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CGP77675

Catalog No. T30855   CAS 234772-64-6
Synonyms: CGP-77675, 1-(4-(4-amino-5-(3-methoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)phenethyl)piperidin-4-ol, ZINC1488120, CGP 77675

CGP77675 (ZINC1488120) is a potent and selective inhibitor of Src family kinase with IC50s of 5-20 and 40 nM for the phosphorylation of peptide substrates and autophosphorylation of purified Src. CGP77675 exhibits anticancer activity.

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CGP77675 Chemical Structure
CGP77675, CAS 234772-64-6
Pack Size Availability Price/USD Quantity
1 mg In stock $ 43.00
2 mg In stock $ 64.00
5 mg In stock $ 113.00
10 mg In stock $ 183.00
25 mg In stock $ 372.00
50 mg In stock $ 597.00
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Purity: 98.23%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description CGP77675 (ZINC1488120) is a potent and selective inhibitor of Src family kinase with IC50s of 5-20 and 40 nM for the phosphorylation of peptide substrates and autophosphorylation of purified Src. CGP77675 exhibits anticancer activity.
Targets&IC50 EGFR:0.15 μM (IC50), KDR:1.0 μM (IC50), v-Abl:0.31 μM (IC50), Lck:0.29 μM (IC50), Src:0.02 μM (IC50)
In vitro CGP77675 inhibits Src, EGFR, KDR, v-Abl, and Lck with IC50s of 20, 150, 1000, 310, and 290 nM, respectively. CGP77675 dose-dependently inhibits phosphorylation of poly-Glu-Tyr (IC50 = 5.5 nM), and of the optimal Src substrate (OSS) peptide (IC50 = 16.7 nM). In rat fetal long bone cultures, CGP77675 inhibits the parathyroid hormone-induced bone resorption (IC50 = 0.8 μM). In Src-overexpressing IC8.1 cells, CGP77675 (0.04-10 μM) dose-dependently inhibits phosphorylation of Fak (IC50 = 0.2 μM) and paxillin(IC50 = 0.5 μM), but not of Src(IC50 = 5.7μM)[3].
In vivo In female rats of the Sprague-Dawley-derived strain Tif:RAlf, CGP77675 (10 and 50 mg/kg;orally) partially prevents bone loss and rescues bone microarchitectural features. In male mice, CGP77675 (1, 5, and 25 mg/kg; s.c.) inhibits IL-1β-induced hypercalcemia without affecting serum amyloid protein levels[3].
Synonyms CGP-77675, 1-(4-(4-amino-5-(3-methoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)phenethyl)piperidin-4-ol, ZINC1488120, CGP 77675
Molecular Weight 443.54
Formula C26H29N5O2
CAS No. 234772-64-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 25 mg/mL (56.4 mM), sonification/heating is recommended.

TargetMolReferences and Literature

1. Breitenlechner CB, et al. Crystal structures of active SRC kinase domain complexes. J Mol Biol. 2005 Oct 21;353(2):222-31. 2. Zhang Q, et al. Inhibition of Src kinases combined with CD40 ligand blockade prolongs murine cardiac allograft survival. Transplantation. 2005 Oct 27;80(8):1112-20. 3. Missbach M, et al. A novel inhibitor of the tyrosine kinase Src suppresses phosphorylation of its major cellularsubstrates and reduces bone resorption in vitro and in rodent models in vivo. Bone. 1999 May;24(5):437-49.

Related compound libraries

This product is contained In the following compound libraries:
Tyrosine Kinase Inhibitor Library Anti-Cancer Active Compound Library Anti-Cancer Compound Library Bioactive Compound Library Anti-Ovarian Cancer Compound Library Cytoskeletal Signaling Pathway Compound Library Anti-Pancreatic Cancer Compound Library Anti-Cancer Metabolism Compound Library Anti-Cardiovascular Disease Compound Library Anti-Prostate Cancer Compound Library

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Keywords

CGP77675 234772-64-6 Angiogenesis Cytoskeletal Signaling JAK/STAT signaling Tyrosine Kinase/Adaptors Src Bcr-Abl VEGFR EGFR CGP-77675 1-(4-(4-amino-5-(3-methoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)phenethyl)piperidin-4-ol ZINC1488120 ZINC 1488120 CGP 77675 ZINC-1488120 inhibitor inhibit

 

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