GSK1904529A
- Product Name
- GSK1904529A
- CAS No.
- 1089283-49-7
- Chemical Name
- GSK1904529A
- Synonyms
- CS-29;GSK 4529;GSK1904529A;GSK1904529A, >=98%;GSK1904529A ,S1093;GSK1904529A (GSK-4529;IGF-IR, IGF-IIR inhibitor;GSK1904529A, 10 mM in DMSO;IGF-1R inhibitor GS1904529A;GSK1904529A ISO 9001:2015 REACH
- CBNumber
- CB92501005
- Molecular Formula
- C44H47F2N9O5S
- Formula Weight
- 851.96
- MOL File
- 1089283-49-7.mol
GSK1904529A Property
- Density
- 1.39
- storage temp.
- Store at -20°C
- solubility
- ≥42.6 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
- form
- solid
- pka
- 11.12±0.70(Predicted)
- color
- Light yellow to yellow
- InChIKey
- MOSKATHMXWSZTQ-UHFFFAOYSA-N
- SMILES
- C(NC1=C(F)C=CC=C1F)(=O)C1=CC(C2=C(C3C=CN=C(NC4=CC(CC)=C(N5CCC(N6CCN(S(C)(=O)=O)CC6)CC5)C=C4OC)N=3)N3C(=N2)C=CC=C3)=CC=C1OC
N-Bromosuccinimide Price
- Product number
- SML3675
- Product name
- GSK1904529A
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $145.35
- Updated
- 2025/07/31
- Product number
- SML3675
- Product name
- GSK1904529A
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $616
- Updated
- 2025/07/31
- Product number
- 29155
- Product name
- GSK1904529A
- Packaging
- 5mg
- Price
- $116
- Updated
- 2024/03/01
- Product number
- 29155
- Product name
- GSK1904529A
- Packaging
- 25mg
- Price
- $456
- Updated
- 2024/03/01
- Product number
- 29155
- Product name
- GSK1904529A
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
GSK1904529A Chemical Properties,Usage,Production
Uses
A selective inhibitor of IGF-1R and IR with IC50s of 27 nM and 25 nM, respectively.
Uses
GSK 1904529A is a small-molecule inhibitor of the insulin-like growth factor-I receptor tyrosine kinase.
Definition
ChEBI: N-(2,6-difluorophenyl)-5-[3-[2-[5-ethyl-2-methoxy-4-[4-(4-methylsulfonyl-1-piperazinyl)-1-piperidinyl]anilino]-4-pyrimidinyl]-2-imidazo[1,2-a]pyridinyl]-2-methoxybenzamide is a member of benzamides.
Biological Activity
gsk1904529a is a small-molecule inhibitor of the insulin-like growth factor-i receptor (igf-ir) with ic50 value of 27 nm 1.gsk1904529a is a reversible and atp-competitive inhibitor with ki value of 1.6 nm. in nih-3t3/lisn cells, gsk1904529a potently inhibited phosphorylation of igf-ir with ic50 value of 22 nm. it also demonstrated to be a selective inhibitor since it showed poor inhibitory activity against 45 other serine/threonine and tyrosine kinases. when treated with whole-cell extracts, gsk1904529a significantly inhibited the ligand-induced phosphorylation of igf-ir and decreased phosphorylation of downstream signaling including akt, irs-1 and erk at concentrations > 0.01μm. gsk1904529a suppressed cell proliferation in a variety of tumor cells. the ic50 values for nci-h929, tc-71, sk-n-mc, colo 205, mcf7 and prec are 81, 35, 43, 124, 137 and 68 nm, respectively. in colo 205, mcf-7, and nci-h929 cells, gsk1904529a treatment resulted in cell accumulation in g1 and decrease in s and g2-m phases. moreover, in nih-3t3/lisn xenograft model, once daily administration of gsk1904529a at 30 mg/kg inhibited 56% of tumor growth 1.
in vivo
GSK1904529A (30 mg/kg; p.o. once or twice daily for 21 d) has antitumor activity in mice[1].
GSK1904529A (1-30 mg/kg; a single p.o.) decreases IGF-I-induced IGF-IR phosphorylation in a dose-dependent manner in mice[1].
GSK1904529A (30 mg/kg; p.o. once or twice daily for 21 d) has no significant alterations in the blood glucose levels in mice[1].
| Animal Model: | Female athymic nu/nu CD-1 mice are bring NIH-3T3/LISN tumor[1] |
| Dosage: | 30 mg/kg |
| Administration: | P.o. once or twice daily for 21 d |
| Result: | Resulted in 56% (once daily) and 98% (twice daily) inhibition of tumor growth. No significant decrease in body weight on the once-daily schedule. Observed 11-13% of body weight loss, and recovered to near baseline 6 days after the cessation of treatment in twice-daily group. |
target
IGF1R
References
1. sabbatini p, rowand j l, groy a, et al. antitumor activity of gsk1904529a, a small-molecule inhibitor of the insulin-like growth factor-i receptor tyrosine kinase. clinical cancer research, 2009, 15(9): 3058-3067.
GSK1904529A Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from GSK1904529A manufacturers
- Product
- GSK1904529A 1089283-49-7
- Price
- US $1.10/g
- Min. Order
- 1g
- Purity
- 99.0% min
- Supply Ability
- 100 tons min
- Release date
- 2021-05-12