Company Name: |
ChemeGen(Shanghai) Biotechnology Co.,Ltd.
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Tel: |
18818260767 |
Email: |
sales@chemegen.com |
Products Intro: |
Product Name:KP372-1 CAS:1374996-60-7 Purity:98% Package:10 mg;50 mg;100 mg;500 mg;1 g;5 g;10 g
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Company Name: |
Absin Bioscience Inc.
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Tel: |
021-38015121 15000105423 |
Email: |
wulan@absin.cn |
Products Intro: |
Product Name:KP372-1 CAS:1374996-60-7 Purity:>98% Package:5mg;10mg
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Company Name: |
MedBioPharmaceutical Technology Inc
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Tel: |
021-69568360 18916172912 |
Email: |
order@med-bio.cn |
Products Intro: |
Product Name:6H-INDENO[1,2-E]TETRAZOLO[1,5-B][1,2,4]TRIAZIN-6-ONE CAS:1374996-60-7 Purity:98% Package:5mg; 1mg; 10mg Remarks:Medbio
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Company Name: |
TargetMol Chemicals Inc.
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Tel: |
4008200310 |
Email: |
marketing@tsbiochem.com |
Products Intro: |
Product Name:KP372-1 CAS:1374996-60-7 Purity:98% Package:10mg/RMB 8780;5mg/RMB 4720;1mg/RMB 1270
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| 6H-INDENO[1,2-E]TETRAZOLO[1,5-B][1,2,4]TRIAZIN-6-ONE Basic information |
Product Name: | 6H-INDENO[1,2-E]TETRAZOLO[1,5-B][1,2,4]TRIAZIN-6-ONE | Synonyms: | ZERENEX E/6026591;6H-INDENO[1,2-E]TETRAZOLO[1,5-B][1,2,4]TRIAZIN-6-ONE;10H-Indeno[2,1-e]tetrazolo[1,5-b][1,2,4]triazin-10-one (1:1) | CAS: | 1374996-60-7 | MF: | C20H8N12O2 | MW: | 448.37 | EINECS: | | Product Categories: | | Mol File: | Mol File | |
| 6H-INDENO[1,2-E]TETRAZOLO[1,5-B][1,2,4]TRIAZIN-6-ONE Chemical Properties |
storage temp. | 2-8°C | solubility | DMSO: soluble10mg/mL, clear | form | powder | color | light yellow to dark yellow |
Hazard Codes | Xn | Risk Statements | 22 | WGK Germany | 3 |
| 6H-INDENO[1,2-E]TETRAZOLO[1,5-B][1,2,4]TRIAZIN-6-ONE Usage And Synthesis |
Description | KP372-1 is a specific Akt inhibitor that demonstrates at least 10-fold selectivity against a panel of additional kinase targets, including CDK1, ERK1, GSK3β, LCK, MEK1, PKA, PKC, and S6K. By blocking Akt signaling, KP372-1 has been shown to inhibit proliferation and to induce apoptosis of thyroid cancer cells with an IC50 value of 30-60 nM in vitro. In acute myelogenous leukemia cells, KP372-1 is reported to inhibit the kinase activity of Akt, PDK1, and FLT3, decreasing the colony-forming ability of these cells with an IC50 value less than 200 nM. | Uses | KP372-1 is a specific Akt inhibitor that demonstrates at least 10-fold selectivity against a panel of additional kinase targets, including CDK1, ERK1, GSK3β, LCK, MEK1, PKA, PKC, and S6K. By blocking Akt signaling, KP372-1 has been shown to inhibit proliferation and to induce apoptosis of thyroid cancer cells. | in vitro | a previous study found that kp372-1 could block signalling downstream of akt in thyroid tumour cells, resulting in inhibition of cell proliferation and increased apoptosis [1]. another study showed that kp372-1 directly inhibited the kinase activity of akt, flt3, and pdk1concentration-dependently. western blot analyses indicated kp372-1 decreased the phosphorylation of akt on both ser(473) and thr(308). moreover, the treatment of aml cell lines with kp372-1 led to rapid generation of reactive oxygen species and stimulation of oxygen consumption. in addition, kp372-1 was able to induce pronounced apoptosis in aml cell lines and primary samples irrespective of their flt3 status, but not in normal cd34(+) cells [2]. | IC 50 | 30-60 nm for thyroid cancer cells | references | [1] mandal, m. ,kim, s.,younes, m.n., et al. the akt inhibitor kp372-1 suppresses akt activity and cell proliferation and induces apoptosis in thyroid cancer cells. british journal of cancer 92(10), 1899-1905 (2005). [2] zeng, z. ,samudio, i.j.,zhang, w., et al. simultaneous inhibition of pdk1/akt and fms-like tyrosine kinase 3 signaling by a small-molecule kp372-1 induces mitochondrial dysfunction and apoptosis in acute myelogenous leukemia. cancer research 66(7), 3737-3746 (2006). |
| 6H-INDENO[1,2-E]TETRAZOLO[1,5-B][1,2,4]TRIAZIN-6-ONE Preparation Products And Raw materials |
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