| Identification | Back Directory | [Name]
PKI 166 | [CAS]
187724-61-4 | [Synonyms]
PKI 166
PKI-166 >=98% (HPLC)
4-[4-[[(1R)-1-Phenylethyl]amino]-1H-pyrrolo[2,3-d]pyrimidin-
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 | [Molecular Formula]
C20H18N4O | [MDL Number]
MFCD09970842 | [MOL File]
187724-61-4.mol | [Molecular Weight]
330.38 |
| Chemical Properties | Back Directory | [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 | [InChI]
1S/C20H18N4O/c1-13(14-5-3-2-4-6-14)23-19-17-11-18(24-20(17)22-12-21-19)15-7-9-16(25)10-8-15/h2-13,25H,1H3,(H2,21,22,23,24)/t13-/m1/s1 | [InChIKey]
XRYJULCDUUATMC-CYBMUJFWSA-N | [SMILES]
OC(C=C1)=CC=C1C2=CC3=C(N2)N=CN=C3N[C@H](C)C4=CC=CC=C4 |
| Safety Data | Back Directory | [Hazard Codes ]
T | [Risk Statements ]
25 | [Safety Statements ]
45 | [RIDADR ]
UN 2811 6.1 / PGIII | [WGK Germany ]
3 | [Storage Class]
6.1C - Combustible acute toxic Cat.3
toxic compounds or compounds which causing chronic effects | [Hazard Classifications]
Acute Tox. 3 Oral |
| Hazard Information | Back Directory | [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 |
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| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
|