CS-1918
VX-745
CAS: 209410-46-8
Molecular Formula: C19H9Cl2F2N3OS
CS-1918 - Names and Identifiers
CS-1918 - Physico-chemical Properties
| Molecular Formula | C19H9Cl2F2N3OS |
| Molar Mass | 436.26 |
| Density | 1.55±0.1 g/cm3(Predicted) |
| Melting Point | 261-264 °C |
| Boling Point | 578.9±60.0 °C(Predicted) |
| Solubility | DMSO: 43.6 mg/mL (100 mM)( < 1 mg/ml refers to the product slightly soluble or insoluble) |
| Appearance | powder |
| Color | white to beige |
| pKa | -0.97±0.40(Predicted) |
| Storage Condition | -20°C |
| Use | Neflamapimod (VX-745) is an effective, highly selective p38α inhibitor that can cross the blood-brain barrier. The IC50 value for p38α is 10 nM and the IC50 value for p38β is 220 nM. Neflamapimod (VX-745) has anti-inflammatory activity. |
| In vitro study | VX-745 selective inhibition of p38α and p38β MAPK with IC50 of 10nM and 220 nM, respectively, but had no effect on p38γ MAPK and other kinases with IC50 greater than 20 μm. In the human peripheral blood mononuclear cell (PBMC) assay, the IC50 for VX-745 inhibition of IL-1β and TNF were 56 and 52nm, respectively. VX-745 inhibited IL-1 and TNFα, induced IL-6 and IL-8 production, and inhibited LPS and IL-1β regulated COX-2 synthesis. 60 nM-20 µm VX-745 inhibited the secretion of IL-6 and VEGF in bone marrow stromal cells (BMSCs), and did not affect the viability of the cells. VX-745 action on BMSCs also inhibited TNF-α induced secretion by IL-6. VX-745 acts on BMSCs, inhibits MM cell proliferation and IL-6 secretion through MM cell adhesion to BMSCs, indicating that VX-745 can inhibit paracrine MM cell growth and overcome cell adhesion-related drug resistance. VX-745 selectively inhibited p38α and p38β MAPK with IC50 of 10nM and 220 nM, respectively, but had no effect on p38γ MAPK and other kinases with IC50 greater than 20 μm. In the human peripheral blood mononuclear cell (PBMC) assay, the IC50 for VX-745 inhibition of IL-1β and TNF were 56 and 52nm, respectively. VX-745 inhibited IL-1 and TNFα, induced IL-6 and IL-8 production, and inhibited LPS and IL-1β regulated COX-2 synthesis. 60 nM-20 µm VX-745 inhibited the secretion of IL-6 and VEGF in bone marrow stromal cells (BMSCs), and did not affect the viability of the cells. VX-745 action on BMSCs also inhibited TNF-α induced secretion by IL-6. VX-745 acts on BMSCs, inhibits MM cell proliferation and IL-6 secretion through MM cell adhesion to BMSCs, indicating that VX-745 can inhibit paracrine MM cell growth and overcome cell adhesion-related drug resistance. |
| In vivo study | VX-745 effective treatment of adjuvant arthritis in mice, ED50 is 5 mg/kg. VX-745, the mice with adjuvant arthritis inhibited bone resorption by 93% and inhibited inflammation by 56%. VX-745 effect on cartilage induced arthritis, showed dose response decreased. 2.5, 5, and 10 mg/kgVX-745 in the rat model of type II collagen-induced arthritis increased the inflammatory effect by 27%, 31%, and 44%, respectively, compared to the control group. In addition, VX-745 protects 32-39% of bone and cartilage. VX-745 effective treatment of adjuvant arthritis in mice with an ED50 of 5 mg/kg. VX-745, the mice with adjuvant arthritis inhibited bone resorption by 93% and inhibited inflammation by 56%. VX-745 effect on cartilage induced arthritis, showed dose response decreased. 2.5, 5, and 10 mg/kgVX-745 in the rat model of type II collagen-induced arthritis increased the inflammatory effect by 27%, 31%, and 44%, respectively, compared to the control group. In addition, VX-745 protects 32-39% of bone and cartilage. |
CS-1918 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.292 ml | 11.461 ml | 22.922 ml |
| 5 mM | 0.458 ml | 2.292 ml | 4.584 ml |
| 10 mM | 0.229 ml | 1.146 ml | 2.292 ml |
| 5 mM | 0.046 ml | 0.229 ml | 0.458 ml |
Last Update：2024-01-02 23:10:35
CS-1918 - Cell Experiment
BMSCs (5 × 104 cells/well) or MM cells (3 × 104 cells/well) are incubated in 96-well culture plates in the presence or absence of VX-745 for 48 hours at 37 °C. DNA synthesis is measured by [3H]-thymidine ([3H]TdR) uptake. Cells are pulsed with [3H]TdR (0.5 μCi/well [.0185 MBq]) during the last 8 hours of 48-hour cultures. Growth inhibition of both MM cells and BMSCs by VX-745.(Only for Reference). Cell lines: Human bone marrow stromal cells (BMSCs) and multiple myeloma (MM) cells
