2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Apoptosis Cell Cycle/DNA Damage Epigenetics
  3. ROR Apoptosis Bcl-2 Family PARP
  4. ROR1-IN-4

ROR1-IN-4 is a selective ROR1 inhibitor with a Kd of 52 nM. ROR1-IN-4 shows potent anti-proliferative activity against TNBC cell line MDA-MB-231 (IC50 = 75 nM). ROR1-IN-4 reduces colony formation, induces apoptosis and inhibits the phosphorylation of ROR1 (Tyr786) in MDA-MB-231 cells. ROR1-IN-4 demonstrates superior anti-tumor efficacy in nude mice bearing MDA-MB-231 subcutaneous xenografts. ROR1-IN-4 can be used for the study of triple-negative breast cancer (TNBC).

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

ROR1-IN-4

ROR1-IN-4 Chemical Structure

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ROR1-IN-4 Related Antibodies

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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Description

ROR1-IN-4 is a selective ROR1 inhibitor with a Kd of 52 nM. ROR1-IN-4 shows potent anti-proliferative activity against TNBC cell line MDA-MB-231 (IC50 = 75 nM). ROR1-IN-4 reduces colony formation, induces apoptosis and inhibits the phosphorylation of ROR1 (Tyr786) in MDA-MB-231 cells. ROR1-IN-4 demonstrates superior anti-tumor efficacy in nude mice bearing MDA-MB-231 subcutaneous xenografts. ROR1-IN-4 can be used for the study of triple-negative breast cancer (TNBC)[1].

IC50 & Target[1]

ROR1

0.052 μM (Kd)

In Vitro

ROR1-IN-4 (Compound 59) (72 h) shows potent anti-proliferative activity against TNBC cell line MDA-MB-231 (IC50 = 0.075 μM), and no significant anti-proliferative activity against non-TNBC cell line MCF-7 (IC50 > 10 μM) and HEK-293T (IC50 = 9.72 μM)[1].
ROR1-IN-4 (0.1-3 μM, 48 h) induces apoptosis and inhibits the phosphorylation of ROR1 (Tyr786) in MDA-MB-231 cells[1].
ROR1-IN-4 (0.1-1 μM, 14 days) reduces colony formation in MDA-MB-231 cells[1].

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

ROR1-IN-4 Related Antibodies

Apoptosis Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.1, 0.3, 1 μM
Incubation Time: 48 h
Result: Induced apoptosis in MDA-MB-231 cells.
Reduced the expression of anti-apoptotic protein Bcl-2.
Increased the expression of pro-apoptotic protein Bax, and promotes the cleavage of PARP in a concentration-dependent manner.
In Vivo

ROR1-IN-4 (Compound 59) (10-20 mg/kg, i.p, every other day, 30 days) demonstrates superior anti-tumor efficacy in nude mice bearing MDA-MB-231 subcutaneous xenografts[1].
ROR1-IN-4 (10 mg/kg, i.p, every other day, 45 days) exerts potent anti-tumor growth and anti-metastasis effects in nude mice with MDA-MB-231-Luc orthotopic breast xenografts[1].

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

Animal Model: MDA-MB-231 cells (5 × 106 in 100 µL mixture of PBS and Matrigel at 1:1 ratio) were subcutaneously implanted into the flanks of 4-5-week-old female BALB/c nude mice to establish the subcutaneous TNBC xenograft model[1]
Dosage: 10, 20 mg/kg
Administration: i.p. every other day for 30 days
Result: Achieved tumor growth inhibition (TGI) rates of 62.1% and 92.1% at doses of 10 mg/kg and 20 mg/kg, respectively.
Showed no significant decrease in body weight of nude mice during the 30-day administration period.
Led to no significant histopathological changes in major organs (heart, liver, spleen, lung, kidney) of nude mice.
Resulted in no increase in tumor size of nude mice in the 20 mg/kg dose group throughout the entire administration period.
Animal Model: MDA-MB-231-Luc cells (3 × 106) were orthotopically implanted into the mammary fat pads of 4-5-week-old female BALB/c nude mice to establish the orthotopic breast TNBC xenograft model[1]
Dosage: 10 mg/kg
Administration: i.p. every other day for 45 days
Result: Significantly reduced the size of orthotopic breast tumors in nude mice.
Inhibited tumor metastasis effectively: no tumor metastasis was found in nude mice at the 45th day of treatment.
Caused no obvious pathological changes in the heart and kidneys of nude mice; only mild inflammatory cell infiltration was observed in the liver, and the degree of spleen lesions and tumor cell invasion was lower than that in the vehicle group.
Delayed the occurrence of mouse death.
Showed no significant abnormal changes in the body weight.
Molecular Weight

516.58

Formula

C29H30F2N6O
SMILES

FC(C1=CC(NC(C2=CC=C(C(C3=CC=C4N=C(N=CC4=C3)N)=C2)C)=O)=CC=C1CN5CCN(CC5)C)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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ROR1-IN-4 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.

Keywords:

ROR1-IN-4RORApoptosisBcl-2 FamilyPARPRAR-related orphan receptorpoly ADP ribose polymerasetriple-negative breast cancerapoptosisMDA-MB-231ROR1Inhibitorinhibitorinhibit

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