AG-490A tyrosine kinase inhibitor of JAK2, EGFR, JAK3 and Neu

AG-490 (CAS 133550-30-8)

AG-490 | CAS 133550-30-8 is rated 5.0 out of 5 by 1.
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Synonym: Tyrphostin B42
Application: A tyrosine kinase inhibitor of JAK2, EGFR, JAK3 and Neu
CAS Number: 133550-30-8
Purity: ≥98%
Molecular Weight: 294.30
Molecular Formula: C17H14N2O3
* Refer to Certificate of Analysis for lot specific data (including water content).
Submit a review for this product and receive 15 CruzCredits

AG-490 is a tyrosine kinase inhibitor of JAK2, EGFR, and Neu that belongs to the family of tyrphostins. In acute lymphoblastic leukemia studies the compound has been reported to inhibit JAK2 from B cell precursors. Additionally, AG-490 has been observed to block cytokine-induced activation of JAK2 in eosinophils and STAT3 activation in T cell lymphoma cells. Unlike other kinase inhibitors, AG-490 does not inhibit JAK1, Lck, Btk, Tyk2, Syk, Lyn, and Src. Research indicates that AG-490 inhibits IL-7 mediated proliferation. Inhibition of Jak kinase activity by AG-490 leads to lower levels of p85 phosphorylation and p-13 kinase activation. AG-490 is an inhibitor of JAK3.


References

1. Dadi, H., et al. 1994. Blood. 84: 1579-1586. PMID: 7520779
2. Sharfe, N., et al. 1995. Blood. 86: 2077-2085. PMID: 7662955
3. Meydan, N., et al. 1996. Nature. 379: 645-648. PMID: 8628398
4. Wang, L.H., et al. 1999. J. Immunol. 162: 3897-3904. PMID: 10201908
5. Kirken, R.A., et al. 1999. J. Leukoc. Biol. 65: 891-899. PMID: 10380915
6. De Vos, J., et al. 2000. Br. J. Haematol. 109: 823-828. PMID: 10929036

Physical State :
Solid
Solubility :
Soluble in DMSO (30 mg/ml), DMF (40 mg/ml), ethanol (15 mg/ml), methanol, acetone, chloroform, and 1:10 DMSO:PBS (pH7.2) (~0.1 mg/ml). Insoluble in water.
Storage :
Store at -20° C
Melting Point :
232.00° C (Predicted)
Boiling Point :
615.21° C at 760 mmHg
Density :
1.34 g/cm3
Refractive Index :
n20D 1.68
IC50 :
EGFR: IC50 = 2 µM (human A431 cells); ErbB2 : IC50 = 13.5 µM; HER1 autophosphorylation: IC50 = 0.1 µM; Epidermal growth factor receptor autophosphorylation: IC50 = 0.1 µM; JAK1: IC50 = 3.38 µM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
5328779
MDL Number :
MFCD00236452
SMILES :
C1=CC=C(C=C1)CNC(=O)/C(=C/C2=CC(=C(C=C2)O)O)/C#N

Download SDS (MSDS)

Certificate of Analysis

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AG-490  Product Citations

See how others have used AG-490. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 15 total

PMID: # 27702536  Yang, LC. et al. 2017. Carbohydr Polym. 155: 466-474.

PMID: # 28548090  Jayatilaka, H.|Tyle, P.|Chen, JJ.|Kwak, M.|Ju, J.|Kim, HJ.|Lee, JSH.|Wu, PH.|Gilkes, DM.|Fan, R.|Wirtz, D.| et al. 2017. Nat Commun. 8: 15584.

PMID: # 29018784  Ju, KD. et al. 2017. J Cancer Prev. 22: 189-194.

PMID: # 28526849  Wu, Z. et al. 2017. Sci Rep. 7: 2210.

PMID: # 28112370  Doi, T. et al. 2017. Oncol. Rep. 37: 1545-1554.

PMID: # 27283206  2016. CNS Neurosci Ther. 22: 771-81.

PMID: # 26677135  Gao, Q. et al. 2016. Int. J. Mol. Med. 37: 347-58.

PMID: # 25879793  Li, W. et al. 2015. J. Periodontol. 86: 917-26.

PMID: # 26188365  Acevedo-Olvera, LF. et al. 2015. Cytokine. 75: 142-50.

PMID: # 25193864  Kavarthapu, R. et al. 2014. Oncotarget. 5: 9079-91.

Citations 1 to 10 of 15 total

What is the appearance of the compound?

Asked by: two2igm05
Thank you for your question. AG-490, sc-202046, is in yellow powder form.
Answered by: Chemical Support 4
Date published: 2017-05-02

Is this compound stable to be stored at -20℃ after dissolving in DMSO?

Asked by: two2igm05
Thank you for your question. AG-490, sc-202046, can be stored at -80℃ for 6 months when dissolved in DMSO or for 3 years -20℃ as a powder.
Answered by: TechService7
Date published: 2016-12-16
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Rated 5 out of 5 by from Ali Ali, et. al. (PubMed ID 9287353) was able to demonstrate that AG-490 had no effect on the association of Jak2 with the GST-AT1A fusion protein. -SCBT Publication Review
Date published: 2015-07-06
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