AG-1478
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MedKoo CAT#: 401019

CAS#: 153436-53-4

Description: Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTK. Tyrphostins are a class of antiproliferative compounds which act as PTK blockers. PTK inhibitors which preferentially inhibit the epidermal growth factor receptor (EGFR) kinase and block EGFR-dependent cell proliferation. AG-1478 is an inhibitor of EGFR kinase with an IC50 value of 3 nM.1 Due to its potency and selectivity, AG-1478 has been used in a broad range of studies. It reversibly inhibits rat brain Kv1.5 potassium channels (IC50 = 9.8 µM) independent of protein tyrosine kinase (PTK) activity.2 AG-1478 also inhibits the growth of leiomyoma and myometrium cell cultures with IC50 values of 5.6 and 5.7 µM, respectively. This inhibitor suppresses MAP kinase activation and strongly inhibits induction of fos gene expression and DNA synthesis.


Chemical Structure

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AG-1478
CAS# 153436-53-4

Theoretical Analysis

MedKoo Cat#: 401019
Name: AG-1478
CAS#: 153436-53-4
Chemical Formula: C16H14ClN3O2
Exact Mass: 315.07745
Molecular Weight: 315.75426
Elemental Analysis: C, 60.86; H, 4.47; Cl, 11.23; N, 13.31; O, 10.13

Price and Availability

Size Price Availability Quantity
100.0mg USD 450.0 2 Weeks
200.0mg USD 750.0 2 Weeks
500.0mg USD 1550.0 2 Weeks
1.0g USD 2650.0 2 Weeks
2.0g USD 4650.0 2 Weeks
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Synonym: AG1478; AG-1478; AG 1478; Tyrphostin AG 1478.

IUPAC/Chemical Name: N-(3-chlorophenyl)-6,7-dimethoxyquinazolin-4-amine

InChi Key: GFNNBHLJANVSQV-UHFFFAOYSA-N

InChi Code: InChI=1S/C16H14ClN3O2/c1-21-14-7-12-13(8-15(14)22-2)18-9-19-16(12)20-11-5-3-4-10(17)6-11/h3-9H,1-2H3,(H,18,19,20)

SMILES Code: COC1=CC2=NC=NC(NC3=CC=CC(Cl)=C3)=C2C=C1OC

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, not in water

Shelf Life: >5 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

Preparing Stock Solutions

The following data is based on the product molecular weight 315.75426 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

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1: Hegab AE, Sakamoto T, Nomura A, Ishii Y, Morishima Y, Iizuka T, Kiwamoto T, Matsuno Y, Homma S, Sekizawa K. Niflumic acid and AG-1478 reduce cigarette smoke-induced mucin synthesis: the role of hCLCA1. Chest. 2007 Apr;131(4):1149-56. PubMed PMID: 17426222.

2: Clayton AH, Perugini MA, Weinstock J, Rothacker J, Watson KG, Burgess AW, Nice EC. Fluorescence and analytical ultracentrifugation analyses of the interaction of the tyrosine kinase inhibitor, tyrphostin AG 1478-mesylate, with albumin. Anal Biochem. 2005 Jul 15;342(2):292-9. PubMed PMID: 15913535.

3: Choi BH, Choi JS, Rhie DJ, Yoon SH, Min DS, Jo YH, Kim MS, Hahn SJ. Direct inhibition of the cloned Kv1.5 channel by AG-1478, a tyrosine kinase inhibitor. Am J Physiol Cell Physiol. 2002 Jun;282(6):C1461-8. PubMed PMID: 11997261.

4: Stekelenburg J, Klein BY, Ben-Bassat H, Rojansky N. Opposing effects of cyclosporin A and tyrphostin AG-1478 indicate a role for Src protein in the cellular control of mineralization. J Cell Biochem. 1998 Oct 1;71(1):116-26. PubMed PMID: 9736460.

5: Han Y, Caday CG, Nanda A, Cavenee WK, Huang HJ. Tyrphostin AG 1478 preferentially inhibits human glioma cells expressing truncated rather than wild-type epidermal growth factor receptors. Cancer Res. 1996 Sep 1;56(17):3859-61. PubMed PMID: 8752145.

AG-1478

100.0mg / USD 450.0


Additional Information