LT-540-717
LT-540-717 (compound 32) is a potent FLT3 inhibitor (IC50=0.62 nM) with antiproliferative activity. LT-540-717 also inhibits several acquired FLT3 mutations, FLT3 (ITD, D835V), FLT3 (ITD, F691L), FLT3 (D835Y) and FLT3 (D835V). LT-540-717 has potential to be an anti-AML agent.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2143089-35-2
- 分子式: C24H24N8O2
- 分子量:456.50
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| ACHN | GI50 |
<1 μM
Compound: 32; LT-540-717
|
Antiproliferative activity against human ACHN cells assessed as inhibition of cell growth
Antiproliferative activity against human ACHN cells assessed as inhibition of cell growth
|
[PMID: 37163951] |
| BaF3 | IC50 |
0.009 μM
Compound: 32; LT-540-717
|
Antiproliferative activity against mouse BaF3 cells harboring FLT3 ITD/D835V mutant assessed as inhibition of cell growth incubated for 72 hrs
Antiproliferative activity against mouse BaF3 cells harboring FLT3 ITD/D835V mutant assessed as inhibition of cell growth incubated for 72 hrs
|
[PMID: 37163951] |
| BaF3 | IC50 |
0.039 μM
Compound: 32; LT-540-717
|
Antiproliferative activity against mouse BaF3 cells harboring FLT3 ITD mutant assessed as inhibition of cell growth incubated for 72 hrs
Antiproliferative activity against mouse BaF3 cells harboring FLT3 ITD mutant assessed as inhibition of cell growth incubated for 72 hrs
|
[PMID: 37163951] |
| BaF3 | IC50 |
0.043 μM
Compound: 32; LT-540-717
|
Antiproliferative activity against mouse BaF3 cells harboring FLT3 D835V mutant assessed as inhibition of cell growth incubated for 72 hrs
Antiproliferative activity against mouse BaF3 cells harboring FLT3 D835V mutant assessed as inhibition of cell growth incubated for 72 hrs
|
[PMID: 37163951] |
| BaF3 | IC50 |
0.054 μM
Compound: 32; LT-540-717
|
Antiproliferative activity against mouse BaF3 cells harboring FLT3 ITD/N676D mutant assessed as inhibition of cell growth incubated for 72 hrs
Antiproliferative activity against mouse BaF3 cells harboring FLT3 ITD/N676D mutant assessed as inhibition of cell growth incubated for 72 hrs
|
[PMID: 37163951] |
| BaF3 | IC50 |
0.095 μM
Compound: 32; LT-540-717
|
Antiproliferative activity against mouse BaF3 cells harboring FLT3 ITD/F691L mutant assessed as inhibition of cell growth incubated for 72 hrs
Antiproliferative activity against mouse BaF3 cells harboring FLT3 ITD/F691L mutant assessed as inhibition of cell growth incubated for 72 hrs
|
[PMID: 37163951] |
| BaF3 | IC50 |
2.922 μM
Compound: 32; LT-540-717
|
Cytotoxicity against mouse BaF3 cells assessed as inhibition of cell growth incubated for 72 hrs
Cytotoxicity against mouse BaF3 cells assessed as inhibition of cell growth incubated for 72 hrs
|
[PMID: 37163951] |
| HL-60 | IC50 |
972.1 nM
Compound: 32; LT-540-717
|
Antiproliferative activity against human HL-60 cells expressing low level wild type FLT3 assessed as inhibition of cell growth
Antiproliferative activity against human HL-60 cells expressing low level wild type FLT3 assessed as inhibition of cell growth
|
[PMID: 37163951] |
| K562 | IC50 |
572.1 nM
Compound: 32; LT-540-717
|
Antiproliferative activity against human K562 cells deficit of oncogenic FLT3 assessed as inhibition of cell growth
Antiproliferative activity against human K562 cells deficit of oncogenic FLT3 assessed as inhibition of cell growth
|
[PMID: 37163951] |
| KM12 | GI50 |
<1 μM
Compound: 32; LT-540-717
|
Antiproliferative activity against human KM12 cells assessed as inhibition of cell growth
Antiproliferative activity against human KM12 cells assessed as inhibition of cell growth
|
[PMID: 37163951] |
| LOX IMVI | GI50 |
<1 μM
Compound: 32; LT-540-717
|
Antiproliferative activity against human LOX IMVI cells assessed as inhibition of cell growth
Antiproliferative activity against human LOX IMVI cells assessed as inhibition of cell growth
|
[PMID: 37163951] |
| MOLM-13 | IC50 |
16.3 nM
Compound: 32; LT-540-717
|
Antiproliferative activity against human MOLM-13 cells harboring FLT3 ITD mutant assessed as inhibition of cell growth
Antiproliferative activity against human MOLM-13 cells harboring FLT3 ITD mutant assessed as inhibition of cell growth
|
[PMID: 37163951] |
| MV4-11 | IC50 |
0.015 μM
Compound: 32; LT-540-717
|
Antiproliferative activity against human MV4-11 cells harboring FLT3 ITD mutant assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay
Antiproliferative activity against human MV4-11 cells harboring FLT3 ITD mutant assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent assay
|
[PMID: 37163951] |
| NCI-H460 | GI50 |
<1 μM
Compound: 32; LT-540-717
|
Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth
Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth
|
[PMID: 37163951] |
| PBMC | IC50 |
831.3 nM
Compound: 32; LT-540-717
|
Cytotoxicity against human PBMC cells assessed as inhibition of cell growth
Cytotoxicity against human PBMC cells assessed as inhibition of cell growth
|
[PMID: 37163951] |
| SR | GI50 |
<1 μM
Compound: 32; LT-540-717
|
Antiproliferative activity against human SR cells assessed as inhibition of cell growth
Antiproliferative activity against human SR cells assessed as inhibition of cell growth
|
[PMID: 37163951] |
| SR | GI50 |
0.3 μM
Compound: 32; LT-540-717
|
Antiproliferative activity against human SR cells not addicted to FLT3 ITD mutant assessed as inhibition of cell growth
Antiproliferative activity against human SR cells not addicted to FLT3 ITD mutant assessed as inhibition of cell growth
|
[PMID: 37163951] |
| SW-620 | GI50 |
<1 μM
Compound: 32; LT-540-717
|
Antiproliferative activity against human SW-620 cells assessed as inhibition of cell growth
Antiproliferative activity against human SW-620 cells assessed as inhibition of cell growth
|
[PMID: 37163951] |
| THP-1 | IC50 |
903.5 nM
Compound: 32; LT-540-717
|
Antiproliferative activity against human THP-1 cells expressing wild type FLT3 assessed as inhibition of cell growth
Antiproliferative activity against human THP-1 cells expressing wild type FLT3 assessed as inhibition of cell growth
|
[PMID: 37163951] |
| U-937 | IC50 |
692.3 nM
Compound: 32; LT-540-717
|
Antiproliferative activity against human U-937 cells expressing low level wild type FLT3 assessed as inhibition of cell growth
Antiproliferative activity against human U-937 cells expressing low level wild type FLT3 assessed as inhibition of cell growth
|
[PMID: 37163951] |
化学情報
-
CAS 番号 2143089-35-2
-
分子量 456.50
-
分子式 C24H24N8O2
-
SMILES
O=C(NC1=CC=C(N2CCNCC2)C=C1)C3=NNC=C3NC4=NC=NC(OC5=CC=CC=C5)=C4
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)