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/ Linsitinib

Linsitinib {[allProObj[0].p_purity_real_show]}

货号：A139562 同义名： OSI-906

Linsitinib（OSI-906）是一种高效、选择性和口服可用的IGF-1受体和胰岛素受体（IR）的双重抑制剂，IC50分别为35 nM和75 nM。

Linsitinib 化学结构 CAS号：867160-71-2
Linsitinib 化学结构
CAS号：867160-71-2
Linsitinib 3D分子结构
CAS号：867160-71-2
Linsitinib 化学结构 CAS号：867160-71-2
Linsitinib 3D分子结构 CAS号：867160-71-2
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Linsitinib 纯度/质量文件 产品仅供科研

货号：A139562 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
• Cell, 2025. Ambeed. [ A122167 ]
• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
更多 >
产品名称 IGF-1R ↓ Insulin Receptor ↓ 其他靶点 纯度
BMS-536924 ++

IGF-1R, IC50: 100 nM

 		+++

Insulin Receptor, IC50: 73 nM

 		FAK,MEK 98%
GSK1904529A +++

IGF-1R, IC50: 27 nM

 		+++

Insulin Receptor, IC50: 25 nM

 		98+%
Picropodophyllin ++++

IGF-1R, IC50: 1 nM

 		99%+
NVP-AEW541 ++

IGF-1R, IC50: 0.15 μM

 		++

Insulin Receptor, IC50: 0.14 μM

 		FLT3 99%+
NVP-ADW742 +

IGF-1R, IC50: 0.17 μM

 		98%
GSK1838705A +++

IGF-1R, IC50: 2 nM

 		++++

Insulin Receptor, IC50: 1.6 nM

 		ALK 98%
BMS-754807 ++++

IGF-1R, IC50: 1.8 nM

 		++++

Insulin Receptor, IC50: 1.7 nM

 		99%+
Linsitinib +++

IGF-1R, IC50: 35 nM

 		++

Insulin Receptor, IC50: 75 nM

 		99%+
AG1024 +

IGF-1R, IC50: 7 μM

 		+

Insulin Receptor, IC50: 57 μM

 		98%
PQ401 +

IGF-1R, IC50: <1 μM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Linsitinib 生物活性

靶点

  • IGF-1R

    IGF-1R, IC50:35 nM

  • Insulin Receptor

    Insulin Receptor, IC50:75 nM
描述 IGF-1R (insulin-like growth factor-1 receptor) plays a key role in transformation, growth and survival of malignant cells, and has been considered as a general and promising target for cancer treatment. Linsitinib is a potent and selective IGF-1R receptor with IC50 value of 35nM, also show inhibitory effect against Insulin receptor and insulin receptor-related receptor with IC50 values of 75nM for both (measured by purified recombinant kinase activity). Treatment with Linsitinib at concentration ranging in 0.01-1μM for 2h could dose-dependently inhibited autophosphorylation of IGF-1R, at phosphorylation of the downstream, including AKT, ERK and p70S6K with IC50 of 24nM, 130nM, 28nM and 60nM, respectively, in 3T3/huIGF-1R (LISN) cells. Also the inhibition on phosphorylation of both IGF-1R and IR by Linsitinib was shown in HT-29 and Colo-205 cells. The antiproliferative effect of Linsitinib could be observed in a panel of cell lines from various tumor types with IC50 ranging in 0.021-0.81μM, including HT29, Colo205, SW620 (colorectal), DU4475, MCF7 (breast), 3T3/huIGF-1R (mouse fibroblast), H358, H292 (non-small-cell lung), BxPC3 (pancreatic) and A673 (rhabdomyosarcoma) cell lines. A further study showed that a panel of non-small-cell lung cancer and colorectal cancer (CRC) tumor cell lines exhibiting an epithelial phenotype exhibited greater sensitivity to Linsitinib than those tumor cells that have undergone an epithelial–mesenchymal transition. A single oral dose of 75mg/kg Linsitinib inhibited the autophosphorylation of IGF-1R 2-24h after dose in LISN tumor xenograft models, suggesting the pharmacodynamics of this compound. Oral administration of Linsitinib at 75mg/kg once-daily for 12 days significantly inhibit tumor growth in a LISN xenograft model[1].
作用机制 Linsitinib can attach to the ATP-binding pocket of tyrosine kinase receptors, causing dual inhibition of both IR and IGF-1R.[1]

