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1089283-49-7

gsk 1904529a

CAS: 1089283-49-7

Molecular Formula: C44H47F2N9O5S

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1089283-49-7 - Names and Identifiers

Name gsk 1904529a
Synonyms CS-29
gsk 4529
GSK 4529
GSK1904529A
GSK-1904529A
GSK 1904529A
gsk 1904529a
N-(2,6-difluorophenyl)-5-(3-(2-(5-ethyl-2-methoxy-4-(4-(4-(methylsulfonyl)piperazin-1-yl)piperidin-1-yl)phenylamino)pyrimidin-4-yl)H-imidazo[1,2-a]pyridin-2-yl)-2-methoxybenzamide
N-(2,6-Difluorophenyl)-5-[3-[2-[[5-ethyl-2-(methyloxy)-4-[4-[4-(methylsulfonyl)-1-piperazinyl]-1-piperidinyl]phenyl]amino]-4-pyrimidinyl]imidazo[1,2-a]pyridin-2-yl]-2-(methyloxy)benzamide
n-(2,6-difluorophenyl)-5-(3-(2-((5-ethyl-2-(methyloxy)-4-(4-(4-(methylsulfonyl)-1-piperazinyl)-1-piperidinyl)phenyl)amino)-4-pyrimidinyl)imidazo(1,2-a)pyridin-2-yl)-2-(methyloxy)benzamide
N-(2,6-Difluorophenyl)-5-[3-[2-[[5-ethyl-2-(methyloxy)-4-[4-[4-(methylsulfonyl)-1-piperazinyl]-1-piperidinyl]phenyl]amino]-4-pyrimidinyl]imidazo[1,2-a]pyridin-2-yl]-2-(methyloxy)benzamide GSK 1904529A
CAS 1089283-49-7
InChI InChI=1S/C44H47F2N9O5S/c1-5-28-26-35(38(60-3)27-36(28)53-19-15-30(16-20-53)52-21-23-54(24-22-52)61(4,57)58)49-44-47-17-14-34(48-44)42-40(50-39-11-6-7-18-55(39)42)29-12-13-37(59-2)31(25-29)43(56)51-41-32(45)9-8-10-33(41)46/h6-14,17-18,25-27,30H,5,15-16,19-24H2,1-4H3,(H,51,56)(H,47,48,49)

1089283-49-7 - Physico-chemical Properties

Molecular FormulaC44H47F2N9O5S
Molar Mass851.96
Density1.39
pKa11.12±0.70(Predicted)
Storage Condition-20℃
In vitro studyGSK1904529A is a selective inhibitor with IC50 of 27 and 25 nM for IGF-IR and IR, respectively. GSK1904529A is a reversible ATP competitive inhibitor. The K I values for GSK1904529A at IGF-IR and IR were 1.3 and 1.6 nM, respectively. GSK1904529A effectively inhibited IGF-IR and IR phosphorylation at concentrations greater than 0.01 μm and subsequently blocked downstream signaling. Cell Proliferation experiments showed that GSK1904529A effectively inhibited NIH-3T3/LISN, TC-71, SK-N-MC, SK-ES, and RD-ES cells with IC50 of 60, 35, 43, 61, and 62 nM, respectively. GSK1904529A also inhibits other multiple myeloma and Ewing's sarcoma cell lines, including NCI-H929, MOLP-8, LP-1, and KMS-12-BM, among others.
In vivo studyMice carrying NIH-3T3/LISN tumor were treated orally with 30mg GSK1904529A per kilogram of body weight twice a day, and the tumor inhibition rate was 98%, treatment once a day showed a tumor inhibition rate of 75%. GSK1904529A can be used to treat a variety of IGF-IR-dependent tumors, including prostate, colon, breast, pancreatic, ovarian, and sarcoma.

1089283-49-7 - Preparation solution concentration reference

 1mg5mg10mg
1 mM1.174 ml5.869 ml11.738 ml
5 mM0.235 ml1.174 ml2.348 ml
10 mM0.117 ml0.587 ml1.174 ml
5 mM0.023 ml0.117 ml0.235 ml
Last Update：2024-01-02 23:10:35

1089283-49-7 - Reference Information

biological activity GSK1904529A (GSK 4529) is a selective IGF-1R and IR inhibitor. in the cell-free test, IC50 is 27 nM and 25 nM respectively, acting on IGF-1R/InsR ratio acting on Akt1/2/, Aurora A/B,B-Raf, CDK2, EGFR and other selectivity is more than 100 times higher.
target TargetValue Insulin Receptor (Cell-free assay) 25 nM IGF-1R (Cell-free assay) 27 nM
TargetValue
Insulin Receptor (Cell-free assay) 25 nM
IGF-1R (Cell-free assay) 27 nM
in vitro study GSK1904529A are selective inhibitors, and IC50 is 27 and 25 nM respectively when acting on IGF-IR and IR. GSK1904529A is a reversible ATP competitive inhibitor. When the GSK1904529A acts on IGF-IR and IR, the K I values are 1.3 and 1.6 nM respectively. GSK1904529A concentrations greater than 0.01 μM effectively inhibit IGF-IR and IR phosphorylation, and then block downstream signals. Cell proliferation experiments showed that GSK1904529A effectively inhibited NIH-3T3/LISN, TC-71, SK-N-MC, SK-ES, and RD-ES cells with IC50 of 60, 35, 43, 61, and 62 nM respectively. GSK1904529A also inhibits other multiple myeloma and Ewing's sarcoma cell lines, including NCI-H929, MOLP-8, LP-1, and KMS-12-BM.
in vivo study mice carrying NIH-3T3/LISN tumors were orally treated with 30mg of GSK1904529A per kilogram according to their body weight twice a day, and the results showed that the tumor inhibition rate was 98%. However, GSK1904529A acts on mice carrying COLO 205 transplanted tumors and is treated once a day, the results showed that the tumor inhibition rate was 75%. GSK1904529A can be used to treat a variety of IGF-IR-dependent tumors, including prostate cancer, colon cancer, breast cancer, pancreatic cancer, ovarian cancer, and sarcoma.
Last Update：2024-04-09 21:49:45
1089283-49-7
Supplier List
Shanghai Yuanye Bio-Technology Co., Ltd.
Product Name: GSK1904529A Visit Supplier Webpage Request for quotation
CAS: 1089283-49-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409 Click to send a QQ message
Wechat: 18301782025
Shanghai Yuanye Bio-Technology Co., Ltd.
Product Name: GSK1904529A Visit Supplier Webpage Request for quotation
CAS: 1089283-49-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409 Click to send a QQ message
Wechat: 18301782025
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1089283-49-7
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