Cat. No.: HY-163081

PARP7-IN-17

Name: PARP7-IN-17
Brand: MedChemExpress
SKU: HY-163081
Price: 200.00 USD
Availability: InStock
Rating: 5 (1 reviews)

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PARP7-IN-17 is an orally active, selective PARP7 inhibitor with an IC₅₀ of 4.5 nM. PARP7-IN-17 restores type I interferon signaling and induces IFN-beta and CXCL10 expression. PARP7-IN-17 promotes TBK1 and STAT1 phosphorylation. PARP7-IN-17 can be used for research on colon cancer.

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

Purity : 99.81%
CAS No.: 3024030-10-9
Formula: C₂₀H₂₀F₃N₇O₂
Molecular Weight:447.41

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

PARP7-IN-17 Chemical Structure

CAS No.: 3024030-10-9

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

PARP7

4.5 nM (IC₅₀)

STAT1

All PARP Isoforms :

All CXCR Isoforms :

All STAT Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CT26	IC50	16.17 μM	Cytotoxicity against mouse CT26 colorectal cancer cells assessed as viability reduction incubated 6 days by MTT assay. Cytotoxicity against mouse CT26 colorectal cancer cells assessed as viability reduction incubated 6 days by MTT assay.	38059836
CT26	IC50	36.07 μM	Cytotoxicity against mouse CT26 colorectal cancer cells assessed as viability reduction incubated 6 days by CellTiter-Glo assay. Cytotoxicity against mouse CT26 colorectal cancer cells assessed as viability reduction incubated 6 days by CellTiter-Glo assay.	38059836
AML12	IC50	50 μM	Cytotoxicity against normal mouse AML12 hepatocytes assessed as viability reduction incubated 6 days by MTT assay with IC50 greater than 50 μM. Cytotoxicity against normal mouse AML12 hepatocytes assessed as viability reduction incubated 6 days by MTT assay with IC50 greater than 50 μM.	38059836

In Vitro

Anti-cancerCytokines & ChemokinesInnate ImmunityOthers

Anti-cancer

PARP7-IN-17 (6 days) in CT26 and AML12 cells shows weak cytotoxicity, with CT26 MTT IC₅₀ 16.17 μM, CT26 CTG IC₅₀ 36.07 μM, and AML12 MTT IC₅₀ >50 μM^[1].

Anti-cancer

Cytokines & Chemokines

PARP7-IN-17 (0.04-0.44 μM; 2-day exposure) in CT26 cells increases IFN-β and CXCL10 mRNA expression dose-dependently^[1].

Anti-cancer

Innate Immunity

PARP7-IN-17 (4.00 μM alone; 0.14-4.00 μM with DMXAA 20 μg/mL; 3-day exposure) in CT26 cells promotes TBK1 and STAT1 phosphorylation^[1].

Others

PARP7-IN-17 (Compound (S)-XY-05) (1 h reaction; 20 min antibody incubation) in cell-free ARTD assays is a potent PARP7 inhibitor (IC₅₀ 4.5 nM) and shows weaker activity against PARP1, PARP2, TNKS1, TNKS2, PARP10, PARP11, PARP12, and PARP14^[1].
PARP7-IN-17 (1 μM) in a 371-kinase panel shows no obvious inhibitory activity at 1 μM^[1].
PARP7-IN-17 in Caco-2 monolayers has high permeability and low efflux (efflux ratio 0.80)^[1].
PARP7-IN-17 in CYP inhibition assays does not substantially inhibit CYP2C9, CYP2D6, or CYP3A4/5 (IC₅₀ >30 μM)^[1].
PARP7-IN-17 in cross-species liver hepatocytes is metabolically stable^[1].

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

Real Time qPCR^[1]

Cell Line:

CT26 cells
Concentration:

0.04, 0.14, 0.44 μM
Incubation Time:

2 days (exposure)
Result:

Increased IFN-β and CXCL10 mRNA expression relative to β-actin in a dose-dependent manner compared with blank control.

