ZSTK474
- CAS No.
- 475110-96-4
- Chemical Name:
- ZSTK474
- Synonyms
- CS-438;ZSTK 474;ZSTK474 BASE;ZSTK474 ，S1072;ZSTK474/ZSTK-474;ZSTK474 USP/EP/BP;ZSTK474, 10 mM in DMSO;ZSTK474, ATP-competitve PI3K inhibitor;2-(2-Difluoromethylbenzimidazol-1-yl)-4,6-dimorpholino-1,3,5-triazine;2-(DifluoroMethyl)-1-[4,6-di(4-Morpholinyl)-1,3,5-triazin-2-yl]-1H-benziMidaz
- CBNumber:
- CB0505419
- Molecular Formula:
- C19H21F2N7O2
- Molecular Weight:
- 417.41
- MDL Number:
- MFCD08705334
- MOL File:
- 475110-96-4.mol
| Product description | Number | Pack Size | Price |
| ZSTK 474 | D6342 | 100MG | $267 |
| ZSTK474 ≥98% | 17381 | 5mg | $49 |
| ZSTK474 ≥98% | 17381 | 10mg | $77 |
| ZSTK474 ≥98% | 17381 | 25mg | $168 |
| ZSTK474 ≥98% | 17381 | 50mg | $263 |
| More product size | |||
| Melting point | 217-219 °C(Solv: ethanol (64-17-5)) |
|---|---|
| Boiling point | 640.3±65.0 °C(Predicted) |
| Density | 1.57 |
| storage temp. | -20°C |
| solubility | Soluble in DMSO (up to 20 mg/ml) or in Ethanol (up to 2.5 mg/ml with warming). |
| pka | 5.21±0.10(Predicted) |
| form | White powder. |
| color | White or off-white |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months. |
| InChI | InChI=1S/C19H21F2N7O2/c20-15(21)16-22-13-3-1-2-4-14(13)28(16)19-24-17(26-5-9-29-10-6-26)23-18(25-19)27-7-11-30-12-8-27/h1-4,15H,5-12H2 |
| InChIKey | HGVNLRPZOWWDKD-UHFFFAOYSA-N |
| SMILES | C1(C(F)F)N(C2=NC(N3CCOCC3)=NC(N3CCOCC3)=N2)C2=CC=CC=C2N=1 |
| FDA UNII | K0068GK39A |
| UNSPSC Code | 12352200 |
| NACRES | NA.77 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H315-H319-H335 |
| Precautionary statements | P264-P280-P302+P352-P321-P332+P313-P362-P305+P351+P338-P337+P313-P261-P271-P304+P340-P312-P403+P233-P405-P501 |
| WGK Germany | WGK 3 |
| HS Code | 29349990 |
| Storage Class | 11 - Combustible Solids |
ZSTK474 price More Price(30)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| TCI Chemical | D6342 | ZSTK 474 | 475110-96-4 | 100MG | $267 | 2025-07-31 | Buy |
| Cayman Chemical | 17381 | ZSTK474 ≥98% | 475110-96-4 | 5mg | $49 | 2024-03-01 | Buy |
| Cayman Chemical | 17381 | ZSTK474 ≥98% | 475110-96-4 | 10mg | $77 | 2024-03-01 | Buy |
| Cayman Chemical | 17381 | ZSTK474 ≥98% | 475110-96-4 | 25mg | $168 | 2024-03-01 | Buy |
| Cayman Chemical | 17381 | ZSTK474 ≥98% | 475110-96-4 | 50mg | $263 | 2024-03-01 | Buy |
ZSTK474 Chemical Properties,Uses,Production
Description
ZSTK474 (475110-96-4) is a novel Class I phosphatidylinositol 3-kinase (PI3K) inhibitor. ZSTK474 is an ATP-competitive inhibitor of all four Class I PI3K isoforms. However, it inhibits PI3Kδ most potently, with a Ki of 1.8 nM, while inhibiting the α, β and γ isoforms at slightly higher concentrations (6.7 nM, 10.4 nM and 11.7 nM, respectively)1. Displays potent antitumor activity against human cancer xenografts (A549, PC-3 and WiDr) when administered to mice2. ZSTK474 displays potent anti-inflammatory activity via modulation of human CD14+ monocyte-derived dendritic cell functions and suppresses experimental autoimmune encephalomyelitis3. Ameliorates the progression of adjuvant-induced arthritis in a rat model4.
