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AG-490

Cayman Chemical Item Number 10010311

(CAS 133550-30-8)

AG-490 (CAS 133550-30-8)

See more	Receptor Biochemistry (344) Inhibitors (546) Apoptosis (191) Cancer (666)

Description

Protein tyrosine kinase (Ptk) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of Ptks. Tyrphostins are a class of antiproliferative compounds which act as Ptk blockers.¹ Leukemic cells from patients in relapse have constitutively activated JAK2 Ptk. AG-490 is an inhibitor of JAK2 activity and selectively blocks leukemic cell growth in vitro and in vivo by inducing programmed cell death, with no deleterious effect on normal hematopoiesis. AG-490 almost completely blocks growth of all pre-B acute leukemia (ALL) cells at a concentration of 5 µM.²

1 Gazit, A., Yaish, P., Gilon, C., et al. Tyrphostins I: Synthesis and biological activity of protein tyrosine kinase inhibitors. J Med Chem 32(10) 2344-2352 (1989).

2 Meydan, N., Grunberger, T., Dadi, H., et al. Inhibition of acute lymphoblastic leukaemia by a Jak-2 inhibitor. Nature 379 645-648 (1996).

Formal Name	2-cyano-3-(3,4-dihydroxyphenyl)-N-(phenylmethyl)-2-propenamide
CAS Number	133550-30-8
Molecular Formula	C₁₇H₁₄N₂O₃
Formula Weight	294.3
Formulation	A crystalline solid
Purity	≥98%
λ_max	257, 363 nm
Stability	2 years
Storage	-20°C
Shipping	Room temperature in continental US; may vary elsewhere
SMILES	Copy SMILES to clipboard N#C/C(=C\c1ccc(O)c(O)c1)/C(=O)NCc1ccccc1

Background Reading

Gazit, A., Yaish, P., Gilon, C., et al. Tyrphostins I: Synthesis and biological activity of protein tyrosine kinase inhibitors. J Med Chem 32(10) 2344-2352 (1989).

Meydan, N., Grunberger, T., Dadi, H., et al. Inhibition of acute lymphoblastic leukaemia by a Jak-2 inhibitor. Nature 379 645-648 (1996).

AG-490 is available in the following screening library:

Kinase Screening Library (96-Well)

Size	Price	Quantity	Subtotal
5 mg	$27.00		$0.00
10 mg	$51.00		$0.00
25 mg	$122.00		$0.00
50 mg	$216.00		$0.00
Bulk	Contact
		Cart Total	$0.00

Pricing updated 2012-05-25. 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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Batch-specific Information

Cayman Chemical is a manufacturer, supplier and vendor of biochemical reagents, assay kits, antibodies, and proteins.

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