1. Cell Cycle/DNA Damage
    Epigenetics
    Apoptosis
  2. PARP
    Apoptosis
  3. Mefuparib hydrochloride

Mefuparib hydrochloride (Synonyms: MPH)

Cat. No.: HY-122661
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Mefuparib hydrochloride (MPH) is an orally active, substrate-competitive and selective PARP1/2 inhibitor with IC50s of 3.2 nM and 1.9 nM, respectively. Mefuparib hydrochloride induces apoptosis and possesses prominent anticancer activity in vitro and in vivo.

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Mefuparib hydrochloride Chemical Structure

Mefuparib hydrochloride Chemical Structure

CAS No. : 1449746-00-2

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Description

Mefuparib hydrochloride (MPH) is an orally active, substrate-competitive and selective PARP1/2 inhibitor with IC50s of 3.2 nM and 1.9 nM, respectively. Mefuparib hydrochloride induces apoptosis and possesses prominent anticancer activity in vitro and in vivo[1][2].

IC50 & Target[1]

PARP1

3.2 nM (IC50)

PARP2

1.9 nM (IC50)

TNKS1

1.6 μM (IC50)

TNKS2

1.3 μM (IC50)

In Vitro

Mefuparib hydrochloride (1-10 μM; 48 hours) causes cell apoptosis[1].
Mefuparib hydrochloride (MPH; 1-10 μM; 24 hours) causes V-C8 cells into typical G2/M arrest[1].
Mefuparib hydrochloride (1-10 μM; 24 hours) causes the accumulation of DSB marked by the increased levels of γH2AX in the MDA-MB-436 (BRCA1−/−) cells in a concentration-dependent manner[1].
Mefuparib hydrochloride exerts potent in vitro proliferation-inhibitory effects on cancer cells derived from different human tissues with an average IC50 of 2.16 μM (0.12 μM~3.64 μM)[1].
Mefuparib hydrochloride inhibits PARP3 (IC50>10 μM), PARP6 (IC50>10 μM), TNKS1 (IC50=1.6 μM), TNKS2 (IC50=1.3 μM)[1].

Apoptosis Analysis[1]

Cell Line: V-C8 cells
Concentration: 1, 3, 10 μM
Incubation Time: 48 hours
Result: Caused cell apoptosis.

Cell Cycle Analysis[1]

Cell Line: V-C8 cells
Concentration: 1, 3, 10 μM
Incubation Time: 24 hours
Result: Cell came into typical G2/M arrest.

Western Blot Analysis[1]

Cell Line: MDA-MB-436 (BRCA1−/−) cells
Concentration: 1, 10 μM
Incubation Time: 24 hours
Result: Caused the accumulation of DSB marked by the increased levels of γH2AX in the MDA-MB-436 (BRCA1−/−) cells in a concentration-dependent manner.
In Vivo

Mefuparib hydrochloride (MPH; 40-160 mg/kg; orally; once every other day; for 21 days) displays dose- and time-dependent killing on V-C8 xenografts accompanied by complete disappearance of some xenografts, especially in the high-dose group[1].
Mefuparib hydrochloride (160 mg/kg; orally; once every other day; for 21 days) inhibits the growth of the BR-05-0028 breast patient-derived xenograft (PDX) without obvious loss of body weight[1].
Mefuparib hydrochloride (10, 20, 40 mg/kg; oral) has a T1/2 of 1.07-1.3 hours and a C max of 116-725 ng/mL for SD rats[1].
Mefuparib hydrochloride (5, 10, 20 mg/kg; oral) has a T1/2 of 2.16-2.7 hours and a C max of 114-608 ng/mL for cynomolgus monkeys[1].

Animal Model: Nude mice with V-C8 xenografts[1]
Dosage: 40, 80, 160 mg/kg
Administration: Orally; once every other day; for 21 days
Result: Displayed dose- and time-dependent killing on V-C8 xenografts accompanied by complete disappearance of some xenografts, especially in the high-dose group.
Animal Model: SD rats[1]
Dosage: 10, 20, 40 mg/kg (Pharmacokinetic Analysis)
Administration: Oral
Result: Had a T1/2 of 1.07-1.3 hours and a C max of 116-725 ng/mL.
Molecular Weight

334.77

Formula

C₁₇H₁₆ClFN₂O₂

CAS No.

1449746-00-2

SMILES

O=C(C1=C(OC(C2=CC=C(CNC)C=C2)=C3)C3=CC(F)=C1)N.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

MefuparibMPHPARPApoptosispoly ADP ribose polymerase orallysubstrate-competitiveprominentanticancerInhibitorinhibitorinhibit

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