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ROR1-IN-4

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Catalog No. T212080

ROR1-IN-4 is a selective inhibitor of ROR1 with a dissociation constant (Kd) of 52 nM. It exhibits potent antiproliferative activity in the triple-negative breast cancer (TNBC) cell line MDA-MB-231, with an IC50 of 75 nM. ROR1-IN-4 reduces colony formation, induces apoptosis (apoptosis), and inhibits phosphorylation of ROR1(Tyr786) in these cells. Additionally, ROR1-IN-4 demonstrates significant antitumor efficacy in nude mice bearing subcutaneous MDA-MB-231 xenograft tumors. This compound is applicable for research related to TNBC.

ROR1-IN-4

ROR1-IN-4

😃Good
Catalog No. T212080
ROR1-IN-4 is a selective inhibitor of ROR1 with a dissociation constant (Kd) of 52 nM. It exhibits potent antiproliferative activity in the triple-negative breast cancer (TNBC) cell line MDA-MB-231, with an IC50 of 75 nM. ROR1-IN-4 reduces colony formation, induces apoptosis (apoptosis), and inhibits phosphorylation of ROR1(Tyr786) in these cells. Additionally, ROR1-IN-4 demonstrates significant antitumor efficacy in nude mice bearing subcutaneous MDA-MB-231 xenograft tumors. This compound is applicable for research related to TNBC.
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Product Introduction

Bioactivity
Description
ROR1-IN-4 is a selective inhibitor of ROR1 with a dissociation constant (Kd) of 52 nM. It exhibits potent antiproliferative activity in the triple-negative breast cancer (TNBC) cell line MDA-MB-231, with an IC50 of 75 nM. ROR1-IN-4 reduces colony formation, induces apoptosis (apoptosis), and inhibits phosphorylation of ROR1(Tyr786) in these cells. Additionally, ROR1-IN-4 demonstrates significant antitumor efficacy in nude mice bearing subcutaneous MDA-MB-231 xenograft tumors. This compound is applicable for research related to TNBC.
Targets&IC50
ROR1:0.052 μM (Kd)
In vitro
ROR1-IN-4 (Compound 59) exhibits potent antiproliferative activity in triple-negative breast cancer (TNBC) cell line MDA-MB-231, with an IC50 of 0.075 μM, whereas it shows no significant antiproliferative effect in non-TNBC cell lines MCF-7 (IC50 > 10 μM) and HEK-293T (IC50 = 9.72 μM). Additionally, ROR1-IN-4 (0.1-3 μM, 48 h) induces apoptosis and suppresses the phosphorylation of ROR1 (Tyr786) in MDA-MB-231 cells. Furthermore, ROR1-IN-4 (0.1-1 μM, 14 days) reduces colony formation in MDA-MB-231 cells.
In vivo
Compound ROR1-IN-4 (Compound 59), administered intraperitoneally at doses of 10-20 mg/kg every other day for 30 days, demonstrates excellent antitumor activity in nude mice with MDA-MB-231 subcutaneous xenograft tumors. Additionally, ROR1-IN-4 at 10 mg/kg, delivered intraperitoneally every other day for 45 days, exhibits strong inhibition of tumor growth and metastasis in nude mice with MDA-MB-231-Luc orthotopic breast xenograft tumors.
Chemical Properties
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2OTargetMol | reagent mix well and clarify
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