Linsitinib 细胞实验

Cell Line
Concentration Treated Time Description References
CAFs 5 μM Linsitinib evidently inhibited fibroblast proliferation J Clin Invest. 2024 Nov 15;134(22):e183366.
iKras cells 1 μM 24 h Enhanced nab-PTX uptake and cytotoxicity Nat Nanotechnol. 2021 Jul;16(7):830-839.
A549 2 μM 1 day Linsitinib alone or in combination with Dasatinib suppressed the phosphorylation of IGF-1R, Src, and Akt Mol Cancer. 2015 Jun 4;14:113.
H226B 1 μM 5 days Linsitinib treatment increased the stability of IGF-1R and Src proteins, enhancing the reciprocal co-activation of IGF-1R and Src Mol Cancer. 2015 Jun 4;14:113.
liv7k oral cancer cell line 10 µM 72 h To test the drug response of Linsitinib in liv7k oral cancer cells, the results showed cell viability under hypoxic and normoxic conditions. Nat Commun. 2018 Jun 29;9(1):2546.
CAFs 5 μM Linsitinib significantly reduced the CAF-mediated inhibition of T cell migration J Clin Invest. 2024 Nov 15;134(22):e183366.
OMM1.3 cells 1 μM 24 h To study the effect of Linsitinib on UM cell proliferation and cell cycle. It was found that Linsitinib alone had a less significant inhibitory effect on UM cell proliferation. Mol Cancer Ther. 2023 Jan 3;22(1):63-74.
UM001 cells 1 μM 24 h To study the effect of Linsitinib on UM cell proliferation and cell cycle. It was found that Linsitinib alone had a less significant inhibitory effect on UM cell proliferation. Mol Cancer Ther. 2023 Jan 3;22(1):63-74.
92.1 cells 1 μM 24 h To study the effect of Linsitinib on UM cell proliferation and cell cycle. It was found that Linsitinib alone had a less significant inhibitory effect on UM cell proliferation. Mol Cancer Ther. 2023 Jan 3;22(1):63-74.
HCT-15 0.14 μM 96 h Evaluate the effect of Linsitinib on HCT-15 cells, results show that Linsitinib exhibits resistance in HCT-15 cells. Nat Commun. 2024 May 9;15(1):3909.
HT115 0.14 μM 96 h Evaluate the effect of Linsitinib on HT115 cells, results show that Linsitinib exhibits resistance in HT115 cells. Nat Commun. 2024 May 9;15(1):3909.
LS1034 0.14 μM 96 h Evaluate the effect of Linsitinib on LS1034 cells, results show that Linsitinib exhibits sensitivity in LS1034 cells. Nat Commun. 2024 May 9;15(1):3909.
NCI-H508 0.14 μM 96 h Evaluate the effect of Linsitinib on NCI-H508 cells, results show that Linsitinib exhibits sensitivity in NCI-H508 cells. Nat Commun. 2024 May 9;15(1):3909.
SNU-61 0.14 μM 96 h Evaluate the effect of Linsitinib on SNU-61 cells, results show that Linsitinib exhibits resistance in SNU-61 cells. Nat Commun. 2024 May 9;15(1):3909.
HCC4006 1 μM 72 h Evaluate the effect of Linsitinib combined with Osimertinib on HCC4006 cells, results showed that the combination enhanced the effect of Osimertinib. Nat Commun. 2020 Sep 14;11(1):4607.
HCC827 1 μM 72 h Evaluate the effect of Linsitinib combined with Osimertinib on HCC827 cells, results showed that the combination enhanced the effect of Osimertinib. Nat Commun. 2020 Sep 14;11(1):4607.
H3255 1 μM 72 h Evaluate the effect of Linsitinib combined with Osimertinib on H3255 cells, results showed that the combination enhanced the effect of Osimertinib. Nat Commun. 2020 Sep 14;11(1):4607.

