ZSTK474
ZSTK474
CAS: 475110-96-4
Molecular Formula: C19H21F2N7O2
ZSTK474 - Names and Identifiers
ZSTK474 - Physico-chemical Properties
| Molecular Formula | C19H21F2N7O2 |
| Molar Mass | 417.41 |
| Density | 1.57 |
| Melting Point | 217-219 °C(Solv: ethanol (64-17-5)) |
| Boling Point | 640.3±65.0 °C(Predicted) |
| Solubility | Soluble in DMSO (up to 20 mg/ml) or in Ethanol (up to 2.5 mg/ml with warming). |
| Appearance | White powder. |
| Color | White or off-white |
| pKa | 5.21±0.10(Predicted) |
| Storage Condition | -20°C |
| 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. |
| Use | ZSTK474 can inhibit type I PI3K subtype, IC50 is 37 nM, and has the most significant effect on PI3Kδ. |
| In vitro study | At a concentration of 1 μm, ZSTK474 was effective in reducing PI3K activity to 4.7% of the control level, whereas LY2194002 only reduced its activity to 44.6% of the control. ZSTK474 inhibits recombinant p110β,-γ, and-δ activity with IC50 of 17 nM,53 nM, and 6 nM, respectively. ZSTK474 exhibited potent anti-proliferative activity against a panel of 39 human carcinoid cell lines, with an average GI50 of 0.32 μm, LY294002 and wortmannin were more potent than average GI50 of 7.4 μm and 10 μm, respectively. 1 μm ZSTK474 treatment blocked platelet-derived growth factor-induced cell membrane edge wave motion and PIP3 production in mouse embryonic fibroblasts (MEFs). 10 μm ZSTK474 induced OVCAR3 cell apoptosis and induced complete G1 phase arrest of cell cycle, but did not cause A549 cell apoptosis. 0.5 μm ZSTK474 treatment significantly reduced phosphorylated Akt and GSK-3β levels, as well as expression of cyclin D1 protein. ZSTK474 also dose-dependently inhibited the phosphorylation of other downstream signaling components involved in the regulation of cell proliferation, including FKHRL1,FKHR,TSC-2,mTOR, and p70S6K. ZSTK474 did not inhibit mTOR at 0.1 μm, and even at a concentration of 100 μm, ZSTK474 only inhibited mTOR activity by less than 40%. ZSTK474 blocked VEGF-induced cell migration and tube formation in human umbilical vein endothelial cells (HUVECs) and inhibited HIF-1α expression and VEGF secretion in RXF-631L of cells, showing potent in vitro anti-angiogenic activity. ZSTK474 treatment inhibits the production of IFNγ and IL-17 in T cells activated by concanavalin A and inhibits proliferation and PGE(2) production by fibroblast-like synoviocytes (FLS). |
| In vivo study | Oral administration of ZSTK474 dose-dependently inhibited the growth of B16F10 Melanoma in mice implanted subcutaneously on day 14, resulting in 100,200, 400, or 28.5% mg/kg doses, respectively, or 4.9% tumor regression, superior to the other four major anticancer drugs irinotecan,cisplatin,doxorubicin, and 5-fluorouracil, with respective maximum tolerated doses for tumor regression of 96%,35.7%,24%, or 68.3%. ZSTK474 treatment at 400 mg/kg completely inhibited the growth of A549,PC-3, and WiDr in mice and induced the regression of A549 xenografts. ZSTK474 significantly inhibited tumor growth in the RXF-631L xenograft model, consistent with a significant reduction in the number of microvessels in ZSTK474 treated mice. Oral administration of ZSTK474 ameliorates the development of adjuvant arthritis in rats. |
ZSTK474 - Risk and Safety
| HS Code | 29349990 |
ZSTK474 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.396 ml | 11.978 ml | 23.957 ml |
| 5 mM | 0.479 ml | 2.396 ml | 4.791 ml |
| 10 mM | 0.24 ml | 1.198 ml | 2.396 ml |
| 5 mM | 0.048 ml | 0.24 ml | 0.479 ml |
Last Update：2024-01-02 23:10:35
ZSTK474 - Reference Information
| biological activity | ZSTK474 inhibits type I PI3K subtype. in cell-free test, IC50 is 37 nM, which has the most significant effect on PI3Kδ. Phase 1/2. |
| target | TargetValue PI3Kδ (Cell-free say) 4.6 nM PI3Kα (Cell-free say) 16 nM PI3K (Cell-free say) 37 nM PI3Kβ (Cell-free say) 44 nM PI3Kγ (Cell-free say) 49 nM |
| Target | Value |
| PI3Kδ (Cell-free assay) | 4.6 nM |
| PI3Kα (Cell-free assay) | 16 nM |
| PI3K (Cell-free assay) | 37 nM |
| PI3Kβ (Cell-free assay) | 44 nM |
| PI3Kγ (Cell-free assay) | 49 nM |
