Linsitinib (OSI-906)

Linsitinib (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。Phase 3。

Linsitinib (OSI-906) Chemical Structure

Linsitinib (OSI-906) Chemical Structure

CAS: 867160-71-2

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 1550.54 现货
5mg RMB 1393.48 现货
50mg RMB 5899.91 现货
200mg RMB 13677.3 现货
1g RMB 31941 现货
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400-668-6834

info@selleck.cn

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客户使用Selleck的Linsitinib (OSI-906)发表文献185

产品质控

批次: 纯度: 99.99%
99.34

常与Linsitinib (OSI-906)一起在实验中被使用的化合物

Osimertinib (AZD9291)


Linsitinib和Osimertinib联合使用可抑制AXL低表达EGFR突变的NSCLC细胞系(包括HCC4006/HCC827/H3255细胞)的活力。

Wang R, et al. Nat Commun. 2020 Sep 14;11(1):4607.

Gefitinib


Gefitinib抑制HCC827细胞中HIF-1α和VEGF的表达,Linsitinib抑制H1975细胞中VEGF的产生。

Yeo CD, et al. Exp Lung Res. 2017 Feb;43(1):29-37.

Lapatinib


Linsitinib和Lapatinib联合使用可显着抑制裸鼠KYSE450异种移植模型中异种移植物的生长。

Kang J, et al. Int J Mol Sci. 2022 Sep 8;23(18):10382.

Afatinib


Linsitinib和Afatinib联合治疗对H1975异种移植物中的肿瘤生长显示出不仅仅是相加效应。

Lee Y, et al. Mol Carcinog. 2016 May;55(5):991-1001.

Aspirin


Linsitinib和Aspirin抑制干细胞样结肠癌细胞的生长,降低CD133/CD44/CD24的表达,并上调CDX2/PTEN的表达。

Guo Y, et al. Saudi J Biol Sci. 2022 Feb;29(2):872-877.

