2. Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR MAPK/ERK Pathway Stem Cell/Wnt
  3. RET VEGFR PDGFR Akt ERK
  4. RET-IN-33

RET-IN-33 (Compound CN-3) 是一种中等选择性的 RET 突变体抑制剂。RET-IN-33 有效抑制 G810 突变体，IC50 值分别为 4.43 nM (G810R)、3.28 nM (G810C) 和 0.51 nM (G810S)。RET-IN-33 也抑制其他 RET 突变体：V804M (IC50 0.73 nM)、V804L (IC50 0.36 nM)、Y806H (IC50 0.74 nM) 以及 M918T (IC50 0.55 nM)。RET-IN-33 也抑制其他激酶，对 VEGFR2 的 IC50 为 1.50 nM，对 PDGFRα 的 IC50 为 1.60 nM。RET-IN-33 可阻断 RET 突变体的自磷酸化及下游 SHC/AKT/ERK 信号通路。RET-IN-33 可选择性抑制 RET 驱动细胞模型的增殖，而不影响非 RET 依赖型细胞或正常细胞。RET-IN-33 在 RET 驱动的异种移植模型中表现出剂量依赖性的抗肿瘤功效。RET-IN-33 可用于甲状腺髓样癌、甲状腺乳头状癌和非小细胞肺癌的研究。

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RET-IN-33

RET-IN-33 Chemical Structure

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RET-IN-33 相关抗体

Top Publications Citing Use of Products

查看 VEGFR 亚型特异性产品:

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

查看 PDGFR 亚型特异性产品:

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PDGFR PDGFRβ PDGFRα

查看 Akt 亚型特异性产品:

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Akt Akt1 Akt2 Akt3

查看 ERK 亚型特异性产品:

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ERK ERK1 ERK2 ERK5 ERK8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

RET-IN-33 (Compound CN-3) is a moderately selective inhibitor of RET mutants. RET-IN-33 potently inhibits G810 mutants, with IC50 values of 4.43 nM (G810R), 3.28 nM (G810C) and 0.51 nM (G810S), respectively. RET-IN-33 also inhibits other RET mutants: V804M (IC50 0.73 nM), V804L (IC50 0.36 nM), Y806H (IC50 0.74 nM) and M918T (IC50 0.55 nM). RET-IN-33 also inhibits other kinases, with an IC50 of 1.50 nM against VEGFR2 and 1.60 nM against PDGFRα. RET-IN-33 blocks the autophosphorylation of RET mutants and the downstream SHC/AKT/ERK signaling pathway. RET-IN-33 selectively inhibits the proliferation of RET-driven cell models without affecting non-RET-dependent or normal cells. RET-IN-33 exhibits dose-dependent antitumor efficacy in RET-driven xenograft models. RET-IN-33 can be used for the research of medullary thyroid carcinoma, papillary thyroid carcinoma and non-small cell lung cancer[1].

IC50 & Target[1]

VEGFR2

1.50 nM (IC50)

PDGFRα

1.60 nM (IC50)

体外研究
(In Vitro)

RET-IN-33 可强效抑制野生型 RET 及多种具有临床相关性的 RET 激酶突变体，所有受试 RET 亚型的 IC50 范围为 0.36 nM 至 40.2 nM[1]。
RET-IN-33 (1.50-54.8 nM) 可强效抑制 PDGFRα 和 VEGFR2，其 IC50 值分别为 1.60 nM 和 1.50 nM，且对 FGFR1 的抑制作用较弱，IC50 值为 54.8 nM[1]。
RET-IN-33 (72 h) 可强效且选择性地抑制 RET 依赖性 TT 和 LC-2/ad 细胞的增殖，其 IC50 值分别为 2.48 nM 和 17.05 nM[1]。
RET-IN-33 (1-100 nM (TT cells), 10-1000 nM (LC-2/ad cells); 24 h) 可在 TT 和 LC-2/ad 细胞中诱导剂量依赖性 G0−G1 期细胞周期阻滞，在最高测试浓度下，分别将 G0−G1 期细胞比例提升至 75.1% 和 79.0%[1]。

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

RET-IN-33 相关抗体:

Cell Proliferation Assay[1]

Cell Line: RET-dependent human cancer cell lines (TT, LC-2/ad)
Concentration: A certain concentration
Incubation Time: 72 h
Result: Inhibited proliferation of TT cells with an IC50 of 2.48 nM.
Inhibited proliferation of LC-2/ad cells with an IC50 of 17.05 nM.
Outperformed pralsetinib in TT cells.

