Rac/Cdc42-IN-1
Rac/Cdc42-IN-1, the major phase I metabolite of the oral Rac/Cdc42 inhibitor MBQ-167 (HY-112842) in vivo, is a selective Rac inhibitor. Rac/Cdc42-IN-1 functions by blocking the GTP-binding activation of Rac1, targeting the autophosphorylation of Thr423/Thr402/Thr436 and Ser141/Ser144/Ser154 in downstream PAK1/2/3, with an inhibitory effect superior to that of MBQ-167. Rac/Cdc42-IN-1 significantly inhibits cell migration, and suppresses tumor growth and distant metastasis to the lung, liver and kidney in HER2+ breast cancer mouse models. Rac/Cdc42-IN-1 can be used for targeted research on metastatic breast cancer.
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- CAS No.: 2143950-05-2
- Formule: C20H14N4
- Masse moléculaire:310.35
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Stockage:
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Activité biologique
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Chemical Information
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Activité biologique
Rac/Cdc42-IN-1 (M6) (500 nM; 72 h) exerts no significant effect on the cell viability of triple-negative breast cancer cells MDA-MB-231, MDA-MB-468 and HER2-overexpressing breast cancer cells HER2-BM[1].
Rac/Cdc42-IN-1 (0.001-1000 nM; 120 h) shows no significant cytotoxicity against normal human mammary epithelial cells HMEC[1].
Rac/Cdc42-IN-1 (15-1000 nM; 72 h) exerts no significant effect on the viability of HER2-BM cells[1].
Rac/Cdc42-IN-1 (500 nM; 48 h) does not significantly induce apoptosis in MDA-MB-231, MDA-MB-468 and HER2-BM cells (no obvious change in caspase-3/7 activity)[1].
Rac/Cdc42-IN-1 (250 nM; 24 h) significantly inhibits the autophosphorylation of Group 1 PAK (PAK1/2/3) at Thr423/Thr402/Thr436 and Ser141/Ser144/Ser154 sites in HER2-BM cells, and its inhibitory effect is superior to that of the parent drug MBQ-167 (HY-112842)[1].
Rac/Cdc42-IN-1 (25 nM, 250 nM; 24 h) inhibits the migration of HER2-BM cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231, MDA-MB-468, HER2-BM
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Concentration:500 nM
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Incubation Time:48 h
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Result:Did not significantly alter caspase-3/7 activity in MDA-MB-231, MDA-MB-468 and HER2-BM cells, indicating no obvious induction of apoptosis, whereas MBQ-167 (HY-112842) significantly induced apoptosis at the same concentration.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Severe Combined Immunodeficiency (SCID) mice bearing orthotopic GFP-HER2-BM breast cancer tumors[1]
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Dosage:10 mg/kg
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Administration:i.p.; 5 times per week; for 8 consecutive weeks
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Result:Significantly inhibited tumor growth by approximately 90% compared with the vehicle-treated group.
Also prevented the development of distal metastases to the lungs, livers, and kidneys by about 90%, showing comparable antitumor and antimetastatic efficacy to the parent compound MBQ-167 (HY-112842) at the same dosage.
Chemical Information
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CAS No. 2143950-05-2
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Masse moléculaire 310.35
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Formule C20H14N4
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SMILES
C1(C2=CN=NN2C3=CC4=C(NC5=CC=CC=C54)C=C3)=CC=CC=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Rac/Cdc42-IN-1 Related Classifications
HY-183246 Related Classifications
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