Linsitinib (OSI-906)相关产品

相关信号通路图

IGF-1R抑制剂选择性比较

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
HEK293 Function assay 60 mins Inhibition of full length IGF-1 receptor (unknown origin) autophosphorylation transfected in HEK293 cells pretreated for 60 mins followed by IGF-1 stimulation measured after 10 mins by quantitative Western blot analysis, IC50 = 0.0028 μM. 26951753
HEK293 Function assay 60 mins Inhibition of full length insulin receptor (unknown origin) autophosphorylation transfected in HEK293 cells pretreated for 60 mins followed by IGF-1 stimulation measured after 10 mins by quantitative Western blot analysis, IC50 = 0.016 μM. 26951753
NIH 3T3 Function assay 2 hrs Inhibition of full length human IGF-1R overexpressed in mouse NIH 3T3 cells assessed as IGF1-induced protein phosphorylation incubated for 2 hrs prior to IGF1 induction measured after 15 mins by ELISA, IC50 = 0.024 μM. 24900721
NALM-6 Growth Inhibition Assay IC50=6.3323 μM SANGER
NB6 Growth Inhibition Assay IC50=6.29622 μM SANGER
NCI-H1304 Growth Inhibition Assay IC50=6.27428 μM SANGER
NKM-1 Growth Inhibition Assay IC50=6.1671 μM SANGER
EoL-1-cell Growth Inhibition Assay IC50=6.16563 μM SANGER
SCLC-21H Growth Inhibition Assay IC50=6.10843 μM SANGER
TE-15 Growth Inhibition Assay IC50=6.06605 μM SANGER
C2BBe1 Growth Inhibition Assay IC50=5.9397 μM SANGER
TCCSUP Growth Inhibition Assay IC50=5.93259 μM SANGER
COLO-679 Growth Inhibition Assay IC50=5.88948 μM SANGER
22RV1 Growth Inhibition Assay IC50=5.80019 μM SANGER
YAPC Growth Inhibition Assay IC50=5.76201 μM SANGER
SW1710 Growth Inhibition Assay IC50=5.74751 μM SANGER
NMC-G1 Growth Inhibition Assay IC50=5.70227 μM SANGER
MHH-ES-1 Growth Inhibition Assay IC50=5.59907 μM SANGER
LB1047-RCC Growth Inhibition Assay IC50=5.55933 μM SANGER
DoTc2-4510 Growth Inhibition Assay IC50=5.45371 μM SANGER
CPC-N Growth Inhibition Assay IC50=5.39419 μM SANGER
NCI-H292 Growth Inhibition Assay IC50=5.30044 μM SANGER
PSN1 Growth Inhibition Assay IC50=5.27235 μM SANGER
CAPAN-1 Growth Inhibition Assay IC50=5.25707 μM SANGER
MCF7 Growth Inhibition Assay IC50=5.14517 μM SANGER
MOLT-16 Growth Inhibition Assay IC50=4.95253 μM SANGER
TE-441-T Growth Inhibition Assay IC50=4.90537 μM SANGER
CAL-39 Growth Inhibition Assay IC50=4.8767 μM SANGER
OVCAR-5 Growth Inhibition Assay IC50=4.81226 μM SANGER
DK-MG Growth Inhibition Assay IC50=4.80933 μM SANGER
PANC-10-05 Growth Inhibition Assay IC50=4.6984 μM SANGER
NCI-H1092 Growth Inhibition Assay IC50=4.45687 μM SANGER
LS-411N Growth Inhibition Assay IC50=4.44885 μM SANGER
LCLC-103H Growth Inhibition Assay IC50=4.32195 μM SANGER
NCI-H1648 Growth Inhibition Assay IC50=4.29819 μM SANGER
NTERA-S-cl-D1 Growth Inhibition Assay IC50=4.28615 μM SANGER
NB13 Growth Inhibition Assay IC50=4.26887 μM SANGER
BB49-HNC Growth Inhibition Assay IC50=4.15213 μM SANGER
GP5d Growth Inhibition Assay IC50=4.05362 μM SANGER
TGW Growth Inhibition Assay IC50=4.01311 μM SANGER
MZ2-MEL Growth Inhibition Assay IC50=3.92086 μM SANGER
ES8 Growth Inhibition Assay IC50=3.83877 μM SANGER
SW837 Growth Inhibition Assay IC50=3.76333 μM SANGER
SK-LU-1 Growth Inhibition Assay IC50=3.76295 μM SANGER
MS-1 Growth Inhibition Assay IC50=3.53429 μM SANGER
LU-99A Growth Inhibition Assay IC50=3.47105 μM SANGER
CAL-12T Growth Inhibition Assay IC50=3.40713 μM SANGER
A427 Growth Inhibition Assay IC50=3.25699 μM SANGER
