| Identification | Back Directory | [Name]
PIK-75 | [CAS]
372196-67-3 | [Synonyms]
PIK 75
CS-669
PIK75(HCl salt)
PIK-75, free base
PIK-75 Hydrochloride
PI3-Kinase a Inhibitor VIII
N'-((6-Bromoimidazo[1,2-a]pyridin-3-yl)methylene)-N,2-dimethyl-5-nitrobenzenesulfonohydrazide
(Z)-N'-((6-bromoimidazo[1,2-a]pyridin-3-yl)methylene)-N,2-dimethyl-5-nitrobenzenesulfonohydrazide
2-Methyl-5-nitro-1-benzenesulfonic acid 2-[(6-bromoimidazo[1,2-a]pyridin-3-yl)methylene]-1-methylhydrazide
Benzenesulfonic acid, 2-Methyl-5-nitro-, 2-[(6-broMoiMidazo[1,2-a]pyridin-3-yl)Methylene]-1-Methylhydrazide | [Molecular Formula]
C16H14BrN5O4S | [MDL Number]
MFCD20526318 | [MOL File]
372196-67-3.mol | [Molecular Weight]
452.28 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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. | [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. | [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. |
| [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) |
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