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| | PKI-402 Basic information |
| Product Name: | PKI-402 | | Synonyms: | 1-(4-(3-ethyl-7-morpholino-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-yl)phenyl)-3-(4-(1-methylpiperazine-4-carbonyl)phenyl)urea;1-(4-(3-ethyl-7-morpholino-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-yl)phenyl)-3-(4-(4-methylpiperazine-1-carbonyl)phenyl)urea;PKI-402;PKI402;1-(4-(3-Ethyl-7-morpholino-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-yl)phenyl)-3-(4-(4-methylpiper;PKI-402;1-[4-[3-Ethyl-7-(morpholin-4-yl)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-yl]phenyl]-3-[4-[(4-methylpiperazin-1-yl)carbonyl]phenyl]urea;CS-167;Urea, N-[4-[3-ethyl-7-(4-morpholinyl)-3H-1,2,3-triazolo[4,5-d]pyrimidin-5-yl]phenyl]-N'-[4-[(4-methyl-1-piperazinyl)carbonyl]phenyl]- | | CAS: | 1173204-81-3 | | MF: | C29H34N10O3 | | MW: | 570.65 | | EINECS: | | | Product Categories: | PI3K/Akt/mTOR;Akt;mTOR;PI3K | | Mol File: | 1173204-81-3.mol |  |
| | PKI-402 Chemical Properties |
| Boiling point | 670.6±55.0 °C(Predicted) | | density | 1.43 | | storage temp. | Store at -20°C | | solubility | insoluble in EtOH; insoluble in H2O; ≥14.28 mg/mL in DMSO | | form | solid | | pka | 13.80±0.70(Predicted) |
| | PKI-402 Usage And Synthesis |
| Uses | A selective, reversible and ATP-competitive Class I PI3K inhibitor. PI3Kα, IC50=1 nM; PI3Kβ, IC50=7 nM; PI3Kγ, IC50=16 nM; PI3Kδ, IC50=14 nM. | | Uses | PKI 402 is a potent pan-PI3K/mTOR dual inhibitor and a potential antitumor drug. | | Biological Activity | pki-402 is a selective, equipotent and atp-competitive class i pi3k inhibitor (ic50= 1 nm, 7 nm, 16 nm and 14 nm for pi3kα, pi3kβ, pi3kγ and pi3kδ, respectively.)pi3k (phosphatidylinositol-4,5-bisphosphate 3-kinase) is a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer. it plays a key role in pi3k/akt/mtor pathway.in multiple human cancer cell lines (e.g. breast, brain, pancreas and nscl), pki-402 inhibited growth of cancer cells, and attenuated phosphorylation of effector of pi3k and mtor. in mda-mb-361, 30 nm pki-402 caused cleaved of the apoptosis marker—parp.in mda-mb-361 mouse tumor xenograft models, administration of 100 mg/kg of pki-402 daily for 5 days decreased the initial tumor volume from 260 mm3 to 129 mm3 and inhibited tumor regrowth for 70 days, single dose of pki-402 blocked phosphorylation of akt and led to cleaved parp.1. mallon r, hollander i, feldberg l et al. antitumor efficacy profile of pki-402, a dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor. mol cancer ther. 2010 apr;9(4):976-84. | | target | PI3Kα |
| | PKI-402 Preparation Products And Raw materials |
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