SNU-423 Growth Inhibition Assay IC50=3.20313 μM SANGER
NCI-H747 Growth Inhibition Assay IC50=3.04992 μM SANGER
NCI-H526 Growth Inhibition Assay IC50=3.04085 μM SANGER
GI-ME-N Growth Inhibition Assay IC50=3.00565 μM SANGER
NCI-H2141 Growth Inhibition Assay IC50=2.96896 μM SANGER
RCC10RGB Growth Inhibition Assay IC50=2.95281 μM SANGER
GB-1 Growth Inhibition Assay IC50=2.93404 μM SANGER
NCI-H1623 Growth Inhibition Assay IC50=2.92024 μM SANGER
CHP-126 Growth Inhibition Assay IC50=2.76317 μM SANGER
NCI-H1882 Growth Inhibition Assay IC50=2.75227 μM SANGER
TE-10 Growth Inhibition Assay IC50=2.70838 μM SANGER
LOXIMVI Growth Inhibition Assay IC50=2.6021 μM SANGER
HCC1143 Growth Inhibition Assay IC50=2.45368 μM SANGER
CP66-MEL Growth Inhibition Assay IC50=2.29014 μM SANGER
LU-134-A Growth Inhibition Assay IC50=2.277 μM SANGER
LP-1 Growth Inhibition Assay IC50=2.25807 μM SANGER
OPM-2 Growth Inhibition Assay IC50=2.102 μM SANGER
EW-3 Growth Inhibition Assay IC50=2.09844 μM SANGER
LS-513 Growth Inhibition Assay IC50=2.05305 μM SANGER
MC-IXC Growth Inhibition Assay IC50=1.9898 μM SANGER
SK-PN-DW Growth Inhibition Assay IC50=1.91298 μM SANGER
NCI-H2171 Growth Inhibition Assay IC50=1.77716 μM SANGER
LB647-SCLC Growth Inhibition Assay IC50=1.76583 μM SANGER
LC-2-ad Growth Inhibition Assay IC50=1.73887 μM SANGER
TE-1 Growth Inhibition Assay IC50=1.70945 μM SANGER
HL-60 Growth Inhibition Assay IC50=1.66928 μM SANGER
HuH-7 Growth Inhibition Assay IC50=1.60098 μM SANGER
NCI-H1770 Growth Inhibition Assay IC50=1.51113 μM SANGER
TGBC24TKB Growth Inhibition Assay IC50=1.50193 μM SANGER
SK-MEL-3 Growth Inhibition Assay IC50=1.48556 μM SANGER
EKVX Growth Inhibition Assay IC50=1.34568 μM SANGER
L-363 Growth Inhibition Assay IC50=1.34208 μM SANGER
TE-8 Growth Inhibition Assay IC50=1.31462 μM SANGER
RD Growth Inhibition Assay IC50=1.26455 μM SANGER
CAL-85-1 Growth Inhibition Assay IC50=1.23138 μM SANGER
T84 Growth Inhibition Assay IC50=1.20914 μM SANGER
MEL-JUSO Growth Inhibition Assay IC50=1.15759 μM SANGER
IGROV-1 Growth Inhibition Assay IC50=1.15444 μM SANGER
ES3 Growth Inhibition Assay IC50=1.12297 μM SANGER
SIMA Growth Inhibition Assay IC50=1.06825 μM SANGER
SJSA-1 Growth Inhibition Assay IC50=1.03653 μM SANGER
CMK Growth Inhibition Assay IC50=0.99929 μM SANGER
SNU-387 Growth Inhibition Assay IC50=0.99393 μM SANGER
ES6 Growth Inhibition Assay IC50=0.91066 μM SANGER
ABC-1 Growth Inhibition Assay IC50=0.90352 μM SANGER
HCC2998 Growth Inhibition Assay IC50=0.88263 μM SANGER
PANC-08-13 Growth Inhibition Assay IC50=0.86377 μM SANGER
COLO-668 Growth Inhibition Assay IC50=0.84666 μM SANGER
TE-12 Growth Inhibition Assay IC50=0.76486 μM SANGER
NH-12 Growth Inhibition Assay IC50=0.76046 μM SANGER
RH-1 Growth Inhibition Assay IC50=0.74859 μM SANGER
NCI-H358 Growth Inhibition Assay IC50=0.67082 μM SANGER
SK-MM-2 Growth Inhibition Assay IC50=0.65491 μM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=0.60236 μM SANGER
NB69 Growth Inhibition Assay IC50=0.58257 μM SANGER
DOK Growth Inhibition Assay IC50=0.556 μM SANGER
SIG-M5 Growth Inhibition Assay IC50=0.53557 μM SANGER
NOS-1 Growth Inhibition Assay IC50=0.52267 μM SANGER
SJRH30 Growth Inhibition Assay IC50=0.50822 μM SANGER
A375 Growth Inhibition Assay IC50=0.47617 μM SANGER
BFTC-905 Growth Inhibition Assay IC50=0.46758 μM SANGER
NB10 Growth Inhibition Assay IC50=0.45437 μM SANGER
COLO-320-HSR Growth Inhibition Assay IC50=0.41368 μM SANGER
