product name NPS-1034
Description: NPS-1034 is novel a dual Met/Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively. NPS-1034 inhibits various constitutively active mutant forms of MET and HGF-activated wild-type MET. It inhibited the proliferation of cells expressing MET and promoted the regression of tumors in a mouse xenograft via anti-angiogenic & pro-apoptotic actions.
References: Cancer Res. 2014 Jan 1;74(1):253-62; Invest New Drugs. 2014 Jun;32(3):389-99.
551.54
Formula
C31H23F2N5O3
CAS No.
1221713-92-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (181.3 mM)
Water: <1 mg/mL
Ethanol: 4 mg/mL (7.3 mM)
Solubility (In vivo)
PBS: 11mg/mL
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19402584
| In Vitro |
In vitro activity: In HCC827/GR cells, NPS-1034 does not show significant antiproliferative effects, while overcomes gefitinib resistance by inhibiting the phosphorylation of MET, Akt, and Erk. In H820 cells, NPS-1034 enhances sensitivity to EGFR-TKIs. In HCC78 cells, NPS-1034 inhibits ROS1 activity and cell proliferation. In addition, a combination of gefitinib and NPS-1034 enhances cell death by inducing caspase-3 and PARP-1 cleavage. NPS-1034 inhibits the viability of the MKN45 and SNU638 cell lines, which highly express the MET gene and p-MET, with IC50 of 112.7 and 190.3 nmol, respectively. Kinase Assay: The in vitro NPS-1034 profile of inhibition of RTKs is analyzed using RTK assay kits according to the manufacturers protocols. Cell Assay: To perform the MTT assay, cells (0.5 × 104/well, HCC827/GR, HCC-78 and H820 cells) are plated in 96-well sterile plastic plates and allowed to attach overnight. Cells are exposed to varying doses of gefitinib, erlotinib, PHA-665752, and NPS-1034 in medium containing 1% FBS. After 72 hours, 15 μL of MTT solution (5 mg/mL) is added to each well and plates are incubated for 4 hours. Crystalline formazan is solubilized with 100 μL of a 10% (w/v) SDS solution for 24 hours. Absorbance at 595 nm is read spectrophotometrically using a microplate reader. |
|---|---|
| In Vivo | In SCID mice bearing HCC827/GR tumor xenografts, NPS-1034 (10 mg/kg, p.o.) decreases tumor growth, and the combination of gefitinib and NPS-1034 results in enhanced tumor growth inhibition via the inhibition of tumor proliferation and the induction of apoptosis. In nude mice bearing MKN45 xenograft tumors, NPS-1034 (30 mg/kg, p.o.) decreases tumor growth through the inhibition of angiogenesis and the promotion of apoptosis. |
| Animal model | SCID mice bearing HCC827/GR tumor xenografts |
| Formulation & Dosage | Dissolved in PBS; 10 mg/kg; oral gavage |
| References | Cancer Res. 2014 Jan 1;74(1):253-62; Invest New Drugs. 2014 Jun;32(3):389-99. |
Related Posts
product name NPS-1034
Description: NPS-1034 is novel a dual Met/Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively. NPS-1034 inhibits various constitutively active mutant forms of MET and HGF-activated wild-type MET. It inhibited the proliferation of cells expressing MET and promoted the regression of tumors in a mouse xenograft via anti-angiogenic & pro-apoptotic actions.
References: Cancer Res. 2014 Jan 1;74(1):253-62; Invest New Drugs. 2014 Jun;32(3):389-99.
551.54
Formula
C31H23F2N5O3
CAS No.
1221713-92-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (181.3 mM)
Water: <1 mg/mL
Ethanol: 4 mg/mL (7.3 mM)
Solubility (In vivo)
PBS: 11mg/mL
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19402584
| In Vitro |
In vitro activity: In HCC827/GR cells, NPS-1034 does not show significant antiproliferative effects, while overcomes gefitinib resistance by inhibiting the phosphorylation of MET, Akt, and Erk. In H820 cells, NPS-1034 enhances sensitivity to EGFR-TKIs. In HCC78 cells, NPS-1034 inhibits ROS1 activity and cell proliferation. In addition, a combination of gefitinib and NPS-1034 enhances cell death by inducing caspase-3 and PARP-1 cleavage. NPS-1034 inhibits the viability of the MKN45 and SNU638 cell lines, which highly express the MET gene and p-MET, with IC50 of 112.7 and 190.3 nmol, respectively. Kinase Assay: The in vitro NPS-1034 profile of inhibition of RTKs is analyzed using RTK assay kits according to the manufacturers protocols. Cell Assay: To perform the MTT assay, cells (0.5 × 104/well, HCC827/GR, HCC-78 and H820 cells) are plated in 96-well sterile plastic plates and allowed to attach overnight. Cells are exposed to varying doses of gefitinib, erlotinib, PHA-665752, and NPS-1034 in medium containing 1% FBS. After 72 hours, 15 μL of MTT solution (5 mg/mL) is added to each well and plates are incubated for 4 hours. Crystalline formazan is solubilized with 100 μL of a 10% (w/v) SDS solution for 24 hours. Absorbance at 595 nm is read spectrophotometrically using a microplate reader. |
|---|---|
| In Vivo | In SCID mice bearing HCC827/GR tumor xenografts, NPS-1034 (10 mg/kg, p.o.) decreases tumor growth, and the combination of gefitinib and NPS-1034 results in enhanced tumor growth inhibition via the inhibition of tumor proliferation and the induction of apoptosis. In nude mice bearing MKN45 xenograft tumors, NPS-1034 (30 mg/kg, p.o.) decreases tumor growth through the inhibition of angiogenesis and the promotion of apoptosis. |
| Animal model | SCID mice bearing HCC827/GR tumor xenografts |
| Formulation & Dosage | Dissolved in PBS; 10 mg/kg; oral gavage |
| References | Cancer Res. 2014 Jan 1;74(1):253-62; Invest New Drugs. 2014 Jun;32(3):389-99. |