CHMFL-ABL-121
CHMFL-ABL-121 is a highly potent type II ABL kinase inhibitor with IC50s of 2 nM and 0.2 nM against purified inactive ABL wt and T315I kinase protein, respectively.
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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: 2270879-07-5
- 分子式: C30H31F3N6OS
- 分子量:580.67
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
|
ABL wt 2 nM (IC50) |
ABL-T315I 0.2 nM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | EC50 |
<10 nM
Compound: 24
|
Inhibition of BCR/ABL T315I mutant (unknown origin) expressed in mouse BAF3 cells assessed as inhibition of BCR/ABL T315I mutant autophosphorylation at Y245 site after 1 hr by immunoblotting analysis
Inhibition of BCR/ABL T315I mutant (unknown origin) expressed in mouse BAF3 cells assessed as inhibition of BCR/ABL T315I mutant autophosphorylation at Y245 site after 1 hr by immunoblotting analysis
|
[PMID: 30317026] |
| BaF3 | EC50 |
<10 nM
Compound: 24
|
Inhibition of BCR/ABL T315I mutant (unknown origin) expressed in mouse BAF3 cells assessed as inhibition of CrkL phosphorylation after 1 hr by immunoblotting analysis
Inhibition of BCR/ABL T315I mutant (unknown origin) expressed in mouse BAF3 cells assessed as inhibition of CrkL phosphorylation after 1 hr by immunoblotting analysis
|
[PMID: 30317026] |
| BaF3 | EC50 |
<10 nM
Compound: 24
|
Inhibition of BCR/ABL T315I mutant (unknown origin) expressed in mouse BAF3 cells assessed as inhibition of ErK phosphorylation after 1 hr by immunoblotting analysis
Inhibition of BCR/ABL T315I mutant (unknown origin) expressed in mouse BAF3 cells assessed as inhibition of ErK phosphorylation after 1 hr by immunoblotting analysis
|
[PMID: 30317026] |
| BaF3 | EC50 |
<10 nM
Compound: 24
|
Inhibition of BCR/ABL T315I mutant (unknown origin) expressed in mouse BAF3 cells assessed as inhibition of STAT5 phosphorylation after 1 hr by immunoblotting analysis
Inhibition of BCR/ABL T315I mutant (unknown origin) expressed in mouse BAF3 cells assessed as inhibition of STAT5 phosphorylation after 1 hr by immunoblotting analysis
|
[PMID: 30317026] |
| BaF3 | GI50 |
<0.001 μM
Compound: 24
|
Inhibition of wild type C-terminal FLAG-tagged human TEL fused ABL (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of wild type C-terminal FLAG-tagged human TEL fused ABL (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
<0.001 μM
Compound: 24
|
Inhibition of wild type C-terminal FLAG-tagged human TEL fused CSF1R (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of wild type C-terminal FLAG-tagged human TEL fused CSF1R (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
0.002 μM
Compound: 24
|
Inhibition of wild type C-terminal FLAG-tagged human TEL fused FLT1 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of wild type C-terminal FLAG-tagged human TEL fused FLT1 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
0.002 μM
Compound: 24
|
Inhibition of wild type C-terminal FLAG-tagged human TEL fused PDGFRalpha (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of wild type C-terminal FLAG-tagged human TEL fused PDGFRalpha (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
0.002 μM
Compound: 24
|
Inhibition of wild type C-terminal FLAG-tagged human TEL fused VEGFR2 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of wild type C-terminal FLAG-tagged human TEL fused VEGFR2 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
0.003 μM
Compound: 24
|
Inhibition of wild type C-terminal FLAG-tagged human TEL fused ABL T315I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of wild type C-terminal FLAG-tagged human TEL fused ABL T315I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
0.004 μM
Compound: 24
|
Inhibition of wild type C-terminal FLAG-tagged human TEL fused FLT3 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of wild type C-terminal FLAG-tagged human TEL fused FLT3 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
0.006 μM
Compound: 24
|
Inhibition of BCR/ABL T315I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of BCR/ABL T315I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
0.007 μM
Compound: 24
|
Inhibition of wild type BCR/ABL (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of wild type BCR/ABL (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
0.008 μM
Compound: 24
|
Inhibition of wild type C-terminal FLAG-tagged human TEL fused PDGFRbeta (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of wild type C-terminal FLAG-tagged human TEL fused PDGFRbeta (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
0.015 μM
Compound: 24
|
Inhibition of BCR/ABL Q252H mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of BCR/ABL Q252H mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
0.017 μM
Compound: 24
|
Inhibition of BCR/ABL M351T mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of BCR/ABL M351T mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