ES4 Growth Inhibition Assay IC50=0.41038 μM SANGER
RS4-11 Growth Inhibition Assay IC50=0.33758 μM SANGER
SNU-C1 Growth Inhibition Assay IC50=0.29313 μM SANGER
EW-11 Growth Inhibition Assay IC50=0.28432 μM SANGER
LS-1034 Growth Inhibition Assay IC50=0.27132 μM SANGER
EW-18 Growth Inhibition Assay IC50=0.27001 μM SANGER
LAN-6 Growth Inhibition Assay IC50=0.26348 μM SANGER
HT-144 Growth Inhibition Assay IC50=0.26191 μM SANGER
LB771-HNC Growth Inhibition Assay IC50=0.25915 μM SANGER
HT-29 Growth Inhibition Assay IC50=0.24248 μM SANGER
SK-N-DZ Growth Inhibition Assay IC50=0.23698 μM SANGER
NCI-H2122 Growth Inhibition Assay IC50=0.23299 μM SANGER
NCI-H650 Growth Inhibition Assay IC50=0.21384 μM SANGER
LCLC-97TM1 Growth Inhibition Assay IC50=0.20955 μM SANGER
NCI-H727 Growth Inhibition Assay IC50=0.19794 μM SANGER
EW-7 Growth Inhibition Assay IC50=0.18881 μM SANGER
EW-16 Growth Inhibition Assay IC50=0.18777 μM SANGER
G-401 Growth Inhibition Assay IC50=0.1823 μM SANGER
NCI-H1355 Growth Inhibition Assay IC50=0.18135 μM SANGER
Saos-2 Growth Inhibition Assay IC50=0.16526 μM SANGER
ML-2 Growth Inhibition Assay IC50=0.15896 μM SANGER
GDM-1 Growth Inhibition Assay IC50=0.13672 μM SANGER
ES1 Growth Inhibition Assay IC50=0.10696 μM SANGER
COLO-205 Growth Inhibition Assay IC50=0.10454 μM SANGER
HMV-II Growth Inhibition Assay IC50=0.08846 μM SANGER
EW-1 Growth Inhibition Assay IC50=0.08585 μM SANGER
TE-11 Growth Inhibition Assay IC50=0.07822 μM SANGER
KS-1 Growth Inhibition Assay IC50=0.03835 μM SANGER
A4-Fuk Growth Inhibition Assay IC50=0.02806 μM SANGER
NCI-H522 Growth Inhibition Assay IC50=6.33306 μM SANGER
MV-4-11 Growth Inhibition Assay IC50=6.37079 μM SANGER
LB2241-RCC Growth Inhibition Assay IC50=6.38667 μM SANGER
NCI-H1417 Growth Inhibition Assay IC50=6.40847 μM SANGER
HT-1197 Growth Inhibition Assay IC50=6.57122 μM SANGER
P30-OHK Growth Inhibition Assay IC50=6.6277 μM SANGER
ALL-PO Growth Inhibition Assay IC50=6.71916 μM SANGER
OVCAR-4 Growth Inhibition Assay IC50=6.75405 μM SANGER
HCC2157 Growth Inhibition Assay IC50=6.77475 μM SANGER
NCI-H838 Growth Inhibition Assay IC50=6.9649 μM SANGER
NCI-H1299 Growth Inhibition Assay IC50=6.9709 μM SANGER
SW954 Growth Inhibition Assay IC50=7.20068 μM SANGER
NCI-H441 Growth Inhibition Assay IC50=7.34065 μM SANGER
SK-MEL-2 Growth Inhibition Assay IC50=7.48373 μM SANGER
KARPAS-45 Growth Inhibition Assay IC50=7.65929 μM SANGER
CAL-54 Growth Inhibition Assay IC50=7.82977 μM SANGER
KYSE-180 Growth Inhibition Assay IC50=7.88941 μM SANGER
NCI-H187 Growth Inhibition Assay IC50=7.95947 μM SANGER
RT-112 Growth Inhibition Assay IC50=8.09677 μM SANGER
NCI-H1437 Growth Inhibition Assay IC50=8.09795 μM SANGER
SNU-449 Growth Inhibition Assay IC50=8.28272 μM SANGER
HCC1187 Growth Inhibition Assay IC50=8.29391 μM SANGER
NCI-H2030 Growth Inhibition Assay IC50=8.37714 μM SANGER
HuO-3N1 Growth Inhibition Assay IC50=8.37844 μM SANGER
COLO-792 Growth Inhibition Assay IC50=8.41527 μM SANGER
MIA-PaCa-2 Growth Inhibition Assay IC50=8.85508 μM SANGER
SK-N-FI Growth Inhibition Assay IC50=9.0425 μM SANGER
MMAC-SF Growth Inhibition Assay IC50=9.09751 μM SANGER
NCI-H28 Growth Inhibition Assay IC50=9.10469 μM SANGER
ETK-1 Growth Inhibition Assay IC50=9.29974 μM SANGER
NCI-H1993 Growth Inhibition Assay IC50=9.44261 μM SANGER
no-11 Growth Inhibition Assay IC50=9.4712 μM SANGER
ChaGo-K-1 Growth Inhibition Assay IC50=9.51583 μM SANGER
