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Chemical Structure| 1221713-92-3 Chemical Structure| 1221713-92-3

Structure of NPS-1034
CAS No.: 1221713-92-3

Chemical Structure| 1221713-92-3

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NPS-1034 is a dual Met/Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively.

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Product Details of NPS-1034

CAS No. :1221713-92-3
Formula : C31H23F2N5O3
M.W : 551.54
SMILES Code : O=C(C1=C(C)N(C)N(C2=CC=C(F)C=C2)C1=O)NC3=CC=C(OC4=C5C(NC=C5C6=CC=CC=C6)=NC=C4)C(F)=C3
MDL No. :MFCD29905447
InChI Key :RGAZVGZUBCFHRJ-UHFFFAOYSA-N
Pubchem ID :46194178

Safety of NPS-1034

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of NPS-1034

RTK

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
MIA PaCa-2 cells 0, 10, 20, 40, 80, 160 µM 1 day NPS-1034 dose-dependently reduces the viability and clonogenicity of PDAC cells PMC11241054
BxPC-3 cells 0, 10, 20, 40, 80, 160 µM 1 day NPS-1034 dose-dependently reduces the viability and clonogenicity of PDAC cells PMC11241054
Caki-1 0, 10, 20, 40, 80, 160 µM 24 hours To evaluate the cytotoxic effects of NPS-1034 on RCC cell lines, showing significant reduction in cell viability PMC11506434
786-0 0, 10, 20, 40, 80, 160 µM 24 hours To evaluate the cytotoxic effects of NPS-1034 on RCC cell lines, showing significant reduction in cell viability PMC11506434
A498 0, 10, 20, 40, 80, 160 µM 24 hours To evaluate the cytotoxic effects of NPS-1034 on RCC cell lines, showing significant reduction in cell viability PMC11506434
NTERA2 cells 10, 20, 40, 80, 160 µM 24 hours To evaluate the effect of NPS-1034 on NTERA2 cell viability, results showed that NPS-1034 reduced cell viability in a dose-dependent manner. PMC8952763
NCCIT cells 10, 20, 40, 80, 160 µM 24 hours To evaluate the effect of NPS-1034 on NCCIT cell viability, results showed that NPS-1034 reduced cell viability in a dose-dependent manner. PMC8952763
MIA PaCa-2 cells 0, 20, 80 µM 48 hours NPS-1034 induces apoptosis in PDAC cells PMC11241054
BxPC-3 cells 0, 20, 80 µM 48 hours NPS-1034 induces apoptosis in PDAC cells PMC11241054
HCC4011 1 μM 72 hours To evaluate the effect of NPS1034 in combination with osimertinib on the sensitivity of high-AXL-expressing EGFR-mutated NSCLC cells, results showed that the combination significantly reduced the viability of HCC4011 cells. PMC6335418
PC-9GXR 1 μM 72 hours To evaluate the effect of NPS1034 in combination with osimertinib on the sensitivity of high-AXL-expressing EGFR-mutated NSCLC cells, results showed that the combination significantly reduced the viability of PC-9GXR cells. PMC6335418
PC-9 1 μM 72 hours To evaluate the effect of NPS1034 in combination with osimertinib on the sensitivity of high-AXL-expressing EGFR-mutated NSCLC cells, results showed that the combination significantly reduced the viability of PC-9 cells. PMC6335418

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c mice Renca-luc lung metastasis model Oral 10 or 30 mg/kg Once daily for 5 weeks To evaluate the inhibitory effects of NPS-1034 on RCC tumor growth in vivo, showing significant alleviation of tumor burden PMC11506434
Nude mice PC-9 cell-line-derived xenograft (CDX) model Oral gavage 50 mg/kg NPS1034 and 5 mg/kg osimertinib 5 days a week for 10 weeks To evaluate the effect of NPS1034 in combination with osimertinib on high-AXL-expressing EGFR-mutated NSCLC tumors, results showed that the combination significantly inhibited tumor re-growth. PMC6335418

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.81mL

0.36mL

0.18mL

9.07mL

1.81mL

0.91mL

18.13mL

3.63mL

1.81mL

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