0.018 μM
Compound: 24
|
Inhibition of BCR/ABL F317L mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of BCR/ABL F317L mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
0.025 μM
Compound: 24
|
Inhibition of BCR/ABL F317I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of BCR/ABL F317I mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
0.033 μM
Compound: 24
|
Inhibition of wild type C-terminal FLAG-tagged human TEL fused cKIT (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of wild type C-terminal FLAG-tagged human TEL fused cKIT (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
0.035 μM
Compound: 24
|
Inhibition of BCR/ABL H369P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of BCR/ABL H369P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
0.035 μM
Compound: 24
|
Inhibition of BCR/ABL H396P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of BCR/ABL H396P mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
0.036 μM
Compound: 24
|
Inhibition of wild type C-terminal FLAG-tagged human TEL fused FGFR2 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of wild type C-terminal FLAG-tagged human TEL fused FGFR2 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
0.042 μM
Compound: 24
|
Inhibition of wild type C-terminal FLAG-tagged human TEL fused FGFR1 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of wild type C-terminal FLAG-tagged human TEL fused FGFR1 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
0.073 μM
Compound: 24
|
Inhibition of wild type C-terminal FLAG-tagged human TEL fused FGFR3 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of wild type C-terminal FLAG-tagged human TEL fused FGFR3 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
0.075 μM
Compound: 24
|
Inhibition of wild type C-terminal FLAG-tagged human TEL fused FGFR4 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of wild type C-terminal FLAG-tagged human TEL fused FGFR4 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
0.103 μM
Compound: 24
|
Inhibition of BCR/ABL V299L mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of BCR/ABL V299L mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
0.12 μM
Compound: 24
|
Inhibition of wild type C-terminal FLAG-tagged human TEL fused EPHA2 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of wild type C-terminal FLAG-tagged human TEL fused EPHA2 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
0.18 μM
Compound: 24
|
Inhibition of BCR/ABL Y253F mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of BCR/ABL Y253F mutant (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
0.2 μM
Compound: 24
|
Inhibition of wild type C-terminal FLAG-tagged human TEL fused RET (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of wild type C-terminal FLAG-tagged human TEL fused RET (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
0.92 μM
Compound: 24
|
Inhibition of wild type C-terminal FLAG-tagged human TEL fused EPHA1 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of wild type C-terminal FLAG-tagged human TEL fused EPHA1 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
1.05 μM
Compound: 24
|
Inhibition of wild type C-terminal FLAG-tagged human TEL fused SRC (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of wild type C-terminal FLAG-tagged human TEL fused SRC (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
1.36 μM
Compound: 24
|
Inhibition of wild type C-terminal FLAG-tagged human TEL fused DDR1 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of wild type C-terminal FLAG-tagged human TEL fused DDR1 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
1.54 μM
Compound: 24
|
Inhibition of BCR fused DDR2 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of BCR fused DDR2 (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
2.34 μM
Compound: 24
|
Inhibition of wild type C-terminal FLAG-tagged human TEL fused BMX (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Inhibition of wild type C-terminal FLAG-tagged human TEL fused BMX (unknown origin) transfected in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
2.48 μM
Compound: 24
|
Antiproliferative activity in mouse BAF3 cells after 72 hrs by CCK8 assay
Antiproliferative activity in mouse BAF3 cells after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| BaF3 | GI50 |
2.48 μM
Compound: 6
|
Antiproliferative activity in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
Antiproliferative activity in mouse BAF3 cells assessed as growth inhibition after 72 hrs by CCK8 assay
|
[PMID: 32949955] |
| CHO | GI50 |
1.12 μM
Compound: 24
|
Antiproliferative activity in CHO cells after 72 hrs by CCK8 assay
Antiproliferative activity in CHO cells after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| HL-60 | GI50 |
0.87 μM
Compound: 24
|
Antiproliferative activity in human HL60 cells after 72 hrs by CCK8 assay