Last Update：2023-08-16 21:32:38
CS-1918 - Animal Experiment
Animal model: Type II collagen-induced arthritis (CIA) mice model (DBA/1J)
Last Update：2023-08-16 21:32:38
CS-1918 - Reference Information
| biological activity | VX-745 is an effective, selective p38α inhibitor with IC50 of 10 nM, 22 times higher selectivity than p38β and no inhibitory effect on p38γ. Neflamapimod (VX-745) is an effective, selective p38α inhibitor with IC50 of 10 nM, 22 times higher selectivity than p38β, and has no inhibitory effect on p38γ. |
| in vitro study | VX-745 selectively inhibit p38α and p38β MAPK,IC50 is 10nM and 220 nM respectively, but it has no effect on p38γ MAPK and other kinases, IC50 is greater than 20 µM. In human peripheral vascular mononuclear cells (PBMC) experiments, IC50 was 56 and 52nM respectively when VX-745 inhibited IL-1β and TNF. VX-745 inhibit IL-1 and TNFα, induced IL-6 and IL-8 production, and inhibit COX-2 synthesis regulated by LPS and IL-1β. 60 nM-20 µM VX-745 acts on bone marrow stromal cells (BMSCs), inhibits IL-6 and VEGF secretion, and does not affect cell viability. VX-745 action on BMSCs also inhibited TNF-α-induced IL-6 secretion. VX-745 acts on BMSCs and adheres to BMSCs through MM cells to inhibit MM cell proliferation and IL-6 secretion, indicating that VX-745 can inhibit paracrine MM cell growth and overcome cell adhesion-related drug resistance. VX-745 selectively inhibits p38α and p38β MAPK,IC50 is 10nM and 220 nM respectively, but it has no effect on p38γ MAPK and other kinases, IC50 is greater than 20 µM. In human peripheral vascular mononuclear cells (PBMC) experiments, IC50 was 56 and 52nM respectively when VX-745 inhibited IL-1β and TNF. VX-745 inhibit IL-1 and TNFα, induced IL-6 and IL-8 production, and inhibit COX-2 synthesis regulated by LPS and IL-1β. 60 nM-20 µM VX-745 acts on bone marrow stromal cells (BMSCs), inhibits IL-6 and VEGF secretion, and does not affect cell viability. VX-745 action on BMSCs also inhibited TNF-α-induced IL-6 secretion. VX-745 acts on BMSCs and adheres to BMSCs through MM cells to inhibit MM cell proliferation and IL-6 secretion, indicating that VX-745 can inhibit paracrine MM cell growth and overcome cell adhesion-related drug resistance. |
| in vivo study | VX-745 effective treatment of adjuvant arthritis in mice, ED50 is 5 mg/kg. VX-745 acts on adjuvant arthritis mice, inhibiting bone reabsorption by 93% and inflammation by 56%. VX-745 acts on cartilage-induced arthritis, showing a reduced dose response. 2.5, 5, and 10 mg/kgVX-745 act on the rat model of collagen II-induced arthritis, increasing the inflammatory effect by 27%, 31%, and 44%, respectively, compared with the control group. In addition, the VX-745 protects 32-39% bones and cartilage. VX-745 is effective in treating adjuvant arthritis in mice with ED50 of 5 mg/kg. VX-745 acts on adjuvant arthritis mice, inhibiting bone reabsorption by 93% and inflammation by 56%. VX-745 acts on cartilage-induced arthritis, showing a reduced dose response. 2.5, 5, and 10 mg/kgVX-745 act on the rat model of collagen II-induced arthritis, increasing the inflammatory effect by 27%, 31%, and 44%, respectively, compared with the control group. In addition, the VX-745 protects 32-39% bones and cartilage. |
| features | VX-745 are effective, selective p38α and p38β MAPK inhibitors. |
| target | TargetValue p38α 10 nM p38β 220 nM |
| Target | Value |
| p38α | 10 nM |
| p38β | 220 nM |
Last Update：2024-04-09 21:04:16
Supplier List
Product Name: VX-745 Visit Supplier Webpage Request for quotation
CAS: 209410-46-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 209410-46-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Product Name: VX-745 Visit Supplier Webpage Request for quotation
CAS: 209410-46-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 209410-46-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History