| in vitro study | ZSTK474 effectively reduced PI3K activity to 4.7% of the control group level at a concentration of 1 μM, while the LY2194002 only reduced its activity to 44.6% of the control group. ZSTK474 inhibited recombinant p110β,-γ, and-δ activities with IC50 of 17 nM,53 nM, and 6 nM, respectively. ZSTK474 showed effective antiproliferative activity against a group of 39 human carcinoid cell lines with an average GI50 of 0.32 μM, which was more effective than LY294002 and wortmannin with an average GI50 of 7.4 μM and 10 μM, respectively. 1 μM ZSTK474 therapy blocked platelet-derived growth factor-induced membrane marginal wave and PIP3 production in mouse embryonic fibroblasts (MEFs). 10 μM ZSTK474 induced apoptosis of OVCAR3 cells and induced complete G1 phase arrest of cell cycle, but did not cause apoptosis of A549 cells. 0.5 μM ZSTK474 treatment significantly reduced phosphorylated Akt and GSK-3β levels and cyclin D1 protein expression. ZSTK474 also dose-dependently inhibits phosphorylation of other downstream signaling components involved in cell proliferation regulation, including FKHRL1,FKHR,TSC-2,mTOR, and p70S6K. ZSTK474 did not inhibit mTOR at 0.1 μM, even at 100 μM concentration, ZSTK474 only inhibited less than 40% of mTOR activity. ZSTK474 blocked VEGF-induced cell migration and lumen formation in human umbilical vein endothelial cells (HUVECs), and inhibited HIF-1α expression and VEGF secretion in RXF-631L cells, showing effective anti-angiogenic activity in vitro. ZSTK474 treatment inhibited IFNγ and IL-17 production in concanavalin A- activated T cells, and inhibited proliferation and PGE(2) production by fibroblast-like synovial cells (FLS). |
| in vivo study | ZSTK474 oral administration, dose-dependent inhibition of subcutaneous implanted mice B16F10 melanoma growth, at the dose of 100,200, or 400 mg/kg on the 14th day, 28.5%,7.1%, or 4.9% tumor regression is produced, respectively, the effect is better than that of the other four main anticancer drugs, irinotecan,cisplatin,doxorubicin, and 5-fluorouracil, which have their respective maximum tolerated doses of 96%,35.7%,24%, or 68.3% for tumor regression. 400 mg/kg ZSTK474 therapy completely inhibited the growth of A549,PC-3, and WiDr in mice and induced regression of A549 transplanted tumor. ZSTK474 significantly inhibited tumor growth in RXF-631L xenograft models, consistent with a significant reduction in the number of microvasculature in ZSTK474-treated mice. In rats, ZSTK474 oral administration improves the development of adjuvant arthritis. |
Last Update：2024-04-09 20:45:29
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CAS: 475110-96-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
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Product Name: ZSTK474 Request for quotationCAS: 475110-96-4
Tel: 0712-8899838
Email: jy6101@rmastandards.com
Mobile: 86-15787876101
QQ: 2518299249
Wechat: 15787876101
Multiple SpecificationsSpot supply
Product Name: ZSTK474 Request for quotationCAS: 475110-96-4
Tel: 400-968-2212
Email: 3623107365@qq.com
Mobile: 18916960931
QQ: 3623107365
Wechat: 18916960931
Spot supply
Product Name: ZSTK474 Visit Supplier Webpage Request for quotationCAS: 475110-96-4
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328
WhatsApp: +86-18821248368
Spot supply
Product Name: ZSTK474 Visit Supplier Webpage Request for quotationCAS: 475110-96-4
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922
Wechat: 18621343501
WhatsApp: +86-18621343501
Spot supply
Product Name: ZSTK474 Visit Supplier Webpage Request for quotationCAS: 475110-96-4
Tel: 609-228-6898
Email: sales@medchemexpress.com
tech@medchemexpress.com
Mobile: 609-228-6898
Product Name: ZSTK474 Visit Supplier Webpage Request for quotation
CAS: 475110-96-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
CAS: 475110-96-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
View History
ZSTK474
NAPHTHALENE BLACK B
m-Methoxystyrene
exo-3-Benzyl-3-azabicyclo...
OCPA
Lead ribbon
alpha-Irone
RARECHEM AL BE 0472
Residuum
NSC 55746
NAPHTHALENE BLACK B
m-Methoxystyrene
exo-3-Benzyl-3-azabicyclo...
OCPA
Lead ribbon
alpha-Irone
RARECHEM AL BE 0472
Residuum
NSC 55746