Cell Proliferation Assay[1]

Cell Line: Ba/F3 cells expressing RET fusions or resistance mutations (Ba/F3-CCDC6-RET, Ba/F3-CCDC6-RET-V804M, Ba/F3-CCDC6-RET-G810C, Ba/F3-CCDC6-RET-G810R, Ba/F3-KIF5B-RET, Ba/F3-KIF5B-RET-V804M, Ba/F3-KIF5B-RET-G810C, Ba/F3-KIF5B-RET-G810R)
Concentration: A certain concentration
Incubation Time: 72 h
Result: Inhibited proliferation of Ba/F3-CCDC6-RET cells with an IC50 of 6.1 nM.
Inhibited proliferation of Ba/F3-CCDC6-RET-V804M cells with an IC50 of 13.6 nM.
Inhibited proliferation of Ba/F3-CCDC6-RET-G810C cells with an IC50 of 15.3 nM.
Inhibited proliferation of Ba/F3-CCDC6-RET-G810R cells with an IC50 of 10.9 nM.
Inhibited proliferation of Ba/F3-KIF5B-RET cells with an IC50 of 24.1 nM.
Inhibited proliferation of Ba/F3-KIF5B-RET-V804M cells with an IC50 of 25.5 nM.
Inhibited proliferation of Ba/F3-KIF5B-RET-G810C cells with an IC50 of 91.9 nM.
Inhibited proliferation of Ba/F3-KIF5B-RET-G810R cells with an IC50 of 59.6 nM.
Retained far higher potency against G810 mutants compared to pralsetinib.

Cell Proliferation Assay[1]

Cell Line: non-RET-dependent human cancer and normal cell lines (A549, HepG2, HCT-116, KMS-28PE, OCI, MDA-MB-231, HeLa, A375, 293T, HUVEC)
Concentration: A certain concentration
Incubation Time: 72 h
Result: Showed minimal sensitivity in A549, HepG2, OCI, and A375 cells (IC50 > 10 μM).
Inhibited growth of HCT-116 cells with an IC50 of 3760.01 nM.
Inhibited growth of KMS-28PE cells with an IC50 of 5099.82 nM.
Inhibited growth of MDA-MB-231 cells with an IC50 of 3018.00 nM.
Inhibited growth of HeLa cells with an IC50 of 2701.01 nM.
Inhibited growth of 293T cells with an IC50 of 810.93 nM.
Inhibited growth of HUVEC cells with an IC50 of 5676.00 nM.

Cell Cycle Analysis[1]

Cell Line: RET-dependent human cancer cell lines (TT, LC-2/ad)
Concentration: 1-100 nM (TT cells); 10-1000 nM (LC-2/ad cells)
Incubation Time: 24 h
Result: Increased the proportion of G0−G1 phase TT cells to 54.1%, 64.1%, and 75.1% at 1, 10, and 100 nM, respectively (vs 53.5% in control).
Increased the proportion of G0−G1 phase LC-2/ad cells to 60.6%, 70.3%, and 79.0% at 10, 100, and 1000 nM, respectively.
药代动力学
(Parmacokinetics)
Species Dose Route Cmax AUC0-∞ CL T1/2 Bioavailability
Mice[1] 1 mg/kg i.v. 330 ng/mL 126 8115 mL/h/kg 0.690 h /
Mice[1] 10 mg/kg p.o. 50.7 ng/mL 72.9 / 0.835 h 5.8 %
体内研究
(In Vivo)

RET-IN-33 (10-50 mg/kg；腹腔注射；每日一次；14 天) 在 LC-2/ad 异种移植模型中表现出显著的剂量依赖性抗肿瘤活性，在 50 mg/kg 剂量下达到 160% 的最大 TGI，且耐受性良好[1]。
RET-IN-33 (10-25 mg/kg；腹腔注射；每日一次；连续 10 天) 对 Ba/F3-CCDC6-RETG810R 异种移植物具有剂量依赖性抗肿瘤活性，在 25 mg/kg 剂量下达到 61.9% 的 TGI，且耐受性良好[1]。

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

Animal Model: BALB/c nude (female, 6−8 weeks old, 18−20 g, subcutaneous xenograft of LC-2/ad cells)[1]
Dosage: 10 mg/kg; 25 mg/kg; 50 mg/kg
Administration: i.p.; daily; 14 days
Result: Induced dose-dependent tumor growth inhibition with tumor growth inhibition (TGI) values of 123%, 135%, and 160% at 10, 25, and 50 mg/kg, respectively.
Increased corresponding tumor inhibitory rates (IR) from 63.8% to 82.2%.
Caused no significant body-weight loss across all doses.
Animal Model: NOD-SCID (female, 6−8 weeks old, 18−20 g, subcutaneous xenograft of Ba/F3-CCDC6-RET-G810R cells)[1]
Dosage: 10 mg/kg; 25 mg/kg
Administration: i.p.; daily; 10 days
Result: Induced dose-dependent tumor growth inhibition with TGI values of 33.2% and 61.9% at 10 and 25 mg/kg, respectively.
Increased corresponding tumor IR were 22.6% and 52.5%.
Caused no significant body-weight loss across all doses.
分子量

553.58

Formula

C28H30F3N7O2
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-33 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

RET-IN-33RETVEGFRPDGFRAktERKVascular endothelial growth factor receptorPlatelet-derived growth factor receptorPKBProtein kinase BExtracellular signal regulated kinasesSHCAKTPDGFRαpapillary thyroid carcinomanonsmall cell lung cancermedullary thyroid carcinomaVEGFR2FGFR1Inhibitorinhibitorinhibit

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