1221713-92-3
N-(3-fluoro-4-((3-phenyl-1H-pyrrolo[2,3-b]pyridin-4-yl)oxy)phenyl)-2-(4-fluorophenyl)-1,5-dimethyl-3-oxo-2,3-dihydro-1H-pyrazole-4-carboxamide.
CAS: 1221713-92-3
Molecular Formula: C31H23F2N5O3
1221713-92-3 - Names and Identifiers
1221713-92-3 - Physico-chemical Properties
| Molecular Formula | C31H23F2N5O3 |
| Molar Mass | 551.54 |
| Density | 1.416±0.06 g/cm3(Predicted) |
| Solubility | Soluble in DMSO, not in water |
| pKa | 11.05±0.70(Predicted) |
| Storage Condition | -20℃ |
| Use | NPS-1034 is a novel MET inhibitor, which inhibits the activated MET receptor and its constitutively active mutants. NPS-1034, inhibits various constitutively active mutant forms of MET as well as HGF-activated wild-type MET. NPS-1034 inhibited the proliferation of cells expressing activated MET and promoted the regression of tumors formed from such cells in a mouse xenograft model through anti-angiogenic and pro-apoptotic actions. NPS-1034 also inhibited HGF-stimulated activation of MET signaling in the presence or absence of serum. Notably, NPS-1034 inhibited three MET variants that are resistant to the MET inhibitors SU11274, NVP-BVU972, and PHA665752. |
| In vitro study | In HCC827/GR cells, NPS-1034 did not exhibit a significant anti-proliferative effect and was able to overcome gefitinib resistance by inhibiting phosphorylation of MET,Akt, and Erk. In H820 cells, NPS-1034 increased sensitivity to EGFR-TKIs. In HCC78 cells, ROS1 activity and cell proliferation were inhibited by NPS-1034. In addition, binding of gefitinib and NPS-1034 enhanced cell death by inducing caspase-3 and PARP-1 lysis. NPS-1034 inhibited the activity of MKN45 and SNU638 cell lines highly expressing MET gene and p-MET, with IC50 of 112.7 and 190.3 nmol, respectively. |
| In vivo study | In SCID mice loaded with HCC827/GR tumor xenografts, NPS-1034 (10 mg/kg, p.o.) reduces tumor growth, and in combination with gefitinib and NPS-1034 enhances tumor growth inhibition by inhibiting tumor proliferation and inducing apoptosis. NPS-1034 (30 mg/kg, p.o.) reduced tumor growth by inhibiting angiogenesis and promoting apoptosis in nude mice bearing MKN45 xenografts. |
1221713-92-3 - Reference
| Reference Show more | 1. Rho JK, et al. MET and AXL inhibitor NPS-1034 exerts efficacy against lung cancer cells resistant to EGFR kinase inhibitors because of MET or AXL activation. Cancer Res. 2014 Jan 1;74(1):253-62.2. Shin JS, et al. NPS-1034, a novel MET inhibitor, inhibits the activated MET receptor and its constitutively active mutants. Invest New Drugs. 2014 Jun;32(3):389-99. |
1221713-92-3 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.813 ml | 9.065 ml | 18.131 ml |
| 5 mM | 0.363 ml | 1.813 ml | 3.626 ml |
| 10 mM | 0.181 ml | 0.907 ml | 1.813 ml |
| 5 mM | 0.036 ml | 0.181 ml | 0.363 ml |
Last Update：2024-01-02 23:10:35
Supplier List
Spot supply
Product Name: NPS-1034 Request for quotationCAS: 1221713-92-3
Tel: 400-968-2212
Email: 3623107365@qq.com
Mobile: 18916960931
QQ: 3623107365
Wechat: 18916960931
Spot supply
Product Name: NPS-1034 Visit Supplier Webpage Request for quotationCAS: 1221713-92-3
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328
WhatsApp: +86-18821248368
Multiple SpecificationsSpot supply
Product Name: NPS-1034 (Standard) Visit Supplier Webpage Request for quotationCAS: 1221713-92-3
Tel: 609-228-6898
Email: sales@medchemexpress.com
tech@medchemexpress.com
Mobile: 609-228-6898
Spot supply
Product Name: NPS-1034 Visit Supplier Webpage Request for quotationCAS: 1221713-92-3
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922
Wechat: 18621343501
WhatsApp: +86-18621343501
Product Name: N-(3-fluoro-4-((3-phenyl-1H-pyrrolo[2,3-b]pyridin-4-yl)oxy)phenyl)-2-(4-fluorophenyl)-1,5-dimethyl-3-oxo-2,3-dihydro-1H-pyrazole-4-carboxamide. Visit Supplier Webpage Request for quotation
CAS: 1221713-92-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
CAS: 1221713-92-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Spot supply
Product Name: NPS-1034 Request for quotationCAS: 1221713-92-3
Tel: 400-968-2212
Email: 3623107365@qq.com
Mobile: 18916960931
QQ: 3623107365
Wechat: 18916960931
Spot supply
Product Name: NPS-1034 Visit Supplier Webpage Request for quotationCAS: 1221713-92-3
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328
WhatsApp: +86-18821248368
Multiple SpecificationsSpot supply
Product Name: NPS-1034 (Standard) Visit Supplier Webpage Request for quotationCAS: 1221713-92-3
Tel: 609-228-6898
Email: sales@medchemexpress.com
tech@medchemexpress.com
Mobile: 609-228-6898
Spot supply
Product Name: NPS-1034 Visit Supplier Webpage Request for quotationCAS: 1221713-92-3
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922
Wechat: 18621343501
WhatsApp: +86-18621343501
Product Name: N-(3-fluoro-4-((3-phenyl-1H-pyrrolo[2,3-b]pyridin-4-yl)oxy)phenyl)-2-(4-fluorophenyl)-1,5-dimethyl-3-oxo-2,3-dihydro-1H-pyrazole-4-carboxamide. Visit Supplier Webpage Request for quotation
CAS: 1221713-92-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
CAS: 1221713-92-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
View History
1221713-92-3
苯三羰基铬
131184-73-1
十一碳烯-9-酸
847547-91-5
3350-78-5
N-2-propen-1-ylFormamide
N-T-BOC-L-ISOLEUCINOL
897942-79-9
sulfocarbonic anhydride
苯三羰基铬
131184-73-1
十一碳烯-9-酸
847547-91-5
3350-78-5
N-2-propen-1-ylFormamide
N-T-BOC-L-ISOLEUCINOL
897942-79-9
sulfocarbonic anhydride