PKI166
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    WARNING: This product is for research use only, not for human or veterinary use.

Hodoodo CAT#: H532472

CAS#: 187724-61-4

Description: PKI166 is an experimental, reversible inhibitor of epidermal growth factor receptor tyrosine kinase.

Chemical Structure

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PKI166
CAS# 187724-61-4
Instruction

Theoretical Analysis

Hodoodo Cat#: H532472
Name: PKI166
CAS#: 187724-61-4
Chemical Formula: C20H18N4O
Exact Mass: 330.15
Molecular Weight: 330.390
Elemental Analysis: C, 72.71; H, 5.49; N, 16.96; O, 4.84

Price and Availability

Size Price Availability Quantity
5mg USD 300 2 Weeks
10mg USD 550 2 Weeks
25mg USD 850 2 Weeks
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Synonym: PKI166; PKI 166; PKI-166.

IUPAC/Chemical Name: 4-[4-[[(1R)-1-phenylethyl]amino]-7H-pyrrolo[4,5-e]pyrimidin-6-yl]phenol

InChi Key: XRYJULCDUUATMC-CYBMUJFWSA-N

InChi Code: 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

SMILES Code: OC1=CC=C(C2=CC3=C(N[C@@H](C4=CC=CC=C4)C)N=CN=C3N2)C=C1

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 330.39 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Hoekstra R, Dumez H, Eskens FA, van der Gaast A, Planting AS, de Heus G, Sizer KC, Ravera C, Vaidyanathan S, Bucana C, Fidler IJ, van Oosterom AT, Verweij J. Phase I and pharmacologic study of PKI166, an epidermal growth factor receptor tyrosine kinase inhibitor, in patients with advanced solid malignancies. Clin Cancer Res. 2005 Oct 1;11(19 Pt 1):6908-15. PubMed PMID: 16203782.

2: Takada T, Weiss HM, Kretz O, Gross G, Sugiyama Y. Hepatic transport of PKI166, an epidermal growth factor receptor kinase inhibitor of the pyrrolo-pyrimidine class, and its main metabolite, ACU154. Drug Metab Dispos. 2004 Nov;32(11):1272-8. Epub 2004 Jul 27. PubMed PMID: 15280219.