2. Cell Cycle/DNA Damage Epigenetics
  3. PARP
  4. PARP7-IN-18

PARP7-IN-18 is a potent, highly selective, and orally active PARP7 inhibitor with an IC50 of 0.11 nM. PARP7-IN-18 exhibits >1000-fold selectivity over other PARP family members. PARP7-IN-18 inhibits NCI-H1373 lung cancer cell proliferation with an IC50 of 2.5 nM and promotes IFN-β expression. PARP7-IN-18 exhibits favorable pharmacokinetic properties and can be used in research on PARP7-sensitive tumors, such as lung cancer.

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

PARP7-IN-18

PARP7-IN-18 Chemical Structure

CAS No. : 2819999-00-1

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

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

PARP7-IN-18 Related Antibodies

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

PARP7-IN-18 is a potent, highly selective, and orally active PARP7 inhibitor with an IC50 of 0.11 nM. PARP7-IN-18 exhibits >1000-fold selectivity over other PARP family members. PARP7-IN-18 inhibits NCI-H1373 lung cancer cell proliferation with an IC50 of 2.5 nM and promotes IFN-β expression. PARP7-IN-18 exhibits favorable pharmacokinetic properties and can be used in research on PARP7-sensitive tumors, such as lung cancer[1].

IC50 & Target[1]

PARP7

0.11 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
NCI-H1373 IC50
2.5 nM
Compound: 8
Antiproliferative activity against human NCI-H1373 cells incubated for 4 days by luminescence cell viability assay
Antiproliferative activity against human NCI-H1373 cells incubated for 4 days by luminescence cell viability assay
[PMID: 38277917]
RAW264.7 EC50
46 nM
Compound: 8
Upregulation of IFN-beta expression in mouse RAW264.7 cells incubated for 1 day by ELISA
Upregulation of IFN-beta expression in mouse RAW264.7 cells incubated for 1 day by ELISA
[PMID: 38277917]
In Vitro

PARP7-IN-18 (compound 8) inhibits PARP7 with an IC50 of 0.11 nM and shows high selectivity over PARP1, PARP2, PARP11, PARP12 and PARP14 (IC50 > 1000 nM)[1].
PARP7-IN-18 (0.64 nM-10 μM; 4 days) inhibits NCI-H1373 lung cancer cell proliferation, with an IC50 of 2.5 nM[1].
PARP7-IN-18 (0.64 nM-10 μM; 24 h) promotes IFN-β expression in RAW264.7 macrophages, with an EC50 of 46 nM[1].
PARP7-IN-18 shows moderate inhibitory activity against CYP2C9 with an IC50 of 1.2 μM, while only weakly inhibits CYP1A2, CYP2C19, CYP2D6 and CYP3A4[1].
PARP7-IN-18 inhibits hERG potassium channel with an IC50 of 6.8 μM, revealing potential chronic cardiac toxicity risk[1].

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

PARP7-IN-18 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: NCI-H1373
Concentration: 0.64 nM-10 µM
Incubation Time: 4 days
Result: Inhibited NCI-H1373 lung cancer cell proliferation with an IC50 value of 2.5 nM.

ELISA Assay[1]

Cell Line: RAW264.7 macrophages
Concentration: 0.64 nM-10 µM
Incubation Time: 24 h
Result: Promoted IFN-β expression with an EC50 value of 46 nM.
Parmacokinetics
Species Dose Route Tmax T1/2 AUC F Cmax CL Vss
Dog[1] 10 mg/kg p.o. 0.4 h 6.6 h 4.41 μg·h/mL 78 % 3490 μg/mL / /
Dog[1] 2 mg/kg i.v. / 0.6 h 1.14 μg·h/mL / / 29.5 mL/min/kg 1050 mL/kg
Mice[1] 10 mg/kg p.o. 0.3 h 1.9 h 3.43 μg·h/mL 104 % 1.73 μg/mL / /
Mice[1] 2 mg/kg i.v. / 0.4 h 0.66 μg·h/mL / / 51.4 mL/min/kg 681 mL/kg
Rat[1] 10 mg/kg p.o. 0.4 h 0.7 h 1.04 μg·h/mL 30 % 725 μg/mL / /
Rat[1] 2 mg/kg i.v. / 0.7 h 0.68 μg·h/mL / / 49.2 mL/min/kg 1770 mL/kg
In Vivo

PARP7-IN-18 (compound 8) (30 mg/kg; p.o.; once daily; for 21 days) has antitumor activity in NCI-H1373 tumor-bearing CB17 SCID nude mouse model[1].

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

Animal Model: Female CB17 SCID nude mice subcutaneously inoculated with 0.1 mL of NCI-H1373 cells into the right back[1]
Dosage: 30 mg/kg
Administration: Oral gavage (p.o.); once daily; for 21 days
Result: Suppressed NCI-H1373 xenograft tumor growth.
Achieved tumor growth inhibition (TGI) of 81.6%.
Reduced tumor volume and dissected tumor weight compared with the vehicle group.
Molecular Weight

542.94

Formula

C23H26ClF3N6O4
CAS No.
SMILES

O=C1NN=CC(N2CC[C@H]2COCCC(N3C[C@H]4N(C5=C(OCC4)C=C(Cl)C=N5)CC3)=O)=C1C(F)(F)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

PARP7-IN-18 Related Classifications

  • 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
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:

PARP7-IN-182819999-00-1PARPpoly ADP ribose polymerasePARP7 inhibitorselective PARP7 inhibitororally bioavailablePARP1PARP2PARP11PARP12PARP14NCI-H1373RAW264.7IFN-βtype I IFN signalingcGAS-STING pathwayRBN-2397lung cancerNCI-H1373 xenograft modelInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PARP7-IN-18
Cat. No.:
HY-162172
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

SAFETY DATA SHEET (SDS)

Request for HNMR Report

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