Uses
ZSTK474 is a triazine derivative that acts as an inhibitor of class I phosphatidylinositol 3-kinase (PI3K) isoforms (IC50s = 17, 53, and 6 nM for p110β, -γ, and -δ, respectively). It is selective for PI3K, as it has negligible activity against 139 other kinases when tested at 30 μM. ZSTK474 is orally bioavailable and shows strong antitumor activity against human cancer xenografts in mice. The efficacy of ZSTK474 against certain cancer cells and tumors can be enhanced by combination therapy.
Uses
ZSTK474 is an ATP-competitive inhibitor of class I phosphatidylinositol 3 kinase (PI3K) isoforms. Potent PI3K inhibitor.
Definition
ChEBI: A triamino-1,3,5-triazine that is 1,3,5-triazine in which two of the hydrogens have been replaced by morpholin-4-yl groups while the third hydrogen has been replaced by a 2-(difluoromethyl)benzimidazol-1-yl group. It is an inhibitor of phosphatidylinositol 3-kinase.
in vivo
In mice subjected to MCAO, treatment with ZSTK474 is tested at dosages of 50, 100, 200, and 300 mg/kg. Since the 200 mg/kg dose produces significant improvement and no obvious toxic effects (P<0.01), mice are treated with ZSTK474 at a dose of 200 mg/kg/day daily for three post-MCAO days during the remaining experiments of this study. Neurological function is examined in mice suffered from MCAO followed by 24, 48, and 72 h of reperfusion. In the ZSTK474 group, neurological function scores are significantly better than the control group except the corner test[2].
target
PI3Kδ
IC 50
PI3Kδ: 4.6 nM (IC50); PI3Kα: 16 nM (IC50); PI3Kβ: 44 nM (IC50); PI3Kγ: 49 nM (IC50); Autophagy
References
[1] DEXIN KONG Takao Y. ZSTK474 is an ATP-competitive inhibitor of class I phosphatidylinositol 3 kinase isoforms[J]. Cancer Science, 2007, 98 10: 1638-1642. DOI:10.1111/j.1349-7006.2007.00580.x
[2] SHIN-ICHI YAGUCHI. Antitumor activity of ZSTK474, a new phosphatidylinositol 3-kinase inhibitor.[J]. JNCI Journal of the National Cancer Institute, 2006, 98 8: 545-556. DOI:10.1093/jnci/djj133
[3] ZHENYI XUE. ZSTK474, a novel PI3K inhibitor, modulates human CD14+ monocyte-derived dendritic cell functions and suppresses experimental autoimmune encephalomyelitis.[J]. Journal of Molecular Medicine-Jmm, 2014, 92 10: 1057-1068. DOI:10.1007/s00109-014-1158-x
[4] KAZUHIKO HARUTA. Inhibitory effects of ZSTK474, a phosphatidylinositol 3-kinase inhibitor, on adjuvant-induced arthritis in rats.[J]. Inflammation Research, 2012: 551-562. DOI:10.1007/s00011-012-0444-8
ZSTK474 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Capot Chemical Co.,Ltd. | +86-（0）57185586718; +8613336195806 | sales@capot.com | China | 29735 | 60 |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
| career henan chemical co | +86-0371-86658258 +8613203830695 | sales@coreychem.com | China | 29830 | 58 |
| Alchem Pharmtech,Inc. | 8485655694 | sales@alchempharmtech.com | United States | 63687 | 58 |
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | sales@conier.com | China | 49977 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; +17819995354 | marketing@targetmol.com | United States | 32470 | 58 |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | 1026@dideu.com | China | 18884 | 58 |
| Dayang Chem (Hangzhou) Co.,Ltd. | +86-0571-88938639 +8617705817739 | info@dycnchem.com | China | 52725 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471; | sales@sarms4muscle.com | China | 10473 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
