6H-INDENO[1,2-E]TETRAZOLO[1,5-B][1,2,4]TRIAZIN-6-ONE
![6H-INDENO[1,2-E]TETRAZOLO[1,5-B][1,2,4]TRIAZIN-6-ONE Structure](StructureFile/ChemBookStructure3/GIF/CB8270212.gif)
- CAS No.
- 1374996-60-7
- Chemical 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)
- CBNumber:
- CB8270212
- Molecular Formula:
- C20H8N12O2
- Molecular Weight:
- 448.37
- MDL Number:
- MFCD00615743
- MOL File:
- Mol file
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302 | |||||||||
| Precautionary statements | P264-P270-P301+P312-P330-P501 | |||||||||
| Hazard Codes | Xn | |||||||||
| Risk Statements | 22 | |||||||||
| WGK Germany | 3 | |||||||||
| NFPA 704 |
|
6H-INDENO[1,2-E]TETRAZOLO[1,5-B][1,2,4]TRIAZIN-6-ONE price More Price(9)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | SML1029 | KP372-1 1:1 mixture of two isomers | 1374996-60-7 | 5mg | $110 | 2022-05-15 | Buy |
| Sigma-Aldrich | SML1029 | KP372-1 1:1 mixture of two isomers | 1374996-60-7 | 25mg | $435 | 2022-05-15 | Buy |
| Cayman Chemical | 17808 | KP372-1 ≥95% (sum of isomers) | 1374996-60-7 | 1mg | $73 | 2024-03-01 | Buy |
| Cayman Chemical | 17808 | KP372-1 ≥95% (sum of isomers) | 1374996-60-7 | 5mg | $270 | 2024-03-01 | Buy |
| Cayman Chemical | 17808 | KP372-1 ≥95% (sum of isomers) | 1374996-60-7 | 10mg | $502 | 2024-03-01 | Buy |
6H-INDENO[1,2-E]TETRAZOLO[1,5-B][1,2,4]TRIAZIN-6-ONE Chemical Properties,Uses,Production
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
Raw materials
Preparation Products
6H-INDENO[1,2-E]TETRAZOLO[1,5-B][1,2,4]TRIAZIN-6-ONE Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32038 | 58 |
| Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 52925 | 58 |
| ChemeGen(Shanghai) Biotechnology Co.,Ltd. | 18818260767 | sales@chemegen.com | China | 11217 | 58 |
| Absin Bioscience Inc. | 021-38015121 15000105423 | wulan@absin.cn | China | 24731 | 58 |
| MedBioPharmaceutical Technology Inc | 021-69568360 18916172912 | order@med-bio.cn | China | 8140 | 58 |
| TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24649 | 58 |
| Shanghai Yifei Biotechnology Co. , Ltd. | 021-65675885 18964387627 | customer_service@efebio.com | China | 11974 | 58 |
| RD International Technology Co., Limited | 18024082417 | market@ubiochem.com | China | 9272 | 58 |
| ApexBio Technology | -- | sales@apexbt.com | United States | 6251 | 58 |
