IGF-1R

Inhibitory Selectivity

Catalog No.	Inhibitor Name	IGF-1R	Insulin Receptor	Other
A11053	Linsitinib	***	**	IRR
A11021	NVP-AEW541	**	**	FLT3,Tek,FLT1
A10440	GSK1904529A	***	***	IKK3,VEGFR2,Syk
A10658	NVP-ADW742	*
A11054	BMS-536924	**	***	FAK,MEK,LCK
A11400	AG-1024	*	*
A11175	GSK1838705A	***	****	ALK,RSK1,JNK3
A11059	BMS-754807	****	****	TrkB,Met,TrkA
A11951	PQ 401	*
A12195	Picropodophyllin	****

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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BMS-536924

Catalog No. A11054
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IGF-1R 抑制剂

BMS-536924是有效的IGF-IR抑制剂，可导致IGF-IR介导的转化表型逆转。了解更多

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- Qiao Zhou, .et al. BMS-536924, an ATP-competitive IGF-1R/IR inhibitor, decreases viability and migration of temozolomide-resistant glioma cells in vitro and suppresses tumor growth in vivo, Onco Targets Ther., 2015, 8: 689-697 PMID: 25897243
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GSK1904529A

Catalog No. A10440
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IGF-1R 抑制剂

GSK1904529A分别用27和25 nmol/L的IC(50)s选择性抑制IGF-IR和IR。了解更多

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PQ 401

Catalog No. A11951
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IGF-1R 抑制剂

PQ 401是可透过细胞的苯基喹啉基-脲化合物，可抑制IGF-1R自磷酸化，IC50为低于1 μM。了解更多

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Picropodophyllin

Catalog No. A12195
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Picropodophyllin是首个靶向口服小分子igf-1受体抑制剂，IC50为1 nM。对胰岛素受体无影响。了解更多

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XL-228

Catalog No. A13069
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IGF-1R, Aurora, FGFR, ABL, SRC 抑制剂

XL228是靶向IGF1R，AURORA激酶，FGFR1-3，ABL和SRC家族激酶的蛋白激酶抑制剂。XL228是一种Aurora A抑制剂（IC50，f3 nmol/L），对ABL1（Ki，5 nmol/L）以及BCR-ABL1 T315I（Ki，1.4 nmol/L）激酶显示出有效的生化活性。了解更多

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AZD3463

Catalog No. A13065
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ALK/IGF1R 抑制剂

AZD3463是ALK/IGF1R抑制剂。了解更多

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NT157

Catalog No. A16247
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IRS-1/2 抑制剂

NT157是IRS-1/2的选择性抑制剂。了解更多

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NVP-AEW541

Catalog No. A11021
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IGF-1R 抑制剂

NVP-AEW541是一种选择性的IGF-1R激酶抑制剂，可抑制IGF-1R的自磷酸化活性（IC50 = 0.086 uM）并阻止IGF-1介导的MCF-7细胞存活和增殖（IC50分别为0.16和1.64 uM）。了解更多

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- Tsushima H, .et al. Kinase inhibitors of the IGF-1R as a potential therapeutic agent for rheumatoid arthritis, Autoimmunity, 2017, Aug;50(5):329-335 PMID: 28682648
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OSI-906

Catalog No. A11053
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IGF-1R 抑制剂

OSI-906是一种选择性IGF-1R抑制剂，在无细胞试验中IC50为35 nM；对InsR抑制作用适中，IC50为75 nM，对Abl，ALK，BTK，EGFR， FGFR1/2，PKA等没有抑制活性。了解更多

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- Masao Kakoki, .et al. Cyanocobalamin prevents cardiomyopathy in type 1 diabetes by modulating oxidative stress and DNMT-SOCS1/3-IGF-1 signaling, Communications Biology, 2021, 4:775
- Nakamura T, .et al. Naturally Occurring Hair Growth Peptide: Water-Soluble Chicken Egg Yolk Peptides Stimulate Hair Growth Through Induction of Vascular Endothelial Growth Factor Production, J Med Food, 2018, Jul;21(7):701-708 PMID: 29583066
- Tzeng SF, .et al. O-Glycosylation-mediated signaling circuit drives metastatic castration-resistant prostate cancer, FASEB J, 2018, Jun 15:fj201800687 PMID: 29906246
- Takata N, .et al. IGF-2/IGF-1R signaling has distinct effects on Sox1, Irx3, and Six3 expressions during ES cell derived-neuroectoderm development in vitro, In Vitro Cell Dev Biol Anim., 2016, May;52(5):607-15 PMID: 26956358
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BMS-754807

Catalog No. A11059
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IGF-1R 抑制剂

BMS-754807是一种有效的，口服活性生长因子1受体/胰岛素受体家族靶向的激酶抑制剂。了解更多

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- Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961
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AG-1024 (Tyrphostin)

Catalog No. A11400
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IGF-1R 抑制剂

AG-1024 (Tyrphostin)是胰岛素样生长因子-1 (IGF-1) 和胰岛素受体酪氨酸激酶活性的特异性抑制剂。与胰岛素受体相比，IGF-1的IC50值更低。还抑制胰岛素刺激的细胞增殖。了解更多

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- Maeda A, .et al. Safranal, a novel protein tyrosine phosphatase 1B inhibitor, activates insulin signaling in C2C12 myotubes and improves glucose tolerance in diabetic KK-Ay mice., Mol Nutr Food Res. , 2014, 58(6):1177-89 PMID: 24668740
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GSK1838705A

Catalog No. A11175
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IGF-1R 抑制剂

GSK1838705A是一种小分子激酶抑制剂，其抑制IGF-IR和胰岛素受体的IC50分别为2.0和1.6 nmol/L。了解更多

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- Watanabe S, .et al. Insulin augments serotonin-induced contraction via activation of the IR/PI3K/PDK1 pathway in the rat carotid artery, Pflugers Arch, 2016, Apr;468(4):667-77 PMID: 26577585
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NVP-ADW742

Catalog No. A10658
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IGF-1R 抑制剂

NVP-ADW742是一种IGF-1R抑制剂，IC50为0.17μM。了解更多

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- Kazuya Takayama, .et al. Leucine/glutamine and v-ATPase/lysosomal acidification via mTORC1 activation are required for position-dependent regeneration, Sci Rep, 2018, 8: 8278 PMID: 29844341
- Kentaro Hirose, .et al. Mechanistic target of rapamycin complex 1 signaling regulates cell proliferation, cell survival, and differentiation in regenerating zebrafish fins, BMC Dev Biol, 2014, 14: 42. PMID: 25480380
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Indirubin Derivative E804

Catalog No. A21052
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IGF1R inhibitor

E 804 is a potent inhibitor of Insulin-like Growth Factor 1 Receptor (IGF1R), with an IC50 of 0.65 μM for IGF1R. 了解更多

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