2. Protein Tyrosine Kinase/RTK
  3. RET
  4. RET-IN-32

RET-IN-32 是一种具有口服活性的 RET 抑制剂，对野生型和 V804M、G810S 突变型的 IC50 为 0.285、4.602 和 103.5 nM。RET-IN-32 可抑制 Tyr1062 的自磷酸化。RET-IN-32 可完全抑制 BAF3-KIF3B-RET-WT 异种移植物诱导的肿瘤生长。RET-IN-32 可用于甲状腺癌、肺癌的研究。

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RET-IN-32

RET-IN-32 Chemical Structure

CAS No. : 2620629-32-3

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RET-IN-32 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

RET-IN-32 is an orally active RET inhibitor with IC50 values of 0.285, 4.602 and 103.5 nM against wild-type, V804M and G810S mutant forms, respectively. RET-IN-32 inhibits the autophosphorylation of Tyr1062. RET-IN-32 completely suppresses tumor growth induced by BAF3-KIF3B-RET-WT xenografts. RET-IN-32 can be used in the research of thyroid cancer and lung cancer[1].

体外研究
(In Vitro)

RET-IN-32 (Compound 9) (72 h) 可抑制 BAF3-KIF5B-RET-WT 细胞的增殖，其 IC50 为 1.2 nM；同时可抑制 BAF3-KIF5B-RETV804M 细胞的增殖，其 IC50 为 212 nM[1]。
RET-IN-32 (1-100 nM; 12 h) 可在 BAF3-KIF5B-RET-WT 细胞中呈剂量依赖性降低 SPRY4 和 DUSP6 的 mRNA 表达，但对 GSK3B 的 mRNA 表达无影响[1]。
RET-IN-32 (1-1000 nM; 1 h) 可在 10 nM 浓度下显著抑制 BAF3-KIF5B-RET-WT 细胞中 RET Tyr1062 的自磷酸化，在 100 nM 浓度下则几乎实现完全抑制[1]。
RET-IN-32 (1-1000 nM; 12 h) 可在 BAF3-KIF5B-RET-WT 细胞中诱导剂量依赖性 G0/G1 期阻滞并减少 S 期细胞群[1]。
RET-IN-32 (10-1000 nM; 12 h) 可在 100 nM 和 1000 nM 浓度下诱导 BAF3-KIF5B-RET-WT 细胞发生细胞凋亡[1]。

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

RET-IN-32 相关抗体:

Real Time qPCR[1]

Cell Line: BAF3-KIF5B-RET-WT cells
Concentration: 1, 10 and 100 nM
Incubation Time: 12 h
Result: Exhibited dose-dependent inhibition of SPRY4 and DUSP6 mRNA expression.
Had no effect on GSK3B mRNA expression.

Western Blot Analysis[1]

Cell Line: BAF3-KIF5B-RET-WT cells
Concentration: 1, 10, 100 and 1000 nM
Incubation Time: 1 h
Result: Significantly inhibited RET autophosphorylation on Tyr1062 at 10 nM.
Nearly completely inhibited RET autophosphorylation at 100 nM.

Cell Cycle Analysis[1]

Cell Line: BAF3-KIF5B-RET-WT cells
Concentration: 1, 10, 100 and 1000 nM
Incubation Time: 12 h
Result: Induced dose-dependent G0/G1 phase arrest in BAF3-KIF5B-RET-WT cells.
Inhibited S phase progression in BAF3-KIF5B-RET-WT cells.

Apoptosis Analysis[1]

Cell Line: BAF3-KIF5B-RET-WT cells
Concentration: 1, 10, 100 and 1000 nM
Incubation Time: 12 h
Result: Increased the fraction of apoptotic cells in BAF3-KIF5B-RET-WT cells at 100 nM dose compared to the blank control group.
Increased the fraction of apoptotic cells in BAF3-KIF5B-RET-WT cells at 1000 nM dose compared to the blank control group.
药代动力学
(Parmacokinetics)
Species Dose Route AUClast AUCinf Tmax Cmax T1/2 CL Vss Bioavailability
Mice[1] 2 mg/kg i.v. 18200 ng·h/mL 18400 ng·h/mL 0.19 h 3340 ng/mL 3.40 h 1.80 mL/min/kg 0.48 L/kg /
Mice[1] 5 mg/kg i.g. 45700 ng·h/mL 45800 ng·h/mL 1.3 h 10800 ng/mL 2.7 h / / 99.8 %
体内研究
(In Vivo)

RET-IN-32 (Compound 9) (1-10 mg/kg；灌胃；每日 2 次；连续 15 天) 在 BAF3-KIF3B-RET-WT 异种移植模型中展现出强效的、剂量依赖性抗肿瘤功效[1]。

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

Animal Model: Balb/c nude (male, 4-6 weeks old, 18-20 g, subcutaneous xenograft model)[1]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: i.g.; twice daily; 15 days
Result: Produced significant dose-dependent reductions in tumor weight compared to vehicle control.
Achieved complete tumor growth inhibition at 10 mg/kg dose.
Caused no mortality or body weight changes in any treatment group throughout the 15-day study.
分子量

593.68

Formula

C33H35N7O4
CAS 号
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

RET-IN-32 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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:

RET-IN-322620629-32-3RETVEGFR2BAF3-KIF5B-RET-WT cellsBAF3-KIF5B-RETV804M cellslung cancerhuman wild-type RET kinaseTyr1062RETG810S kinaseshuman RETV804M mutant kinasethyroid cancerBAF3-KIF3B-RET-WT xenograftsInhibitorinhibitorinhibit

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