1. Cell Cycle/DNA Damage Epigenetics
  2. PARP
  3. PARP7-IN-22

PARP7-IN-22 (XLY-1) is a PARP7 inhibitor with an IC50 of 0.6 nM. PARP7-IN-22 (XLY-1) is orally active, enhances type I interferon signaling in vitro, restores type I interferon signaling, promotes T cell infiltration into tumor tissues, and significantly inhibits tumor growth. PARP7-IN-22 shows promise for research in the field of cancer immunotherapy.

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PARP7-IN-22 Chemical Structure

PARP7-IN-22 Chemical Structure

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Description

PARP7-IN-22 (XLY-1) is a PARP7 inhibitor with an IC50 of 0.6 nM. PARP7-IN-22 (XLY-1) is orally active, enhances type I interferon signaling in vitro, restores type I interferon signaling, promotes T cell infiltration into tumor tissues, and significantly inhibits tumor growth. PARP7-IN-22 shows promise for research in the field of cancer immunotherapy[1].

IC50 & Target[1]

PARP-7

0.6 nM (IC50)

In Vitro

PARP7-IN-22 (XLY-1) (5μM-20μM, 14 days) demonstrates no substantial influence on the activity of CT26 cells[1].
PARP7-IN-22 (49 nM-4000 nM, 72 h) significantly enhances the expression of IFN-β and CXCL10, as well as the phosphorylation of STAT1, in a dose-dependent manner [1].
PARP7-IN-22 (49 nM-4000 nM, 72 h) administration exhibites a noticeable increase in TBK1 phosphorylation[1].
PARP7-IN-22 (49 nM-4000 nM, 72 h) effectively promotes the type I interferon signaling cascade, thereby exerting anti-tumor effects[1].

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

RT-PCR[1]

Cell Line: CT26 cells
Concentration: 49 nM-4000 nM
Incubation Time: 72 h
Result: Resulted in a gradual increase in the mRNA levels of IFN-β and CXCL10 as the dose ranged from 49 nM to 4000 nM.

Western Blot Analysis[1]

Cell Line: CT26 cells
Concentration: 49 nM-4000 nM
Incubation Time: 72 h
Result: Resulted in a dose-dependent increase in the protein levels of STAT1 and TBK1, with STAT1 protein levels showing a dose-dependent increase in the range of 49 nM to 4000 nM.
In Vivo

PARP7-IN-22 (XLY-1) (Male rats, 5 mg/kg, i.v.; 30 mg/kg, p.o; 0.5-24 h) can be administered orally for further in vivo pharmacodynamic studies[1].
PARP7-IN-22 (CT26 syngeneic model, 25 or 50 mg/kg, p.o., 14 days) demonstrates excellent anti-tumor proliferative effects in the CT26 syngeneic model [1].
PARP7-IN-22 (CT26 syngeneic model, 50 mg/kg, p.o., 14 days) promotes T cell infiltration into tumor tissues and exhibits targeted effects[1].
1.19
Pharmacokinetic Analysis in CT26 Syngeneic Model[1]

药代动力学分析[1]

PARP7-IN-22 (XLY-1) T1/2 (h) Tmax (h) Cmax(g/mL) C0(g/mL) AUC0-∞ (h⋅ng/mL) Vz (L/kg) CL (L/h/kg) MRT0-∞(h) F (%)
i.v. (5 mg/kg) 5.42 1.25 353.80 1632.80 1626.00 0.029 0.004 3.22 -
p.o. (30 mg/kg) 5.52 1.75 674.00 - 2368.10 0.112 0.014 4.84 24.27

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

Molecular Weight

508.42

Formula

C19H22F6N8O2

SMILES

O=C1NN=CC(NCCCCNC(N2CCN(CC2)C3=NC=C(C=N3)C(F)(F)F)=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
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PARP7-IN-22 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.

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PARP7-IN-22
Cat. No.:
HY-163719
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