NCCIT Growth Inhibition Assay IC50=9.53169 μM SANGER
SAS Growth Inhibition Assay IC50=10.248 μM SANGER
A673 Growth Inhibition Assay IC50=10.3704 μM SANGER
NCI-H1522 Growth Inhibition Assay IC50=10.3707 μM SANGER
NCI-H810 Growth Inhibition Assay IC50=10.3907 μM SANGER
IST-MES1 Growth Inhibition Assay IC50=10.4564 μM SANGER
GR-ST Growth Inhibition Assay IC50=10.5024 μM SANGER
SUP-T1 Growth Inhibition Assay IC50=10.7317 μM SANGER
NB5 Growth Inhibition Assay IC50=10.9022 μM SANGER
MZ1-PC Growth Inhibition Assay IC50=10.9571 μM SANGER
SK-CO-1 Growth Inhibition Assay IC50=10.9931 μM SANGER
Capan-2 Growth Inhibition Assay IC50=11.3198 μM SANGER
697 Growth Inhibition Assay IC50=11.6757 μM SANGER
REH Growth Inhibition Assay IC50=11.7451 μM SANGER
GI-1 Growth Inhibition Assay IC50=11.8615 μM SANGER
BB65-RCC Growth Inhibition Assay IC50=12.0916 μM SANGER
NCI-H1651 Growth Inhibition Assay IC50=12.2478 μM SANGER
NCI-H1618 Growth Inhibition Assay IC50=12.3976 μM SANGER
NCI-H2081 Growth Inhibition Assay IC50=12.6141 μM SANGER
GCIY Growth Inhibition Assay IC50=12.7213 μM SANGER
NY Growth Inhibition Assay IC50=13.0643 μM SANGER
PANC-03-27 Growth Inhibition Assay IC50=13.0807 μM SANGER
BHY Growth Inhibition Assay IC50=13.2121 μM SANGER
SK-OV-3 Growth Inhibition Assay IC50=13.3763 μM SANGER
5637 Growth Inhibition Assay IC50=13.7759 μM SANGER
LC-1F Growth Inhibition Assay IC50=14.0356 μM SANGER
SNB75 Growth Inhibition Assay IC50=14.0383 μM SANGER
CHP-212 Growth Inhibition Assay IC50=14.0464 μM SANGER
HT-1376 Growth Inhibition Assay IC50=14.1126 μM SANGER
MONO-MAC-6 Growth Inhibition Assay IC50=14.1502 μM SANGER
CA46 Growth Inhibition Assay IC50=14.1827 μM SANGER
SCC-15 Growth Inhibition Assay IC50=14.5583 μM SANGER
ATN-1 Growth Inhibition Assay IC50=14.6627 μM SANGER
NCI-H2405 Growth Inhibition Assay IC50=14.8157 μM SANGER
NCI-H716 Growth Inhibition Assay IC50=14.8493 μM SANGER
SW620 Growth Inhibition Assay IC50=14.9014 μM SANGER
NCI-H226 Growth Inhibition Assay IC50=14.9085 μM SANGER
SW962 Growth Inhibition Assay IC50=14.9432 μM SANGER
KYSE-150 Growth Inhibition Assay IC50=14.955 μM SANGER
OCUB-M Growth Inhibition Assay IC50=14.9883 μM SANGER
ES7 Growth Inhibition Assay IC50=15.0984 μM SANGER
SW1463 Growth Inhibition Assay IC50=15.4223 μM SANGER
CAKI-1 Growth Inhibition Assay IC50=15.5346 μM SANGER
MKN28 Growth Inhibition Assay IC50=15.5479 μM SANGER
SW13 Growth Inhibition Assay IC50=15.618 μM SANGER
A3-KAW Growth Inhibition Assay IC50=15.9697 μM SANGER
LU-65 Growth Inhibition Assay IC50=15.9768 μM SANGER
Calu-1 Growth Inhibition Assay IC50=16.0368 μM SANGER
ST486 Growth Inhibition Assay IC50=16.0431 μM SANGER
BB30-HNC Growth Inhibition Assay IC50=16.1246 μM SANGER
EGI-1 Growth Inhibition Assay IC50=16.446 μM SANGER
SH-4 Growth Inhibition Assay IC50=16.4731 μM SANGER
MN-60 Growth Inhibition Assay IC50=17.2297 μM SANGER
MPP-89 Growth Inhibition Assay IC50=17.2459 μM SANGER
A2780 Growth Inhibition Assay IC50=17.4139 μM SANGER
Daoy Growth Inhibition Assay IC50=17.4695 μM SANGER
NCI-H2126 Growth Inhibition Assay IC50=17.4771 μM SANGER
NCI-H1563 Growth Inhibition Assay IC50=17.4917 μM SANGER
8-MG-BA Growth Inhibition Assay IC50=17.6648 μM SANGER
786-0 Growth Inhibition Assay IC50=17.8353 μM SANGER
AM-38 Growth Inhibition Assay IC50=17.9306 μM SANGER
COLO-824 Growth Inhibition Assay IC50=18.4436 μM SANGER
SK-MEL-30 Growth Inhibition Assay IC50=18.5082 μM SANGER
