AG957 (Tyrphostin AG957;NSC 654705) 是一种酪氨酸激酶抑制剂，具有抗BCR/ABL酪氨酸激酶活性。AG957抑制p210bcr/abl酶活性，IC50为 2.9 μM。
| 生物活性 | AG957 (Tyrphostin AG957;NSC 654705) is a tyrosine kinase inhibitor with anti-BCR/ABLtyrosine kinase activity[1][2]. AG957 is abcr/ablkinase inhibitor with anIC50of 2.9 μM forp210bcr/ablautokinase activity[3]. |
体外研究
(In Vitro) | AG957 inhibit p210bcr-abl tyrosine kinase activity. AG957 inhibits DNA synthesis as early as 2 h (60% inhibition at 20 microM). AG957 inhibits p210bcr-abl tyrosine phosphorylation in living cells by 1 h without an inhibition of total protein phosphorylation[1].
Tyrphostin AG957, a protein tyrosine kinase (PTK) inhibitor which has activity against the p210BCR/ABLkinase, on beta1 integrin function in CML progenitors[2].
AG957 (0.1-100 μM ) pretreatment results in significant inhibition of proliferation of chronic myelogenous leukemia (CML) colony-forming cells (CFC)
CML CFC[2].
AG957 (25 μM) partially inhibits phosphorylation of several proteins that are BCR/ABL PTK substrates and are involved in normal integrin signaling in BCR/ABL expressing cells[2].
Cell Proliferation Assay[2] | Cell Line: | CML and CFC | | Concentration: | 0, 0.1, 1, 10, 100 μM | | Incubation Time: | Pretreatment for 1 hour | | Result: | A significant dose-dependent inhibition of CML CFC growth was seen following preincubation with AG957. |
Western Blot Analysis[2] | Cell Line: | K562 and BCR/ABL-tranfected M07e cells (MBA-4) | | Concentration: | 25 μM | | Incubation Time: | 24 hours | | Result: | Partially inhibited tyrosine phosphorylation of p210BCR/ABL, the focal adhesion protein paxillin, the p85 regulatory subunit of the PI3K and the adapter protein cbl in K562 cells.
Inhibited phosphorylation of these proteins as well as the adapter protein crkl in MBA4 cells. |
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体内研究
(In Vivo) | AG957 (10 mg/kg; intratracheally 1 h before intratracheal LPS challenge) blocks c-Abl activity in the lung of mice[4].
| Animal Model: | C57BL/6J mice[4] | | Dosage: | 10 mg/kg | | Administration: | Intratracheally 1 h before intratracheal LPS challenge | | Result: | LPS induced significant phosphorylation of paxillin at Y31 and Y118. Inhibition of c-Abl by AG957 attenuated LPS-induced phosphorylation of paxillin at both sites.
LPS induced significant phosphorylation of VE-cadherin in DMSO-treated mice, which was attenuated in AG957-treated mice. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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