| Name | FLT3 |
|---|---|
| Synonyms | CD135; STK 1; Tyrosine protein kinase receptor; STK1; CD135 antigen; FL cytokine receptor; FL cytokine receptor precursor; FLK 2… |
| Name | piperazine |
|---|---|
| CAS | piperazine |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 16446383 | Radomska HS, Basseres DS, Zheng R, Zhang P, Dayaram T, Yamamoto Y, Sternberg DW, Lokker N, Giese NA, Bohlander SK, Schnittger S, Delmotte MH, Davis RJ, Small D, Hiddemann W, Gilliland DG, Tenen DG: Block of C/EBP alpha function by phosphorylation in acute myeloid leukemia with FLT3 activating mutations. J Exp Med. 2006 Feb 20;203(2):371-81. Epub 2006 Jan 30. |
5(0,0,0,5) | Details |
| 16902153 | DeAngelo DJ, Stone RM, Heaney ML, Nimer SD, Paquette RL, Klisovic RB, Caligiuri MA, Cooper MR, Lecerf JM, Karol MD, Sheng S, Holford N, Curtin PT, Druker BJ, Heinrich MC: Phase 1 clinical results with tandutinib (MLN518), a novel FLT3 antagonist, in patients with acute myelogenous leukemia or high-risk myelodysplastic syndrome: safety, pharmacokinetics, and pharmacodynamics. Blood. 2006 Dec 1;108(12):3674-81. Epub 2006 Aug 10. |
5(0,0,0,5) | Details |
| 12124172 | Kelly LM, Yu JC, Boulton CL, Apatira M, Li J, Sullivan CM, Williams I, Amaral SM, Curley DP, Duclos N, Neuberg D, Scarborough RM, Pandey A, Hollenbach S, Abe K, Lokker NA, Gilliland DG, Giese NA: CT53518, a novel selective FLT3 antagonist for the treatment of acute myelogenous leukemia (AML). Cancer Cell. 2002 Jun;1(5):421-32. Up to 30% of acute myelogenous leukemia (AML) patients harbor an activating internal tandem duplication (ITD) within the juxtamembrane domain of the FLT3 receptor, suggesting that it may be a target for kinase inhibitor therapy. |
4(0,0,0,4) | Details |
| 19654408 | Zarrinkar PP, Gunawardane RN, Cramer MD, Gardner MF, Brigham D, Belli B, Karaman MW, Pratz KW, Pallares G, Chao Q, Sprankle KG, Patel HK, Levis M, Armstrong RC, James J, Bhagwat SS: AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). Blood. 2009 Oct 1;114(14):2984-92. Epub 2009 Aug 4. |
4(0,0,0,4) | Details |
| 18175263 | Cheng Y, Paz K: Tandutinib, an oral, small-molecule inhibitor of FLT3 for the treatment of AML and other cancer indications. IDrugs. 2008 Jan;11(1):46-56. |
4(0,0,0,4) | Details |
| 12166950 | Pandey A, Volkots DL, Seroogy JM, Rose JW, Yu JC, Lambing JL, Hutchaleelaha A, Hollenbach SJ, Abe K, Giese NA, Scarborough RM: Identification of orally active, potent, and selective 4-piperazinylquinazolines as antagonists of the platelet-derived growth factor receptor tyrosine kinase family. J Med Chem. 2002 Aug 15;45(17):3772-93. An optimized analogue in this series, 75 (CT53518), inhibits Flt-3, betaPDGFR, and c-Kit receptor phosphorylation with IC (50) values of 50-200 nM, whereas 15-20-fold less potent activity against CSF-1R was observed. |
3(0,0,0,3) | Details |
| 18342808 | Tam WF, Gary Gilliland D: Can FLT3 inhibitors overcome resistance in AML? . Best Pract Res Clin Haematol. 2008 Mar;21(1):13-20. |
3(0,0,0,3) | Details |
| 18559972 | Tam WF, Gu TL, Chen J, Lee BH, Bullinger L, Frohling S, Wang A, Monti S, Golub TR, Gilliland DG: Id1 is a common downstream target of oncogenic kinases in leukemic cells. Blood. 2008 Sep 1;112(5):1981-92. Epub 2008 Jun 17. Oncogenic kinases, such as BCR-ABL, TEL-ABL, TEL-PDGFbetaR, and FLT3-ITD, play a major role in the development of hematopoietic malignancy. |
2(0,0,0,2) | Details |
| 16715961 | Kiyoi H: [The present status of, and problems with the development of FLT3 kinase inhibitors] Rinsho Ketsueki. 2006 Apr;47(4):270-7. |
1(0,0,0,1) | Details |
| 16447713 | Kiyoi H: [Possibility of targeting FLT3 kinase for the treatment of leukemia] Rinsho Ketsueki. 2005 Mar;46(3):187-97. |
1(0,0,0,1) | Details |
| 15585651 | Walters DK, Stoffregen EP, Heinrich MC, Deininger MW, Druker BJ: RNAi-induced down-regulation of FLT3 expression in AML cell lines increases sensitivity to MLN518. Blood. 2005 Apr 1;105(7):2952-4. Epub 2004 Dec 7. |
8(0,0,0,8) | Details |
| 15256420 | Clark JJ, Cools J, Curley DP, Yu JC, Lokker NA, Giese NA, Gilliland DG: Variable sensitivity of FLT3 activation loop mutations to the small molecule kinase inhibitor MLN518. Blood. 2004 Nov 1;104(9):2867-72. Epub 2004 Jul 15. |
8(0,0,0,8) | Details |
| 15242881 | Griswold IJ, Shen LJ, La Rosee P, Demehri S, Heinrich MC, Braziel RM, McGreevey L, Haley AD, Giese N, Druker BJ, Deininger MW: Effects of MLN518, a dual FLT3 and KIT inhibitor, on normal and malignant hematopoiesis. Blood. 2004 Nov 1;104(9):2912-8. Epub 2004 Jul 8. |
6(0,0,0,6) | Details |
| 18282363 | Illmer T, Ehninger G: FLT3 kinase inhibitors in the management of acute myeloid leukemia. . Clin Lymphoma Myeloma. 2007 Dec;8 Suppl 1:S24-34. |
6(0,0,0,6) | Details |
| 19625780 | Schittenhelm MM, Kampa KM, Yee KW, Heinrich MC: The FLT3 inhibitor tandutinib (formerly MLN518) has sequence-independent synergistic effects with cytarabine and daunorubicin. Cell Cycle. 2009 Aug 15;8(16):2621-30. Epub 2009 Aug 24. |
5(0,0,0,5) | Details |