CESS Growth Inhibition Assay IC50=18.7609 μM SANGER
BL-70 Growth Inhibition Assay IC50=18.8156 μM SANGER
NCI-H2170 Growth Inhibition Assay IC50=18.9179 μM SANGER
HT-3 Growth Inhibition Assay IC50=18.983 μM SANGER
BOKU Growth Inhibition Assay IC50=19.0381 μM SANGER
HPAF-II Growth Inhibition Assay IC50=19.3015 μM SANGER
KGN Growth Inhibition Assay IC50=19.4765 μM SANGER
MC-CAR Growth Inhibition Assay IC50=19.6313 μM SANGER
BHT-101 Growth Inhibition Assay IC50=19.777 μM SANGER
SW1783 Growth Inhibition Assay IC50=19.7806 μM SANGER
KP-N-YN Growth Inhibition Assay IC50=20.0262 μM SANGER
LU-165 Growth Inhibition Assay IC50=20.5571 μM SANGER
GOTO Growth Inhibition Assay IC50=20.6451 μM SANGER
EFM-19 Growth Inhibition Assay IC50=21.0716 μM SANGER
CTV-1 Growth Inhibition Assay IC50=21.1054 μM SANGER
HEL Growth Inhibition Assay IC50=21.4216 μM SANGER
SNU-C2B Growth Inhibition Assay IC50=21.426 μM SANGER
ECC4 Growth Inhibition Assay IC50=21.707 μM SANGER
NEC8 Growth Inhibition Assay IC50=21.8368 μM SANGER
KMOE-2 Growth Inhibition Assay IC50=21.8921 μM SANGER
NCI-H524 Growth Inhibition Assay IC50=22.0808 μM SANGER
WSU-NHL Growth Inhibition Assay IC50=22.1577 μM SANGER
SF126 Growth Inhibition Assay IC50=22.2469 μM SANGER
HOP-92 Growth Inhibition Assay IC50=22.3167 μM SANGER
CTB-1 Growth Inhibition Assay IC50=22.4677 μM SANGER
KYSE-270 Growth Inhibition Assay IC50=22.9357 μM SANGER
SK-MEL-24 Growth Inhibition Assay IC50=23.187 μM SANGER
Calu-3 Growth Inhibition Assay IC50=23.2128 μM SANGER
GAMG Growth Inhibition Assay IC50=23.2367 μM SANGER
SW1573 Growth Inhibition Assay IC50=23.7415 μM SANGER
MHH-NB-11 Growth Inhibition Assay IC50=24.0194 μM SANGER
TK10 Growth Inhibition Assay IC50=24.5013 μM SANGER
LB373-MEL-D Growth Inhibition Assay IC50=24.6064 μM SANGER
KALS-1 Growth Inhibition Assay IC50=24.7327 μM SANGER
HUTU-80 Growth Inhibition Assay IC50=25.8032 μM SANGER
HuP-T3 Growth Inhibition Assay IC50=26.1674 μM SANGER
OE19 Growth Inhibition Assay IC50=26.2153 μM SANGER
J82 Growth Inhibition Assay IC50=26.2471 μM SANGER
DU-4475 Growth Inhibition Assay IC50=26.3819 μM SANGER
DMS-53 Growth Inhibition Assay IC50=26.5138 μM SANGER
COLO-741 Growth Inhibition Assay IC50=26.8344 μM SANGER
SW48 Growth Inhibition Assay IC50=26.882 μM SANGER
IGR-1 Growth Inhibition Assay IC50=26.9334 μM SANGER
639-V Growth Inhibition Assay IC50=27.0245 μM SANGER
LK-2 Growth Inhibition Assay IC50=27.4141 μM SANGER
NCI-H2347 Growth Inhibition Assay IC50=27.9699 μM SANGER
NCI-H2228 Growth Inhibition Assay IC50=28.0905 μM SANGER
LS-123 Growth Inhibition Assay IC50=28.1262 μM SANGER
U031 Growth Inhibition Assay IC50=28.252 μM SANGER
NCI-H1792 Growth Inhibition Assay IC50=28.4721 μM SANGER
NCI-H2087 Growth Inhibition Assay IC50=28.7552 μM SANGER
NCI-H2342 Growth Inhibition Assay IC50=29.5208 μM SANGER
SW626 Growth Inhibition Assay IC50=29.756 μM SANGER
LB2518-MEL Growth Inhibition Assay IC50=29.815 μM SANGER
RXF393 Growth Inhibition Assay IC50=30.0952 μM SANGER
LC4-1 Growth Inhibition Assay IC50=30.3092 μM SANGER
NCI-H1694 Growth Inhibition Assay IC50=30.6624 μM SANGER
K5 Growth Inhibition Assay IC50=30.9702 μM SANGER
HDLM-2 Growth Inhibition Assay IC50=30.9725 μM SANGER
BCPAP Growth Inhibition Assay IC50=31.8379 μM SANGER
BC-3 Growth Inhibition Assay IC50=32.1403 μM SANGER
LB996-RCC Growth Inhibition Assay IC50=32.2358 μM SANGER
NCI-H2009 Growth Inhibition Assay IC50=32.4981 μM SANGER
