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| 产地 | 中国 |
| 品牌 | Chemstan |
| 货号 | LC-01 |
| 用途 | 中间体 |
| 包装规格 | 20mg |
| 纯度 | 98%% |
| CAS编号 | 372196-77-5 |
| 是否进口 | 否 |
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Fields of Application :
PIK-75 is a p110α inhibitor with IC50 of 5.8 nM (200-fold more potently than p110β), isoform-specific mutants at Ser773, and also potently inhibits DNA-PK with IC50 of 2 nM.
| CAS Number: | 372196-77-5 |
| Purity: | >98% |
| Molecular Weight: | 452.282 |
| Molecular Formula: | C16H14BrN5O4S |
Quality Control: HPLC、NMR、 LC/MS(Please contact us to get the QC report)
| Synonyms: | PIK-75 Hydrochloride; PIK 75 |
| Chemical Name: | (E)-N'-((6-bromoH-imidazo[1,2-a]pyridin-3-yl)methylene)-N,2-dimethyl-5-nitrobenzenesulfonohydrazidehydrochloride |
| Storage: | 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO |
Note: Products for research use only, not for human use
Description:
PIK-75 shows the impressive potency and iso Form selectivity at p110α while the corresponding IC50 values are 1300 nM, 76 nM and 510 nM For other PI3K iso Forms, p110β, -γ, and -δ, respectively. Furthermore, when binding to purified p110α, PIK-75 is a noncompetitive inhibitor with respect to ATP with Ki of 36 nM and competitive with respect to the substrate PI with Ki of 2.3 nM. PIK-75 also shows potent inhibition of DNA-PK. PIK-75 (1 μM) reduces cell survival by significantly decreasing mitochondrial activity in unstimulated nonasthmatic airway smooth muscle (ASM) cells, asthmatic ASM cells, and lung fibroblasts. While in TGFβ-stimulated ASM cells, PIK75 only decreases mitochondrial activity in asthmatic cells without effects in nonasthmatic cells. A recent study shows that PIK-75 (10 nM) inhibits TNF-α-induced CD38 mRNA expression and significantly attenuates of TNF-α-induced ADP-ribosyl cyclase activity in human airway smooth muscle cells. In the ErbB3WT tumor model, PIK-75 reduces in vitro chemotactic response to HRGβ1 and lowers pAkt levels by 40%. Besides, PIK-75 significantly reduces tumor cell motility and in vivo invasion in ErbB3WT primary tumors. [5] In the CD1 male mice, PIK-75 leads to serious impairments in the insulin tolerance test (ITT) and glucose tolerance test (GTT), and an increase in glucose production during a pyruvate tolerance test (PTT). [6]For the detailed information of PIK-75, the solubility of PIK-75 in water, the solubility of PIK-75 in DMSO, the solubility of PIK-75 in PBS buffer, the animal experiment (test) of PIK-75, the cell expriment (test) of PIK-75, the in vivo, in vitro and clinical trial test of PIK-75, the EC50, IC50,and Affinity of PIK-75.
References:
CC1=C(C=C(C=C1)[N+](=O)[O-])S(=O)(=O)N(C)/N=C/C2=CN=C3N2C=C(C=C3)Br.Cl
