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

ROR1-IN-4 是一种选择性的 ROR1 抑制剂，其 Kd 为 52 nM。ROR1-IN-4 在三阴性乳腺癌 (TNBC) 细胞系 MDA-MB-231 中显示出强效的抗增殖活性 (IC50 = 75 nM)。ROR1-IN-4 能够减少 MDA-MB-231 细胞的集落形成，诱导细胞凋亡 (apoptosis)，并抑制 ROR1 (Tyr786) 的磷酸化。ROR1-IN-4 在承载 MDA-MB-231 皮下异种移植瘤的裸鼠中展现出优越的抗肿瘤效能。ROR1-IN-4 可用于三阴性乳腺癌 (TNBC) 的相关研究。

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ROR1-IN-4

ROR1-IN-4 Chemical Structure

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ROR1-IN-4 相关抗体

Top Publications Citing Use of Products

查看 ROR 亚型特异性产品:

查看所有亚型
RORγ RORα RORβ

查看 Bcl-2 Family 亚型特异性产品:

查看所有亚型
Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3

查看 PARP 亚型特异性产品:

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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

体外研究
(In Vitro)

ROR1-IN-4 (Compound 59) (72 h) 在三阴性乳腺癌 (TNBC) 细胞系 MDA-MB-231 中显示出强效的抗增殖活性 (IC50 = 0.075 μM)，而在非三阴性乳腺癌细胞系 MCF-7 (IC50 > 10 μM) 和 HEK-293T (IC50 = 9.72 μM) 中无显著抗增殖活性[1]。
ROR1-IN-4 (0.1-3 μM, 48 h) 在 MDA-MB-231 细胞中诱导细胞凋亡并抑制 ROR1 (Tyr786) 的磷酸化[1]。
ROR1-IN-4 (0.1-1 μM, 14 天) 减少 MDA-MB-231 细胞的集落形成[1]。

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

ROR1-IN-4 相关抗体:

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.
体内研究
(In Vivo)

ROR1-IN-4 (Compound 59) (10-20 mg/kg, i.p, 每隔一天, 30 天) 在 MDA-MB-231 皮下异种移植瘤的裸鼠中展现出优越的抗肿瘤效能[1]。
ROR1-IN-4 (10 mg/kg, i.p, 每隔一天, 45 天) 在 MDA-MB-231-Luc 原位乳腺异种移植瘤的裸鼠中表现出强效的抗肿瘤生长和抗转移作用[1]。

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.
分子量

516.58

Formula

C29H30F2N6O
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

ROR1-IN-4 相关分类

  • 摩尔计算器

  • 稀释计算器

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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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