2. Cell Cycle/DNA Damage Epigenetics Protein Tyrosine Kinase/RTK Apoptosis
  3. PARP c-Met/HGFR Apoptosis
  4. PARP1/c-Met-IN-1

PARP1/c-Met-IN-1 (Compound 16) is a selective dual inhibitor for PARP1 and c-Met, with IC50s of 3.3 and 32.2 nM, respectively. PARP1/c-Met-IN-1 induces cell apoptosis and cell cycle arrest in G2/M phase in MDA-MB-231 cells. PARP1/c-Met-IN-1 exhibits antitumor activity in mice.

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PARP1/c-Met-IN-1

PARP1/c-Met-IN-1 Chemical Structure

CAS No. : 2944101-99-7

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PARP1/c-Met-IN-1 Related Antibodies

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Description

PARP1/c-Met-IN-1 (Compound 16) is a selective dual inhibitor for PARP1 and c-Met, with IC50s of 3.3 and 32.2 nM, respectively. PARP1/c-Met-IN-1 induces cell apoptosis and cell cycle arrest in G2/M phase in MDA-MB-231 cells. PARP1/c-Met-IN-1 exhibits antitumor activity in mice[1].

IC50 & Target

PARP1

3.3 nM (IC50)

c-Met

32.2 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
MDA-MB-231 IC50
0.045 μM
Compound: 16
Antiproliferative activity against human MDA-MB-231 cells harboring wild type BRCA and c-Met amplification assessed as inhibition of cell growth incubated for 7 days by MTT assay
Antiproliferative activity against human MDA-MB-231 cells harboring wild type BRCA and c-Met amplification assessed as inhibition of cell growth incubated for 7 days by MTT assay
[PMID: 38477575]
MDA-MB-468 IC50
0.17 μM
Compound: 16
Antiproliferative activity against human MDA-MB-468 cells harboring wild type BRCA1/2, HR-proficient and non-c-Met amplification assessed as inhibition of cell growth incubated for 7 days by MTT assay
Antiproliferative activity against human MDA-MB-468 cells harboring wild type BRCA1/2, HR-proficient and non-c-Met amplification assessed as inhibition of cell growth incubated for 7 days by MTT assay
[PMID: 38477575]
NRK IC50
8.73 μM
Compound: 16
Cytotoxicity against NRK cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Cytotoxicity against NRK cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 38477575]
In Vitro

PARP1/c-Met-IN-1 (1 μM) improves the thermal stability of PARP1 and c-Met[1].
PARP1/c-Met-IN-1 (1 μM) inhibits the expressions of PARP1 and c-Met related proteins PAR, p-c-Met and p-AKT, affects the interactions of PARP1/c-Met, causes DNA damage[1].
PARP1/c-Met-IN-1 (0.5-1 μM) diminishes the homologous recombination (HR) function in MDA-MB-231 cells through downregulating expressions of BRCA1 and Rad51[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PARP1/c-Met-IN-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: MDA-MB-231
Concentration: 1 μM
Incubation Time: 72 h
Result: Enhanced the thermostability of these proteins within the temperature range of 43–55 °C.
Decreased expressions of BRCA1 and Rad51.
In Vivo

PARP1/c-Met-IN-1 (12.5-100 mg/kg, i.p. for 28 days) exhibits antitumor efficacy with tumor growth inhibition (TGI) values of 49-77 % and 62-70 % in MDA-MB-231 and HCT116OR xenograft nude mice, respectively[1].

Pharmacokinetic Analysis of PARP1/c-Met-IN-1 in BALB/c mice[1]

route Dose (mg/kg) T1/2 (h) Tmax (h) Cmax (ng/mL) AUC0-t (ng·h/mL) AUC0-inf (ng·h/mL) MRT0-t (h) MRT0-inf (h) CLblood (mL/h/kg)
i.p. 10 1.42 0.25 152.47 95.42 96.70 1.67 1.77 121232

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: MDA-MB-231 and HCT116OR xenograft BALB/c nude mice[1]
Dosage: 12.5-50 mg/kg for MDA-MB-231 xenograft mice, 20-100 mg/kg for HCT116OR xenograft mice
Administration: I.p., 21 days for HCT116OR xenograft mice, 28 days for MDA-MB-231 xenograft mice
Result: Inhibited tumor growth with TGI of 49-77% in MDA-MB-231 xenograft mice.
Inhibited tumor growth with TGI of 62-70% in HCT116OR xenograft mice.
Molecular Weight

708.74

Formula

C40H33FN8O4
CAS No.
SMILES

O=C1C=CC(C2=CC=CN=C2)=NN1CCOC3=C4C(C=C(C=C4)N5CCN(CC5)C(C6=C(C=CC(CC7=NNC(C8=C7C=CC=C8)=O)=C6)F)=O)=NC=C3
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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PARP1/c-Met-IN-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PARP1/c-Met-IN-12944101-99-7PARPc-Met/HGFRApoptosispoly ADP ribose polymerase MDA-MB-231HCT116ORBALB/c miceInhibitorinhibitorinhibit

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