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17β-hydroxy Wortmannin
17β-hydroxy Wortmannin
- CAS No.58053-83-1
- Chemical Name:17β-hydroxy Wortmannin
- CBNumber:CB53152437
- Molecular Formula:C23H26O8
- Formula Weight:430.45
- MOL File:58053-83-1.mol
17β-hydroxy Wortmannin Property
- Boiling point 615.4±55.0 °C(Predicted)
- Density 1.39±0.1 g/cm3(Predicted)
- storage temp. +2C to +8C
- solubility DMF: 3 mg/ml; DMF:PBS (pH 7.2) (1:9): 0.1 mg/ml; DMSO: 2.5 mg/ml; Ethanol: 0.15 mg/ml
- form Off-white solid
- pka 14.49±0.70(Predicted)
- color off-white
- UNSPSC Code 12352200
Safety
-
Symbol(GHS)
- Signal wordDanger
- Hazard statements H300+H310+H330
- Precautionary statements P260-P262-P264-P270-P271-P280-P284-P301+P310-P330-P302+P352-P304+P340-P320-P361+P364-P403+P233-P405-P501
17β-hydroxy Wortmannin Price
More Price(1)
- Brand: Sigma-Aldrich(India)
- Product number: 528119
- Product name : PI 3-K Inhibitor XI, HWT - CAS 58053-83-1 - Calbiochem
- Purity: The PI 3-K Inhibitor XI, HWT, also referenced under CAS 58053-83-1, controls the biological activity of PI 3-K. This small molecule/inhibitor is prima
- Packaging: 5MG
- Price: ₹26250
- Updated: 2022/06/14
- Buy: Buy
17β-hydroxy Wortmannin Chemical Properties,Usage,Production
-
Description
17β-
hydroxy Wortmannin is an analog of wortmannin. It irreversibly binds phosphoinositide 3- kinase (PI3K) and potently blocks fMLP- stimulated respiratory burst in neutrophils (IC50 = 5 nM). 17β- hydroxy Wortmannin inhibits recombinant PI3K and mTOR (IC50 = 2.7 and 193 nM, respectively) and prevents the growth of LNCap prostate cancer cells (IC50 = 1.46 μM). The 17- hydroxyl group has been used to further modify this compound, e.g., by pegylation and conjugation with rapamycin. - Uses 17β-Hydroxywortmannin (Wortmannin-17β-ol) is an orally active inhibitor for phosphatidylinositol-3-kinase (PI-3-kinase) with an IC50 of 0.5 nM, suppresses the osteoclast resorption with an IC50 of 10 nM[1]. 17β-Hydroxywortmannin exhibits antitumor activity[2].
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in vivo
17β-Hydroxywortmannin (0.1 μg/kg, p.o. for 5 weeks) exhibits activity in osteoclast differentation and prevent an estrogen-deficiency induced bone loss in ovafiectomized OVX rats[1].
17β-Hydroxywortmannin (2.5 mg/kg/week, i.v. for 2 weeks) exhibits antitumor efficacy towards U87MG glioma with a therapeutic index of 26 in human tumor xenografted nude mice[2].Animal Model: ovafiectomized rat[1] Dosage: 0.1 μg/kg/day Administration: p.o. for 5 weeks Result: Reduced the bone loss without significant toxicity. Animal Model: U87MG glioma xenografted nude mice[2] Dosage: 2.5 mg/kg/week Administration: i.v. for 2 weeks Result: Inhibited tumor growth. - IC 50 PI3K: 0.5 nM (IC50)
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References
[1] Hall TJ, et al., Wortmannin, a potent inhibitor of phosphatidylinositol 3-kinase, inhibits osteoclastic bone resorption in vitro. Calcif Tissue Int. 1995 Apr;56(4):336-8. DOI:10.1007/BF00318056
[2] Zask A, et al., Synthesis and structure-activity relationships of ring-opened 17-hydroxywortmannins: potent phosphoinositide 3-kinase inhibitors with improved properties and anticancer efficacy. J Med Chem. 2008 Mar 13;51(5):1319-23. DOI:10.1021/jm7012858
17β-hydroxy Wortmannin Preparation Products And Raw materials
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- 抑制剂
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- 化合物 17Β-HYDROXYWORTMANNIN
- 58053-83-1
- PI 3-K Inhibitor XI, HWT
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- PI 3-K Inhibitor XI, HWT - CAS 58053-83-1 - Calbiochem
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