PI-3065 955977-50-1
Product Description
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Molecular Weight: 506.64 PI-3065 is a selective p110δ inhibitor with IC50 of 15 nM, >70-fold selectivity over other PI3K family members.
PI-3065 shows no inhibition on the growth of 4T1 cells, which do not expressing detectable levels of p110δ.
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 Study: [1]
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Chemical Information
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Contact us if you need more details on PI-3065 955977-50-1. We are ready to answer your questions on packaging, logistics, certification or any other aspects about 955977-50-1、955977-50-1 PI-3065. If these products fail to match your need, please contact us and we would like to provide relevant information.
Molecular Weight: 506.64 PI-3065 is a selective p110δ inhibitor with IC50 of 15 nM, >70-fold selectivity over other PI3K family members.
PI-3065 shows no inhibition on the growth of 4T1 cells, which do not expressing detectable levels of p110δ.
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.
Cell lines | 4T1 cells |
---|---|
Concentrations | ~10 μM |
Incubation Time | 48 hours |
Method | 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. |
Animal Study: [1]
Animal Models | Female WT BALB/c mice bearing 4T1 tumors |
---|---|
Formulation | 0.5% methylcellulose with 0.2% Tween 80 |
Dosages | 75 mg/kg, once daily |
Administration | p.o. |
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species | Baboon | Dog | Monkey | Rabbit | Guinea pig | Rat | Hamster | Mouse |
Weight (kg) | 12 | 10 | 3 | 1.8 | 0.4 | 0.15 | 0.08 | 0.02 |
Body Surface Area (m2) | 0.6 | 0.5 | 0.24 | 0.15 | 0.05 | 0.025 | 0.02 | 0.007 |
Km factor | 20 | 20 | 12 | 12 | 8 | 6 | 5 | 3 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Rat dose (mg/kg) = mouse dose (22.4 mg/kg) × | mouse Km(3) | = 11.2 mg/kg |
rat Km(6) |
Chemical Information
Molecular Weight (MW) | 506.64 |
---|---|
Formula | C27H31FN6OS |
CAS No. | 955977-50-1 |
Storage | 3 years -20℃Powder |
---|---|
6 months-80℃in solvent (DMSO, water, etc.) | |
Synonyms | N/A |
Chemical Name | 6-((4-(cyclopropylmethyl)piperazin-1-yl)methyl)-2-(5-fluoro-1H-indol-4-yl)-4-morpholinothieno[3,2-d]pyrimidine |
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Molarity Calculator
Dilution Calculator
Molecular Weight Calculator
Contact us if you need more details on PI-3065 955977-50-1. We are ready to answer your questions on packaging, logistics, certification or any other aspects about 955977-50-1、955977-50-1 PI-3065. If these products fail to match your need, please contact us and we would like to provide relevant information.
Product Categories : PI3K/Akt/mTOR > PI3K Inhibitor
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