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Merck

658401

Sigma-Aldrich

AG 490

A cell-permeable, reversible, substrate competitive, and potent inhibitor of epidermal growth factor receptor kinase autophosphorylation (IC50 = 100 nM).

동의어(들):

AG 490, α-Cyano-(3,4-dihydroxy)-N-benzylcinnamide, Tyrphostin B42, ( E)- N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl)acrylamide, JAK1 Inhibitor II, JAK2 Inhibitor VI, JAK3 Inhibitor XI, α-Cyano-(3,4-dihydroxy)-N-benzylcinnamide, Tyrphostin B42, (E)-N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl)acrylamide, JAK1 Inhibitor II, JAK2 Inhibitor VI, JAK3 Inhibitor XI

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크기 선택

제품정보 (DICE 배송 시 비용 별도)

실험식(Hill 표기법):
C17H14N2O3
CAS 번호:
133550-30-8
Molecular Weight:
294.30
MDL number:
MFCD00236452
UNSPSC 코드:
12352200
NACRES:
NA.77

주요 문서

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기술 서비스
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도움 문의

Quality Level

100

분석

≥98% (HPLC)

양식

solid

제조업체/상표

Calbiochem®

저장 조건

OK to freeze
protect from light

색상

yellow

solubility

DMSO: 100 mg/mL

배송 상태

ambient

저장 온도

−20°C

SMILES string

N(Cc2ccccc2)C(=O)\C(=C\c1cc(c(cc1)O)O)\C#N

InChI

1S/C17H14N2O3/c18-10-14(8-13-6-7-15(20)16(21)9-13)17(22)19-11-12-4-2-1-3-5-12/h1-9,20-21H,11H2,(H,19,22)/b14-8+

InChI key

TUCIOBMMDDOEMM-RIYZIHGNSA-N

관련 카테고리

일반 설명

A cell-permeable, reversible, substrate competitive, and potent inhibitor of epidermal growth factor receptor kinase autophosphorylation (IC50 = 100 nM). Inhibition of JAK2 by AG 490 selectively blocks leukemic cell growth in vitro and in vivo by inducing programmed cell death, with no harmful effect on normal hematopoiesis. Inhibits the constitutive activation of STAT-3 DNA binding and IL-2-induced growth of MF tumor cells. AG 490 has also been shown to inhibit the autokinase activity of JAK3. A 100 mM (5 mg/170 µl) solution of AG490 (Cat. No. 658411) in DMSO is also available.

생화학적/생리학적 작용

Cell permeable: yes
Primary Target
epidermal growth factor receptor kinase autophosphorylation
Product does not compete with ATP.
Reversible: yes
Target IC50: 100 nM against epidermal growth factor receptor kinase autophosphorylation

제조 메모

Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.

기타 정보

Jaleel, M., et al. 2004. Biochemistry43, 8247.
Eriksen, K.W., et al. 2001. Leukemia15, 787.
Kirken, R.A., et al. 1999. Leukoc. Biol.65, 891.
Nielsen, M., et al. 1997. Proc. Natl. Acad. Sci. USA 94, 6764.
Meydan, N., et al. 1996. Nature 379, 645.
Gazit, A., et al. 1991. J. Med. Chem.34, 1896.
Levitzki, A. 1990. Biochem. Pharmacol.40, 913.

법적 정보

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

면책조항

Toxicity: Standard Handling (A)

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

시험 성적서(COA)

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관련 콘텐츠

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