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CGP77675

🥰Excellent
Catalog No. T30855Cas No. 234772-64-6
Alias ZINC1488120, CGP-77675, CGP 77675, 1-(4-(4-amino-5-(3-methoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)phenethyl)piperidin-4-ol

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.

CGP77675

CGP77675

🥰Excellent
Purity: 98.23%
Catalog No. T30855Alias ZINC1488120, CGP-77675, CGP 77675, 1-(4-(4-amino-5-(3-methoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)phenethyl)piperidin-4-olCas No. 234772-64-6
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.
Pack SizePriceAvailabilityQuantity
1 mg$43In Stock
2 mg$64In Stock
5 mg$113In Stock
10 mg$183In Stock
25 mg$372In Stock
50 mg$597In Stock
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Purity:98.23%
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Product Introduction

Bioactivity
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), Src:0.02 μM (IC50), v-ABL:0.31 μM (IC50), Lck:0.29 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].
AliasZINC1488120, CGP-77675, CGP 77675, 1-(4-(4-amino-5-(3-methoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)phenethyl)piperidin-4-ol
Chemical Properties
Molecular Weight443.54
FormulaC26H29N5O2
Cas No.234772-64-6
SmilesNC1=C2C(=CN(C2=NC=N1)C3=CC=C(CCN4CCC(O)CC4)C=C3)C5=CC(OC)=CC=C5
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 55 mg/mL (124 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.2546 mL11.2729 mL22.5459 mL112.7294 mL
5 mM0.4509 mL2.2546 mL4.5092 mL22.5459 mL
10 mM0.2255 mL1.1273 mL2.2546 mL11.2729 mL
20 mM0.1127 mL0.5636 mL1.1273 mL5.6365 mL
50 mM0.0451 mL0.2255 mL0.4509 mL2.2546 mL
100 mM0.0225 mL0.1127 mL0.2255 mL1.1273 mL

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