Western Blot Analysis^[1]

Cell Line:

CT26 cells
Concentration:

4.00 μM (alone); 0.14, 0.42, 1.30, 4.00 μM (with DMXAA 20 μg/mL)
Incubation Time:

3 days (exposure)
Result:

Promoted TBK1 phosphorylation and increased STAT1 phosphorylation in a concentration-dependent manner; total TBK1, total STAT1, and β-actin were also probed.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	C₀	AUC_inf	V_z	Clearance (CL)	MRT_0-inf	AUC_0-∞	MRT_0-∞	F
Mice^[1]	1 mg/kg	i.v.	1.22 h	0.08 h	1360 ng/mL	1593 ng/mL	1797 ng·h/mL	978 mL/kg	577 mL/h/kg	1.52 h	/	/	/
Mice^[1]	10 mg/kg	i.g.	1.76 h	0.50 h	7347 ng/mL	/	/	/	/	/	16999 ng·h/mL	2.52 h	94.6 %

In Vivo

Anti-cancerAdaptive ImmunityCytokines & Chemokines

Anti-cancer

Adaptive Immunity

PARP7-IN-17 (25 mg/kg; i.g.; twice daily; 14 days) does not inhibit CT26 tumor growth in immunodeficient nude mice, indicating that its antitumor efficacy depends on host T cells^[1].

Anti-cancer

Cytokines & Chemokines

Adaptive Immunity

PARP7-IN-17 (6.25-25 mg/kg; i.g.; twice daily; 14 days) produces dose-dependent antitumor efficacy in CT26-bearing immunocompetent mice, achieving 83% TGI at 25 mg/kg twice daily^[1].

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

Animal Model:

Balb/c (female, 6-8 weeks)^[1]
Dosage:

6.25 mg/kg; 12.5 mg/kg; 25 mg/kg
Administration:

i.g.; twice daily; 14 days
Result:

Tumor growth inhibition (TGI) values were 42%, 53%, and 83% at 6.25, 12.5, and 25 mg/kg twice daily, respectively.
Tumor IFN-β mRNA expression was dose-dependently increased, and IHC showed increased IFN-β release in tumors.
Flow cytometry of tumors showed increased percentages of CD3+CD4+ and CD3+CD8+ T cells; IHC showed increased CD8+ T-cell infiltration.

Animal Model:

Balb/c nude (female, 6-8 weeks)^[1]
Dosage:

25 mg/kg
Administration:

i.g.; twice daily; 14 days
Result:

No inhibitory effect on tumor growth was observed in CT26-bearing nude mice.

Related Protocols :

Chemical Information

CAS No. 3024030-10-9
Appearance Solid
Molecular Weight 447.41
Formula C₂₀H₂₀F₃N₇O₂
Color White to off-white
SMILES

O=C(C1=CC=CC2=CN(N=C21)[C@@H](C)C(N3CCN(CC3)C4=NC=C(C=N4)C(F)(F)F)=O)N
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (111.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2351 mL

11.1754 mL

22.3509 mL

5 mM

0.4470 mL

2.2351 mL

4.4702 mL

10 mM

0.2235 mL

1.1175 mL

2.2351 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Hongfeng Gu, et al. Discovery of Highly Selective PARP7 Inhibitors with a Novel Scaffold for Cancer Immunotherapy. J Med Chem. 2023 Dec 7. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2351 mL	11.1754 mL	22.3509 mL	55.8772 mL
	5 mM	0.4470 mL	2.2351 mL	4.4702 mL	11.1754 mL
	10 mM	0.2235 mL	1.1175 mL	2.2351 mL	5.5877 mL
	15 mM	0.1490 mL	0.7450 mL	1.4901 mL	3.7251 mL
	20 mM	0.1118 mL	0.5588 mL	1.1175 mL	2.7939 mL
	25 mM	0.0894 mL	0.4470 mL	0.8940 mL	2.2351 mL
	30 mM	0.0745 mL	0.3725 mL	0.7450 mL	1.8626 mL
	40 mM	0.0559 mL	0.2794 mL	0.5588 mL	1.3969 mL
	50 mM	0.0447 mL	0.2235 mL	0.4470 mL	1.1175 mL
	60 mM	0.0373 mL	0.1863 mL	0.3725 mL	0.9313 mL
	80 mM	0.0279 mL	0.1397 mL	0.2794 mL	0.6985 mL
	100 mM	0.0224 mL	0.1118 mL	0.2235 mL	0.5588 mL

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PARP7-IN-17

All PARP Isoforms

All CXCR Isoforms

All STAT Isoforms