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

Mefuparib hydrochloride  (Synonyms: MPH)

Cat. No.: HY-122661 Purity: 98.94%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

Mefuparib hydrochloride Chemical Structure

Mefuparib hydrochloride Chemical Structure

CAS No. : 1449746-00-2

Size Price Stock Quantity
5 mg USD 200 In-stock
10 mg USD 350 In-stock
25 mg USD 700 In-stock
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

View All PARP Isoform Specific Products:

View All Isoforms
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

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

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].

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

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.
Clinical Trial
Molecular Weight

334.77

Appearance

Solid

Formula

C17H16ClFN2O2
CAS No.
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

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (74.68 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9871 mL 14.9356 mL 29.8713 mL
5 mM 0.5974 mL 2.9871 mL 5.9743 mL
10 mM 0.2987 mL 1.4936 mL 2.9871 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.47 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.47 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.47 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
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.

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

Mefuparib1449746-00-2MPHPARPApoptosispoly ADP ribose polymerase orallysubstrate-competitiveprominentanticancerInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Mefuparib hydrochloride
Cat. No.:
HY-122661
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email address *

Phone number

 

Department *

Organization name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.