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AG-1478

Cayman Chemical Item Number 10010244

NSC 693255; Tyrphostin AG-1478 (CAS 153436-53-4)

AG-1478 (CAS 153436-53-4)

See more	Inhibitors (493) Cancer (606)

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 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.³ This inhibitor suppresses MAP kinase activation and strongly inhibits induction of fos gene expression and DNA synthesis.⁴

1 Levitzki, A., and Gazit, A. Tyrosine kinase inhibition: An approach to drug development. Science 267(5205) 1782-1788 (1995).

2 Choi, B.H., Choi, J., Rhie, D., et al. Direct inhibition of the cloned Kv1.5 channel by AG-1478, a tyrosine kinase inhibitor. Am J Physiol Cell Physiol 282 c1461-c1468 (2002).

3 Shushan, A., Rojansky, N., Laufer, N., et al. The AG1478 tyrosine kinase inhibitor is an effective suppressor of leiomyoma cell growth. Hum Reprod 19(9) 1957-1967 (2004).

4 Daub, H., Weiss, F.U., Wallasch, C., et al. Role of transactivation of the EGF receptor in signalling by G-protein-coupled receptors. Nature 379 557-560 (1996).

Synonyms	NSC 693255 Tyrphostin AG-1478
Formal Name	N-(3-chlorophenyl)-6,7-dimethoxy-4-quinazolinamine
CAS Number	153436-53-4
Molecular Formula	C₁₆H₁₄ClN₃O₂
Formula Weight	315.8
Formulation	A crystalline solid
Purity	>98%
λ_max	222, 255, 346 nm
Stability	2 years
Storage	-20°C
Shipping	Room temperature in continental US; may vary elsewhere
SMILES	Copy SMILES to clipboard COc1cc2c(ncnc2cc1OC)Nc1cccc(Cl)c1

Background Reading

Levitzki, A., and Gazit, A. Tyrosine kinase inhibition: An approach to drug development. Science 267(5205) 1782-1788 (1995).

Daub, H., Weiss, F.U., Wallasch, C., et al. Role of transactivation of the EGF receptor in signalling by G-protein-coupled receptors. Nature 379 557-560 (1996).

Choi, B.H., Choi, J., Rhie, D., et al. Direct inhibition of the cloned Kv1.5 channel by AG-1478, a tyrosine kinase inhibitor. Am J Physiol Cell Physiol 282 c1461-c1468 (2002).

Shushan, A., Rojansky, N., Laufer, N., et al. The AG1478 tyrosine kinase inhibitor is an effective suppressor of leiomyoma cell growth. Hum Reprod 19(9) 1957-1967 (2004).

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AG-1478 is available in the following screening library:

Kinase Screening Library (96-Well)

Size	Price	Quantity	Subtotal
1 mg	$17.00		$0.00
5 mg	$77.00		$0.00
10 mg	$136.00		$0.00
25 mg	$298.00		$0.00
Bulk	Contact
		Cart Total	$0.00

Pricing updated 2012-02-12. Prices are subject to change without notice.

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Warning This product is not for human or veterinary use.

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