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BOC Sciences |
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| Product Name: | PIK-75 | | Synonyms: | 2-Methyl-5-nitro-1-benzenesulfonic acid 2-[(6-bromoimidazo[1,2-a]pyridin-3-yl)methylene]-1-methylhydrazide;PIK-75 Hydrochloride;Benzenesulfonic acid, 2-Methyl-5-nitro-, 2-[(6-broMoiMidazo[1,2-a]pyridin-3-yl)Methylene]-1-Methylhydrazide;PIK75(HCl salt);PI3-Kinase a Inhibitor VIII;PIK 75;CS-669;PIK-75, free base | | CAS: | 372196-67-3 | | MF: | C16H14BrN5O4S | | MW: | 452.28 | | EINECS: | | | Product Categories: | Inhibitors;Antineoplastic | | Mol File: | 372196-67-3.mol |  |
| | PIK-75 Chemical Properties |
| Melting point | >203°C (dec.) | | density | 1.66±0.1 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | Chloroform (Slightly), DMSO (Slightly), Methanol (Slightly, Heated) | | form | Solid | | pka | 2.08±0.50(Predicted) | | color | Light Yellow to Yellow |
| | PIK-75 Usage And Synthesis |
| Uses | PIK-75 is a p110α inhibitor, isoform-specific mutants at Ser773, and also potently inhibits DNA-PK. | | Definition | ChEBI: N-[(6-bromo-3-imidazo[1,2-a]pyridinyl)methylideneamino]-N,2-dimethyl-5-nitrobenzenesulfonamide is a sulfonamide. | | in vivo | PIK-75 (2 mg/kg) potentiates anticancer activity of Gemcitabine (20 mg/kg) in vivo. Gemcitabine (20 mg/kg) or PIK-75 (2 mg/kg) alone reduces the tumor growth to similar degree. Beneficial effect of PIK-75/Gemcitabine is evident as this combination markedly reduces the tumor growth in vivowithout affecting the body weights of mice[3]. | Animal Model: | Mice bearing tumors of MIA PaCa-2[3] | | Dosage: | 2 mg/kg; or combination with Gemcitabine (20 mg/kg) | | Administration: | Administered injection; 5 times per week. 25 days | | Result: | Reduced the tumor growth and enhanced the antitumor effect. |
| | Enzyme inhibitor | This novel phosphoinositide-3 kinase p110α inhibitor (F.Wt. = 488.74; CAS 372196-67-3; Solubility (25°C): 98 mg/mL DMSO, <1 mg/mL Water), also known as (E)-N'-((6-bromoH-imidazo[1,2-a]pyridin-3-yl)methylene)-N,2- dimethyl-5-nitrobenzenesulfonohydrazide-HCl, competes with respect to a substrate (phosphatidylinositol, PI), unlike most other PI3K inhibitors, which bind at or near the ATP site. PIK-75 exhibits impressive isoform selectivity, with an IC50 value of 5.8 nM for p110α, while the corresponding IC50 values are 1300 nM, 76 nM and 510 nM for p110β, p110γ, and p110δ, respectively. | | IC 50 | DNA-PK: 2 nM (IC50); p110α: 5.8 nM (IC50); p110γ: 76 nM (IC50); p110δ: 510 nM (IC50); p110β: 1.3 μM (IC50); hsVPS34: 2.6 μM (IC50); PI3KC2β: 1 μM (IC50); PI3KC2α: 10 μM (IC50); mTORC1: 1 μM (IC50); mTORC2: 10 μM (IC50); ATM: 2.3 μM (IC50); ATR: 21 μM (IC50); PI4KIIIβ: 50 μM (IC50) |
| | PIK-75 Preparation Products And Raw materials |
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