Linsitinib 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice NSCLC xenograft model Oral 25 or 50 mg/kg 6 times per week for 3 weeks Combined treatment with Linsitinib and Dasatinib significantly suppressed tumor growth and increased the levels of active caspase-3 in tumor tissues, while decreasing the expression of PCNA, pIGF-1R, and pSrc Mol Cancer. 2015 Jun 4;14:113.
Mice EO771 and MC38 tumor models Intraperitoneal injection 10 mg/kg Linsitinib significantly enhanced the therapeutic efficacy of immune checkpoint blockade, reduced tumor growth, and prolonged survival J Clin Invest. 2024 Nov 15;134(22):e183366.
NSG mice Metastatic UM mouse model Oral gavage 25-40 mg/kg Daily for two weeks To test the inhibitory effect of Linsitinib in combination with YM-254890 on the growth of metastatic uveal melanoma tumors, results showed that the combination treatment significantly inhibited tumor growth. Mol Cancer Ther. 2023 Jan 3;22(1):63-74.
Mice HCC4006 cell line-derived xenograft model Oral 50 mg/kg Once daily for 10 days Evaluate the effect of Linsitinib combined with Osimertinib on HCC4006 xenograft model, results showed that the combination induced tumor shrinkage and prevented regrowth. Nat Commun. 2020 Sep 14;11(1):4607.
Mice Intracranial xenograft model Oral 50 mg/kg Daily until neurological signs appeared Linsitinib prolonged tumor latency and reduced tumor volumes Cancer Discov. 2021 Feb;11(2):480-499

Linsitinib 动物研究

Dose Mice: 25 mg/kg[2] (p.o.), 5 mg/kg[1] (i.v.), 100 mg/kg[1] (p.o.) Rat: 5 mg/kg[1] (i.v.), 20 mg/kg[1] (p.o.)
Administration p.o., i.v.
Pharmacokinetics
Animal Mice[1] Rats[1] Dogs[1]
Dose 5 mg/kg (i.v.)
25 mg/kg (p.o.) 		5 mg/kg (i.v.)
100 mg/kg (p.o.) 		2.5 mg/kg (i.v.)
5 mg/kg (p.o.)
Administration i.v.
p.o. 		i.v.
p.o. 		i.v.
p.o.
F 100% (p.o.) 92% (p.o.) 64% (p.o.)
AUC0→last 26741 ng·h/ml (p.o.) 424076 ng·h/ml (p.o.) 1328 ng·h/ml (p.o.)
Tβ 2.64 h (i.v.)
t1/2β 1.18 h (i.v.)
T1/2β 2.14 h (i.v.)
CL 12 ml/min/kg (i.v.) 4 ml/min/kg (i.v.) 39 ml/min/kg (i.v.)
Cmax 16.04 μM (p.o.) 34.64 μM (p.o.) 1.20 μM (p.o.)
AUC0→∞ 6954 ng·h/ml (i.v.) 23123 ng·h/ml (i.v.) 1066 ng·h/ml (i.v.)
Vss 2.05 L/kg (i.v.) 0.79 L/kg (i.v.) 4.30 L/kg (i.v.)

Linsitinib 参考文献

[1]Murakami T, Singh AS, et al. Effective molecular targeting of CDK4/6 and IGF-1R in a rare FUS-ERG fusion CDKN2A-deletion doxorubicin-resistant Ewing's sarcoma patient-derived orthotopic xenograft (PDOX) nude-mouse model. Oncotarget. 2016 Jul 26;7(30):47556-47564.

Linsitinib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.37mL

0.47mL

0.24mL

11.86mL

2.37mL

1.19mL

23.73mL

4.75mL

2.37mL

Linsitinib 技术信息

CAS号867160-71-2
分子式C26H23N5O
分子量 421.49
SMILES Code O[C@@]1(C)C[C@@H](C2=NC(C3=CC=C4C=CC(C5=CC=CC=C5)=NC4=C3)=C6C(N)=NC=CN62)C1
MDL No. MFCD12912153
别名 OSI-906
运输蓝冰
InChI Key PKCDDUHJAFVJJB-UHFFFAOYSA-N
Pubchem ID 11640390
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C
溶解方案

DMSO: 50 mg/mL(118.63 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一

Tags: Linsitinib | 867160-71-2 | OSI-906 | OSI906 | OSI 906 | IGF-1R/Insulin Receptor Inhibitor | Protein Tyrosine Kinase/RTK | IGF-1R | Insulin Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Linsitinib 纯度/质量文件 | Linsitinib 亚型比较 | Linsitinib 生物活性 | Linsitinib 动物研究 | Linsitinib 参考文献 | Linsitinib 实验方案 | Linsitinib 技术信息

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