PKI 166
- Product Name
- PKI 166
- CAS No.
- 187724-61-4
- Chemical Name
- PKI 166
- Synonyms
- PKI 166;PKI 166,PKI166;PKI-166 >=98% (HPLC);PKI-166, 10 mM in DMSO;4-[4-[[(1R)-1-Phenylethyl]amino]-1H-pyrrolo[2,3-d]pyrimidin-;(R)-4-(4-((1-Phenylethyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)phenol;4-[4-(((R)-1-Phenylethyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]phenol;(R)-4-[4-[(1-Phenylethyl)amino]-1H-pyrrolo[2,3-d]pyrimidin-6-yl]-phenol;Phenol, 4-[4-[[(1R)-1-phenylethyl]amino]-7H-pyrrolo[2,3-d]pyrimidin-6-yl]-;(R)-6-(4-Hydroxyphenyl)-4-[(1-phenylethyl)amino]-7H-pyrrolo[2,3-d]pyrimidine
- CBNumber
- CB41399257
- Molecular Formula
- C20H18N4O
- Formula Weight
- 330.38
- MOL File
- 187724-61-4.mol
PKI 166 Property
- Density
- 1.324±0.06 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- DMSO: soluble10mg/mL, clear
- form
- powder
- pka
- 9.67±0.15(Predicted)
- color
- white to beige
N-Bromosuccinimide Price
- Product number
- SML1095
- Product name
- PKI-166
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $91
- Updated
- 2025/07/31
- Product number
- SML1095
- Product name
- PKI-166
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $579
- Updated
- 2023/06/20
- Product number
- 21896
- Product name
- PKI-166
- Packaging
- 1mg
- Price
- $36
- Updated
- 2024/03/01
- Product number
- 21896
- Product name
- PKI-166
- Packaging
- 5mg
- Price
- $120
- Updated
- 2024/03/01
- Product number
- 21896
- Product name
- PKI-166
- Packaging
- 10mg
- Price
- $223
- Updated
- 2024/03/01
PKI 166 Chemical Properties,Usage,Production
Uses
PKI-166 is a potent, selective and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 0.7 nM[1].
Biological Activity
PKI-166 is a potent, selective and orally bioactive EGFR tyrosine kinase inhibitor with IC50 of 0.7 nM.
in vitro
Pretreatment with PKI-166 (0-0.5 μM; 1 hour) inhibits EGFR autophosphorylation in human pancreatic cancer cells.
PKI-166 (0.03 μM; 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 |
| Conce ntration: | 0.03 μM |
| Incubation Time: | 6 days |
| Result: | Enhanced the cytotoxicity mediated by gemcitabine. |
in vivo
PKI-166 (100 mg/kg; po; 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. |
target
IC50: 0.7 nM (EGFR tyrosine kinase)
References
[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. PMID:10850439
PKI 166 Preparation Products And Raw materials
Raw materials
Preparation Products
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