CGP77675

Modify Date: 2024-01-14 12:07:48

CGP77675 Structure
CGP77675 structure
 Common Name CGP77675
CAS Number 234772-64-6 Molecular Weight 443.54100
Density N/A Boiling Point N/A
Molecular Formula C26H29N5O2 Melting Point N/A
MSDS USA Flash Point N/A

 Use of CGP77675


CGP77675 is a potent inhibitor of Src family kinases. CGP77675 inhibits Src, EGFR, KDR, v-Abl, and Lck with IC50s of 0.02, 0.15, 1.0, 0.31, and 0.29 μM, respectively. Anticancer activity[1].

 Names

Name 1-[2-[4-[4-amino-5-(3-methoxyphenyl)pyrrolo[2,3-d]pyrimidin-7-yl]phenyl]ethyl]piperidin-4-ol
Synonym More Synonyms

 CGP77675 Biological Activity

Description CGP77675 is a potent inhibitor of Src family kinases. CGP77675 inhibits Src, EGFR, KDR, v-Abl, and Lck with IC50s of 0.02, 0.15, 1.0, 0.31, and 0.29 μM, respectively. Anticancer activity[1].
Related Catalog
Target

IC50: 0.02 μM (Src), 0.15 μM (EGFR), 1.0 μM (KDR), 0.31 μM (v-Abl), 0.29 μM (Lck)[1]

In Vitro CGP77675 inhibits phosphorylation of peptide substrates and autophosphorylation of purified Src (IC50s of 5-20 and 40 nM, respectively) [1]. CGP77675 dose dependently inhibits phosphorylation of poly-Glu-Tyr with an IC50 value of 5.5 nM, and of the optimal Src substrate (OSS) peptide with an IC50 value of 16.7 nM. These IC50 values are similar to the value obtained with chicken Src (20 nM)[1]. CGP77675 inhibits the parathyroid hormone-induced bone resorption in rat fetal long bone cultures with an IC50 of 0.8μM[1]. CGP77675 (0.04-10 μM; 2 hours) potently inhibits tyrosine phosphorylation of the Src substrates Fak and paxillin, but has much less effect on Src (IC50 values 0.2, 0.5, and 5.7μM) in IC8.1 cells[1]. Cell Viability Assay[1] Cell Line: MC3T3-E1 cells Concentration: 0.2, 1, and 5 μM Incubation Time: 3 days Result: Did not influence cell viability for up to 3 days of treatment. Western Blot Analysis[1] Cell Line: Src-overexpressing IC8.1 cells Concentration: 0.04, 0.2, 1, 5, and 10 μM Incubation Time: 2 hours Result: Dose dependently inhibited phosphorylation of Fak and paxillin, but not of Src.
In Vivo CGP77675 (1, 5, and 25 mg/kg; injected s.c.; twice a day) inhibits IL-1b-induced hypercalcemia in Mice[1]. CGP77675 (10 and 50 mg/kg; administered orally; twice a day for 6 weeks) partially prevents bone loss and rescues bone microarchitectural features in young ovx rats[1]. Animal Model: Male mice (Tif:MAGf; Novartis Animal Farm) of 25-30 g body[1] Dosage: 1, 5, and 25 mg/kg Administration: Injected s.c.; twice a day Result: Prevented IL-1b-induced hypercalcemia in mice without affecting serum amyloid protein levels. Animal Model: Eight-week-old (175-209 g) female rats of the Sprague-Dawley-derived strain Tif:RAlf[1] Dosage: 10 and 50 mg/kg Administration: Administered orally; twice a day for 6 weeks Result: Partly prevented bone loss.
References

[1]. 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.

 Chemical & Physical Properties

Molecular Formula C26H29N5O2
Molecular Weight 443.54100
Exact Mass 443.23200
PSA 89.43000
LogP 4.19660
Appearance of Characters powder,white to beige
Storage condition 2-8°C
Water Solubility DMSO: >10mg/mL

 Safety Information

RIDADR NONH for all modes of transport
WGK Germany 3

 Articles2

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 Synonyms

unii-eqh27e0wrv
CGP77675
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Chemsrc provides CGP77675(CAS#:234772-64-6) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of CGP77675 are included as well.>> amp version: CGP77675

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