HTC-C3 Growth Inhibition Assay IC50=33.7519 μM SANGER
LAMA-84 Growth Inhibition Assay IC50=34.4407 μM SANGER
CCRF-CEM Growth Inhibition Assay IC50=34.5715 μM SANGER
AN3-CA Growth Inhibition Assay IC50=35.0568 μM SANGER
NCI-H1734 Growth Inhibition Assay IC50=35.2561 μM SANGER
Ca-Ski Growth Inhibition Assay IC50=35.4101 μM SANGER
U-266 Growth Inhibition Assay IC50=35.6114 μM SANGER
SBC-5 Growth Inhibition Assay IC50=35.7781 μM SANGER
GT3TKB Growth Inhibition Assay IC50=37.115 μM SANGER
MDA-MB-175-VII Growth Inhibition Assay IC50=37.2248 μM SANGER
PFSK-1 Growth Inhibition Assay IC50=37.2435 μM SANGER
IMR-5 Growth Inhibition Assay IC50=37.2487 μM SANGER
Daudi Growth Inhibition Assay IC50=37.3597 μM SANGER
A498 Growth Inhibition Assay IC50=37.7218 μM SANGER
SCC-4 Growth Inhibition Assay IC50=37.7843 μM SANGER
COLO-680N Growth Inhibition Assay IC50=38.2885 μM SANGER
SK-MES-1 Growth Inhibition Assay IC50=38.3215 μM SANGER
SR Growth Inhibition Assay IC50=38.5495 μM SANGER
LNCaP-Clone-FGC Growth Inhibition Assay IC50=38.5637 μM SANGER
SK-HEP-1 Growth Inhibition Assay IC50=38.7822 μM SANGER
BPH-1 Growth Inhibition Assay IC50=38.8329 μM SANGER
NCI-H1755 Growth Inhibition Assay IC50=39.5817 μM SANGER
LXF-289 Growth Inhibition Assay IC50=39.8084 μM SANGER
SW1088 Growth Inhibition Assay IC50=40.2107 μM SANGER
MOLT-4 Growth Inhibition Assay IC50=40.2901 μM SANGER
AsPC-1 Growth Inhibition Assay IC50=40.4583 μM SANGER
HOP-62 Growth Inhibition Assay IC50=40.6568 μM SANGER
A172 Growth Inhibition Assay IC50=40.8511 μM SANGER
SN12C Growth Inhibition Assay IC50=40.9385 μM SANGER
MDA-MB-231 Growth Inhibition Assay IC50=40.9898 μM SANGER
RPMI-2650 Growth Inhibition Assay IC50=41.1593 μM SANGER
KYSE-140 Growth Inhibition Assay IC50=41.8123 μM SANGER
KINGS-1 Growth Inhibition Assay IC50=42.4697 μM SANGER
HSC-3 Growth Inhibition Assay IC50=42.6661 μM SANGER
PC-14 Growth Inhibition Assay IC50=43.1882 μM SANGER
COR-L105 Growth Inhibition Assay IC50=43.6502 μM SANGER
BE-13 Growth Inhibition Assay IC50=44.2371 μM SANGER
NCI-H661 Growth Inhibition Assay IC50=44.2958 μM SANGER
IST-MEL1 Growth Inhibition Assay IC50=44.3599 μM SANGER
HCC1806 Growth Inhibition Assay IC50=44.5873 μM SANGER
COLO-800 Growth Inhibition Assay IC50=44.8453 μM SANGER
IST-SL2 Growth Inhibition Assay IC50=45.1247 μM SANGER
8305C Growth Inhibition Assay IC50=45.309 μM SANGER
UACC-62 Growth Inhibition Assay IC50=46.2875 μM SANGER
COR-L23 Growth Inhibition Assay IC50=47.199 μM SANGER
EFE-184 Growth Inhibition Assay IC50=47.388 μM SANGER
DMS-114 Growth Inhibition Assay IC50=47.4149 μM SANGER
KYSE-520 Growth Inhibition Assay IC50=48.5315 μM SANGER
SNG-M Growth Inhibition Assay IC50=49.434 μM SANGER
A2058 Growth Inhibition Assay IC50=49.4885 μM SANGER
Ba/F3 Function assay Inhibition of full length IGF-1 receptor (unknown origin) transfected in Ba/F3 cells assessed as cell proliferation, IC50 = 0.0076 μM. 26951753
A431 Function assay Inhibition of IGF1R intracellular phosphorylation in human A431 cells by ELISA, IC50 = 0.018 μM. 20346655
3T3 Function assay Inhibition of human IGF1R expressed in mouse 3T3 cells by ELISA based assay, IC50 = 0.024 μM. 21251824
Ba/F3 Function assay Inhibition of full length insulin receptor (unknown origin) transfected in Ba/F3 cells assessed as cell proliferation, IC50 = 0.126 μM. 26951753
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
点击查看更多细胞系数据

