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 Chemical Structure

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)

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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Storage

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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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