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

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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

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Safety

Hazard Codes: T
Risk Statements: 25
Safety Statements: 45
RIDADR: UN 2811 6.1 / PGIII
WGK Germany: 3

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word: Danger
Hazard statements: H301Toxic if swalloed
Precautionary statements: P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML1095
Product name: PKI-166
Purity: ≥98% (HPLC)
Packaging: 5mg
Price: $91
Updated: 2025/07/31

Sigma-Aldrich

Product number: SML1095
Product name: PKI-166
Purity: ≥98% (HPLC)
Packaging: 25mg
Price: $579
Updated: 2023/06/20

Cayman Chemical

Product number: 21896
Product name: PKI-166
Packaging: 1mg
Price: $36
Updated: 2024/03/01

Cayman Chemical

Product number: 21896
Product name: PKI-166
Packaging: 5mg
Price: $120
Updated: 2024/03/01

Cayman Chemical

Product number: 21896
Product name: PKI-166
Packaging: 10mg
Price: $223
Updated: 2024/03/01

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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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PKI 166 Suppliers

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187724-61-4, PKI 166Related Search:

PKI 166

(R)-4-[4-[(1-Phenylethyl)amino]-1H-pyrrolo[2,3-d]pyrimidin-6-yl]-phenol

(R)-6-(4-Hydroxyphenyl)-4-[(1-phenylethyl)amino]-7H-pyrrolo[2,3-d]pyrimidine

4-[4-(((R)-1-Phenylethyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]phenol

4-[4-[[(1R)-1-Phenylethyl]amino]-1H-pyrrolo[2,3-d]pyrimidin-

Phenol, 4-[4-[[(1R)-1-phenylethyl]amino]-7H-pyrrolo[2,3-d]pyrimidin-6-yl]-

PKI-166 >=98% (HPLC)

PKI 166,PKI166

(R)-4-(4-((1-Phenylethyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)phenol

PKI-166, 10 mM in DMSO

187724-61-4