生物活性

产品描述 Linsitinib (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。Phase 3。
靶点
IGF-1R [1]
(Cell-free assay)
Insulin Receptor [1]
(Cell-free assay)
IRR [1]
(Cell-free assay)
35 nM 75 nM 75 nM
体外研究(In Vitro)
体外研究活性 OSI-906 抑制IGF-IR自磷酸化和下游信号蛋白AKT, ERK1/2和S6激酶的激活,IC50为0.028到 0.13 μM。OSI-906通过与C-螺旋相互作用而使靶点蛋白形成中间结构形态。OSI-906作用于肝脏微粒体,具有良好的代谢稳定性。OSI-906浓度为1μM时,完全抑制IR 和IGF-IR磷酸化。OSI-906抑制一些肿瘤细胞系增殖,包括非小细胞肺癌和结肠直肠癌(CRC)肿瘤细胞系,EC50为0.021到 0.810 μM。[1]
激酶实验 蛋白激酶生化实验
通过以ELISA为基础的检测法(IGF-IR, IR, EGFR 和 KDR)或使用100 µM ATP的放射检测法进行蛋白激酶检测实验。在内部ELISA检测实验中,使用聚 (Glu:Tyr)作为底物,结合到96孔实验板表面,使用辣根过氧化物酶标记的自磷酸化抗体测定磷酸化。使用ABTS作为过氧化物酶底物,通过在405/490 nm处测量吸光度而测定结合的抗体。所有实验使用纯化的重组激酶催化域。在昆虫细胞中,人类IGF-IR或EGFR的重组酶表达作为NH2-末端谷胱甘肽S-转移酶融合蛋白,且在内部纯化。通过抑制百分数对log10药品浓度的S型剂量-反应曲线测定IC50值。进行内部实验需重复进行实验,除非另有说明,取三次测量的最小值。
细胞实验 细胞系 MCF7, NCI-H292, Colo-205, HT29, H358, H1703, BxPC3, A673, SW620, DU4475, HepG2 和Hepa-1, RKO 3T3/hulGF-IR, H292 细胞
浓度 0.02-0.8 μM
孵育时间 3天
方法 为了测定细胞增殖,细胞接种在含FCS 10%的合适培养基上,在不同浓度OSI-906存在时,温育3天。通过细胞内ATP含量的荧光量化,使用CellTiterGlo测定抑制细胞生长的情况。数据作为衡量最大增殖的一部分,通过在不同浓度 OSI-906存在时的细胞密度除以对照组(只用DMSO处理)细胞密度。
实验图片 检测方法 检测指标 实验图片 PMID
Western blot p-EGFR / EGFR / p-IGF1R / IGF1R / p-IRS1 / IRS1 / p-ERK / ERK / p-AKT / AKT p-IGF1R / IGF1R / p-mTOR / mTOR cleaved caspase-3 / cleaved PARP pSrc(Y416) / Src p-STAT3(Y705) / STAT3 pS6 / S6 26052929
Immunofluorescence FoxO1 27535223
Growth inhibition assay Cell viability 26136493
体内研究(In Vivo)
体内研究活性 OSI-906 作用于IGF-IR驱动的移植瘤鼠模型,抑制肿瘤生长,按 75 mg / kg剂量处理,导致100% TGI和 55% 衰退,按25 mg/kg剂量处理,导致 60% TGI,没有衰退。OSI-906处理犬,大鼠和小鼠,诱导不同的消除半衰期,消除半衰期分别为1.18 小时, 2.64小时 和2.14小时。OSI-906按不同剂量单独处理给药雌性Sprague-Dawley 大鼠和雌性CD-1小鼠,每天一次,Vmax值与OSI-906 剂量不成比例。OSI-906 按 25 mg/kg剂量处理12天,提高血糖值。OSI-906按75 mg/kg 剂量单独处理IGF-IR-驱动的人全长人类IGF-IR (LISN)移植鼠模型,在4 和24小时间最大程度抑制IGF-IR磷酸化(80%),血浆药物浓度为26.6-4.77 μM。[1] OSI-906 按60 mg/kg剂量单独作用于NCI-H292 移植鼠,处理2,4,24小时,抑制糖吸收。OSI-906 作用于NCI-H292移植鼠模型,抑制肿瘤生长。[2]
动物实验 Animal Models IGF-IR驱动的全长人类IGF-IR (LISN) 移植小鼠模型
Dosages 25 mg/kg和75 mg/kg
Administration 口服处理,每天一次,持续14天
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02546544 Completed
Relapsed Ewing Sarcoma|Refractory Ewing Sarcoma
University of Oxford|European Organisation for Research and Treatment of Cancer - EORTC|European Commission|Astellas Pharma Inc|Oxford University Hospitals NHS Trust
March 2014 Phase 2
NCT01672736 Terminated
Multiple Myeloma
University Health Network Toronto|Multiple Myeloma Research Consortium|Astellas Pharma Inc
September 2012 Phase 1|Phase 2
NCT01529684 Completed
Advanced Solid Tumors|Pharmacokinetics of 14C-OSI-906
Astellas Pharma Global Development Inc.|Astellas Pharma Inc
March 19 2012 Phase 1
NCT01221077 Completed
NSCLC|Non Small Cell Lung Cancer
Astellas Pharma Inc
April 8 2011 Phase 2

化学信息&溶解度

分子量 421.49 分子式

C26H23N5O

CAS号 867160-71-2 SDF Download Linsitinib (OSI-906) SDF
Smiles CC1(CC(C1)C2=NC(=C3N2C=CN=C3N)C4=CC5=C(C=C4)C=CC(=N5)C6=CC=CC=C6)O
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 84 mg/mL ( 199.29 mM; DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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常见问题及建议解决方法

问题 1:
Does the inhibitor dissolve in the vehicle (30% PEG400/0.5%Tween 80/5% propylene glycol) or is it a suspension?

回答:
OSI-906 in 30% PEG400/0.5%Tween 80/5% propylene glycol is a suspension.

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