1. Cell Cycle/DNA Damage Apoptosis
  2. Wee1 Apoptosis
  3. WEE1-IN-7

WEE1-IN-7 (compound 12h) is a potent and orally activeWEE1 inhibitor with an IC50 value of 2.1 nM. WEE1-IN-7 induces apoptosis and cell cycle arrest at the S phase. WEE1-IN-7 shows antitumor activity.

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WEE1-IN-7 Chemical Structure

WEE1-IN-7 Chemical Structure

CAS No. : 2924006-98-2

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Description

WEE1-IN-7 (compound 12h) is a potent and orally activeWEE1 inhibitor with an IC50 value of 2.1 nM. WEE1-IN-7 induces apoptosis and cell cycle arrest at the S phase. WEE1-IN-7 shows antitumor activity[1].

IC50 & Target

IC50: 2.1 nM (WEE1)[1]

In Vitro

WEE1-IN-7 (compound 12h) inhibits cell viability with IC50 values of 84, 82 nM for A427, Lovo cells, respectively[1].
WEE1-IN-7 (0-800 nM; 48 h) induces apoptosis and cell cycle arrest at S phase in a dose-dependent manner[1].

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

Apoptosis Analysis[1]

Cell Line: A427 cells
Concentration: 200, 400, 800 nM
Incubation Time: 48 h
Result: Significantly increased the percentage of both early and late apoptotic cells in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: A427 cells
Concentration: 0, 50, 100, 200, 400 nM
Incubation Time: 48 h
Result: Induced cell cycle arrest at the S phase with the the percentage of cells in the S phase of 37.4%, 46.7%, 48.5%, 59.1%, and 59.1% at 0, 50, 100, 200, and 400 nM, respectively.
In Vivo

WEE1-IN-7 (60 mg/kg; p.o.; daily for 27 days) shows antitumor activity with the tumor growth inhibition (TGI) of 88% in Lovo CDX xenograft mice model[1].
Pharmacokinetic Parameters[1].

Admin. AUC (h·ng/mL) T1/2 (h) Vd (L/kg) CL (L/h/kg) Cmax F (%)
intravenous (1 mg/kg) 118 1.06 11.3 8.20 - -
intragastric (60 mg/kg) 4342 5.94 - - 498 61.64

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

Animal Model: Female C57 mice (Lovo CDX xenograft mice model)[1]
Dosage: 60 mg/kg
Administration: P.o.; daily for 27 days
Result: Showed antitumor activity with the tumor growth inhibition (TGI) of 88%.
Molecular Weight

520.59

Formula

C28H28N10O

CAS No.
SMILES

O=C1C2=CN=C(NC3=CC=C(N4CCN(CC4)C)C=C3)N=C2N(N1CC=C)C5=CC=CC(C6=NC=CN=C6)=N5

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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WEE1-IN-7 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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Product Name:
WEE1-IN-7
Cat. No.:
HY-163697
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