
CAS Number475110-96-4
Synonyms2wxl; ZSTK474; 2-(Difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole; ZSTK-474,ZST K474; ZSTK-474; TCMDC-137004; S1072_Selleck; 2-(Difluoromethyl)-1-[4,6-di(morpholin-4-yl)-1,3,5-triazin-2-yl]-1H-benzimidazole; 4,4'-(6-(2-(difluoromethyl)-1H-benzo[d]imidazol-1-yl)-1,3,5-triazine-2,4-diyl)dimorpholine
Molecular FormulaC19H21F2N7O2
Molecular Weight417.41
Purity≥98 (HPLC)%
Density1.6±0.1 g/cm3
Boiling Point640.3±65.0 °C at 760 mmHg
Appearancepowder
| Chemical & Physical Properties | |
|---|---|
| CAS Number | 475110-96-4 |
| Catalog No. | 2A-9057339 |
| Chinese Name | ZSTK474 |
| Synonyms | 2wxl; ZSTK474; 2-(Difluoromethyl)-1-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]-1H-benzimidazole; ZSTK-474,ZST K474; ZSTK-474; TCMDC-137004; S1072_Selleck; 2-(Difluoromethyl)-1-[4,6-di(morpholin-4-yl)-1,3,5-triazin-2-yl]-1H-benzimidazole; 4,4'-(6-(2-(difluoromethyl)-1H-benzo[d]imidazol-1-yl)-1,3,5-triazine-2,4-diyl)dimorpholine |
| Molecular Formula | C19H21F2N7O2 |
| Molecular Weight | 417.41 |
| Purity | ≥98 (HPLC) |
| Density | 1.6±0.1 g/cm3 |
| Boiling Point | 640.3±65.0 °C at 760 mmHg |
| Appearance | powder |
| Storage Condition | -20°C |
| Application | ZSTK474 is an ATP-competitive pan-class I PI3K inhibitor that inhibits P13Kα, PI3Kβ, PI3Kδ and PI3Kγ with IC50 of 16 nM, 44 nM, 4.6 nM and 49 nM respectively. |
| HTC | 2934999090 |
| SMILES | FC(F)c1[n](c5c(n1)cccc5)c2nc(nc(n2)N4CCOCC4)N3CCOCC3 |
| 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 |
| InChI Key | HGVNLRPZOWWDKD-UHFFFAOYSA-N |
| NACRES Code | NA.77 |
| UNSPSC | 12352200 |
| MSDS | msds/57339_1_475110_96_4.pdf |
| Use of | ZSTK474 is an ATP-competitive pan-class I PI3K inhibitor with IC50s of16 nM, 44 nM, 4.6 nM and 49 nM for PΙ3Κα, PI3Kβ, PI3Kδ and PI3Kγ, respectively. Properties Name 4-[4-[2-(difluoromethyl)benzimidazol-1-yl]-6-morpholin-4-yl-1,3,5-triazin-2-yl]morpholine Synonym More Synonyms ZSTK474 Biological Activity Description ZSTK474 is an ATP-competitive pan-class I PI3K inhibitor with IC50s of16 nM, 44 nM, 4.6 nM and 49 nM for PΙ3Κα, PI3Kβ, PI3Kδ and PI3Kγ, respectively. Related Catalog Signaling Pathways >> Autophagy >> Autophagy Research Areas >> Cancer PI3Kα:16 nM (IC50) PI3Kβ:44 nM (IC50) PI3Kδ:4.6 nM (IC50) PI3Kγ:49 nM (IC50) In Vitro Lineweaver-Burk plot analysis revealed that ZSTK474 inhibits all four PI3K isoforms in an ATP-competitive manner. The Ki values determined for the four PI3K isoforms showed that ZSTK474 inhibited the PI3Kδ isoform most effectively with a Ki of 1.8 nM, whereas the other isoforms are inhibited with 4-10-fold higher Ki values. Therefore, ZSTK474 should be regarded as a pan-PI3K inhibitor. We also determined the IC50 values for inhibiting the four PI3K isoforms with ZSTK474 and LY294002. The IC50 values of ZSTK474 (16, 44, 4.6 and 49 nM for PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ, respectively) are shown to be consistent with the Ki values (6.7, 10.4, 1.8 and 11.7 nM for PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ, respectively), which further supported the idea that ZSTK474 inhibits PI3Kδ most potently. Even at a concentration of 100 µM, ZSTK474 inhibits mTOR activity rather weakly[1]. References [1]. Kong D, et al. ZSTK474 is an ATP-competitive inhibitor of class I phosphatidylinositol 3 kinase isoforms. Cancer Sci, 2007, 98(10), 1638-1642. Chemical & Physical Properties Molecular Formula C19H21F2N7O2 Exact Mass 417.172485 PSA 81.43000 LogP -0.21 Index of Refraction 1.711 InChIKey HGVNLRPZOWWDKD-UHFFFAOYSA-N Safety Information HS Code 2934999090 |
| Tax Rebate | 13.0% |
| Supervision | None. MFN tariff: 6.5%. Ordinary tariff: 20.0% |
| Transport Info | Product name: Summary 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
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