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PKI-166
CAS No. 187724-61-4
PKI-166( —— )
Catalog No. M33468 CAS No. 187724-61-4
PKI-166 is an oral inhibitor of EGF-R tyrosine kinase (IC50:0.7 nM) that is both effective and selective. PKI-166 can effectively inhibit the growth and metastasis of various human cancer cells including pancreatic cancer.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 76 | In Stock |
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| 2MG | 33 | In Stock |
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| 5MG | 69 | In Stock |
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| 10MG | 113 | In Stock |
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| 25MG | 226 | In Stock |
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| 50MG | 369 | In Stock |
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| 100MG | 591 | In Stock |
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| 200MG | 792 | In Stock |
|
| 500MG | Get Quote | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
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Product NamePKI-166
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NoteResearch use only, not for human use.
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Brief DescriptionPKI-166 is an oral inhibitor of EGF-R tyrosine kinase (IC50:0.7 nM) that is both effective and selective. PKI-166 can effectively inhibit the growth and metastasis of various human cancer cells including pancreatic cancer.
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DescriptionPKI-166 is a potent, selective and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 0.7 nM.
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In VitroPretreatment with PKI-166 (0-0.5 μM; 1 hour) inhibits EGFR autophosphorylation in human pancreatic cancer cells.PKI-166 (0.03μ M; 6 days) enhanced the cytotoxicity mediated by gemcitabine.:Western Blot Analysis Cell Line:L3.6pl cells Concentration:0.01 μM, 0.05 μM, 0.5 μM Incubation Time:1 hour Result:Inhibited EGFR autophosphorylation in a dose-dependent manner.Cell Cytotoxicity Assay Cell Line:L3.6pl cells Concentration: 0.03 μM Incubation Time:6 days Result:Enhanced the cytotoxicity mediated by gemcitabine.
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In VivoPKI-166 (100 mg/kg; p.o.; daily; day 7-day 35 after xenograft) inhibits of pancreatic cancer growth.Animal Model:Male athymic nude mice with L3.6pl cells xenograft (8–12 weeks)Dosage:100 mg/kg Administration:Oral administration; daily; from day 7 to day 35 after xenograft Result:Significantly decreased median tumor volume.
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Synonyms——
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PathwayAngiogenesis
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TargetVEGFR
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RecptorVEGFR
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Research Area——
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Indication——
Chemical Information
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CAS Number187724-61-4
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Formula Weight330.38
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Molecular FormulaC20H18N4O
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : ≥ 125 mg/mL (378.35 mM )
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SMILESC[C@@H](Nc1ncnc2[nH]c(cc12)-c1ccc(O)cc1)c1ccccc1
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Bruns CJ, et al. Blockade of the epidermal growth factor receptor signaling by a novel tyrosine kinase inhibitor leads to apoptosis of endothelial cells and therapy of human pancreatic carcinoma. Cancer Res. 2000 Jun 1;60(11):2926-35.?
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