ, with IC50 and Ki values of 5 nM and 1.5 nM, and exhibits less potent activity against p110α, p110β, p110γ with IC50s of 910, 600, >10000 nM. |
| Name | Thieno[3,2-d]pyrimidine, 6-[[4-(cyclopropylmethyl)-1-piperazinyl]methyl]-2-(5-fluoro-1H-indol-4-yl)-4-(4-morpholinyl) |
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| Synonym | More Synonyms |
| Description | PI-3065 is a potent inhibitor of PI3K p110δ, with IC50 and Ki values of 5 nM and 1.5 nM, and exhibits less potent activity against p110α, p110β, p110γ with IC50s of 910, 600, >10000 nM. |
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| Related Catalog | |
| Target |
p110δ:5 nM (IC50) p110β:600 nM (IC50) p110α:910 nM (IC50) |
| In Vitro | PI-3065 exhibits no inhibition of the growth of 4T1 cells, which do not express detectable levels of p110δ[1]. |
| In Vivo | PI-3065 (75 mg/kg, p.o.) inhibits the growth of 4T1 tumours in the BALB/c mice without obvious body weight loss[1]. |
| Animal Admin | Female WT BALB/c mice are orthotopically inoculated in the mammary fat pad on day 0 with 1×105 4T1 cells. Drug (75 mg/kg PI-3065, once daily) or vehicle (0.5% methylcellulose with 0.2% Tween 80) is administered by oral gavage from day -1 (administered 12 h prior to tumour cell inoculation). Tumour growth is monitored weekly by caliper measurement or by measuring luminescence using a Xenogen imaging platform. On day 35, mice are euthanized, tumours and peripheral organs extracted for in vitro luminescence measurement, followed by fixation in 4% PFA and H&E staining. KPC mice are allowed to develop advanced lesions of 5-10 mm (determined by ultrasound imaging) before treatment with vehicle or PI-3065 for a total of 14 days. |
| References |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Molecular Formula | C27H31FN6OS |
| Molecular Weight | 506.638 |
| Exact Mass | 506.226410 |
| PSA | 88.76000 |
| LogP | 2.64 |
| Index of Refraction | 1.698 |
| Storage condition | -20℃ |
| pi 3065 |
| Thieno[3,2-d]pyrimidine, 6-[[4-(cyclopropylmethyl)-1-piperazinyl]methyl]-2-(5-fluoro-1H-indol-4-yl)-4-(4-morpholinyl)- |
| 6-{[4-(Cyclopropylmethyl)-1-piperazinyl]methyl}-2-(5-fluoro-1H-indol-4-yl)-4-(4-morpholinyl)thieno[3,2-d]pyrimidine |
| PI-3065 |