Antiproliferative activity in human HL60 cells after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| K562 | EC50 |
<10 nM
Compound: 24
|
Inhibition of BCR/ABL in human K562 cells assessed as inhibition of BCR/ABL autophosphorylation at Y245 site after 1 hr by immunoblotting analysis
Inhibition of BCR/ABL in human K562 cells assessed as inhibition of BCR/ABL autophosphorylation at Y245 site after 1 hr by immunoblotting analysis
|
[PMID: 30317026] |
| K562 | GI50 |
0.001 μM
Compound: 24
|
Antiproliferative activity in human K562 cells after 72 hrs by CCK8 assay
Antiproliferative activity in human K562 cells after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| KU812 cell line | GI50 |
0.003 μM
Compound: 24
|
Antiproliferative activity in human KU812 cells after 72 hrs by CCK8 assay
Antiproliferative activity in human KU812 cells after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| MEC1 | GI50 |
0.5 μM
Compound: 24
|
Antiproliferative activity in human MEC1 cells after 72 hrs by CCK8 assay
Antiproliferative activity in human MEC1 cells after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| MEG-01 | GI50 |
0.001 μM
Compound: 24
|
Antiproliferative activity in human MEG01 cells after 72 hrs by CCK8 assay
Antiproliferative activity in human MEG01 cells after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| OCI-AML2 | GI50 |
1.42 μM
Compound: 24
|
Antiproliferative activity in human OCI-AML2 cells after 72 hrs by CCK8 assay
Antiproliferative activity in human OCI-AML2 cells after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
| Sf9 | IC50 |
0.0002 μM
Compound: 24
|
Inhibition of inactive wild type His-tagged ABL T315I mutant (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells assessed as reduction in autophosphorylation preincubated for 60 mins followed by ATP addition measured after 8
Inhibition of inactive wild type His-tagged ABL T315I mutant (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells assessed as reduction in autophosphorylation preincubated for 60 mins followed by ATP addition measured after 8
|
[PMID: 30317026] |
| Sf9 | IC50 |
0.002 μM
Compound: 24
|
Inhibition of inactive wild type His-tagged ABL (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells assessed as reduction in autophosphorylation preincubated for 60 mins followed by ATP addition measured after 8 hrs by ADP-G
Inhibition of inactive wild type His-tagged ABL (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells assessed as reduction in autophosphorylation preincubated for 60 mins followed by ATP addition measured after 8 hrs by ADP-G
|
[PMID: 30317026] |
| Sf9 | IC50 |
0.017 μM
Compound: 24
|
Inhibition of active wild type His-tagged ABL (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells using ABLtide as substrate after 1 hr by ADP-Glo assay
Inhibition of active wild type His-tagged ABL (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells using ABLtide as substrate after 1 hr by ADP-Glo assay
|
[PMID: 30317026] |
| Sf9 | IC50 |
0.0002 μM
Compound: 24
|
Inhibition of active wild type His-tagged ABL T315I mutant (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells using ABLtide as substrate after 1 hr by ADP-Glo assay
Inhibition of active wild type His-tagged ABL T315I mutant (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells using ABLtide as substrate after 1 hr by ADP-Glo assay
|
[PMID: 30317026] |
| Sf9 | IC50 |
0.2 nM
Compound: 24
|
Inhibition of active wild type His-tagged ABL T315I mutant (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells using ABLtide as substrate after 1 hr by ADP-Glo assay
Inhibition of active wild type His-tagged ABL T315I mutant (229 to 500 residues) (unknown origin) expressed in baculovirus infected sf9 cells using ABLtide as substrate after 1 hr by ADP-Glo assay
|
[PMID: 30317026] |
| U-937 | GI50 |
0.78 μM
Compound: 24
|
Antiproliferative activity in human U937 cells after 72 hrs by CCK8 assay
Antiproliferative activity in human U937 cells after 72 hrs by CCK8 assay
|
[PMID: 30317026] |
CHMFL-ABL-121 dose-dependently inhibits BCRABL's auto-phosphorylation at Y245 site in K562 (EC50<10 nM),
MEG-01 (EC50<10 nM) and KU812 (EC50<30 nM) cells and also significantly blocks the phosphorylation of downstream signaling mediators STAT5, CrkL and ErK[1].
CHMFL-ABL-121 induces apoptosis and arrests cell cycle at G0/G1 phase[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
-
CAS 番号 2270879-07-5
-
分子量 580.67
-
分子式 C30H31F3N6OS
-
SMILES
O=C(NC1=CC(C(F)(F)F)=C(CN2CCN(C)CC2)C=C1)CCSC3=CC(NN=C4/C=C/C5=CC=CC=N5)=C4C=C3
-
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
[1]. Liu X, et al. Discovery of (E)-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)propanamide (CHMFL-ABL-121) as a highly potent ABL kinase inhibitor capable of overcoming a variety of ABL mutants including T315I for chronic myeloid leukemia. Eur J Med Chem. 2018 Dec 5;160:61-81. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)