Nilotinib
Based on 50 publication(s) in Google Scholar
Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.94%
- CAS No.: 641571-10-0
- Formule: C28H22F3N7O
- Masse moléculaire:529.52
-
Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Nilotinib
More- Nat Cancer. 2025 Apr;6(4):666-681. [Abstract]
- Cell Mol Immunol. 2024 Aug;21(8):856-872. [Abstract]
- Cancer Res. 2025 Jan 2;85(1):101-117. [Abstract]
- Nat Commun. 2026 Feb 24;17(1):1963. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Biomaterials. 2022 Oct:289:121800. [Abstract]
- Cell Rep Med. 2025 Apr 2:102053. [Abstract]
- Cancer Lett. 2024 Aug 1:217150. [Abstract]
- Cell Death Dis. 2021 Sep 25;12(10):875. [Abstract]
- Phytomedicine. 2025 Sep 25:148:157332. [Abstract]
- Cell Syst. 2018 Apr 25;6(4):424-443.e7. [Abstract]
- Biomed Pharmacother. 2025 Jun 20:189:118246. [Abstract]
- Br J Cancer. 2022 Mar;126(5):778-790. [Abstract]
- Talanta. 2026 Sep 1:307:129772. [Abstract]
- Ecotoxicol Environ Saf. 2025 Nov 15:307:119433. [Abstract]
- Breast Cancer Res. 2023 May 5;25(1):51. [Abstract]
- Glia. 2022 Jun;70(6):1084-1099. [Abstract]
- Stem Cell Reports. 2019 May 14;12(5):996-1006. [Abstract]
- Biomolecules. 2022 Jun 11;12(6):819. [Abstract]
- Eur J Pharmacol. 2021 Apr 15:897:173944. [Abstract]
- Toxicology. 2024 May 15:505:153830. [Abstract]
- Cancer Biol Ther. 2019;20(6):877-885. [Abstract]
- Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
- Target Oncol. 2020 Oct;15(5):659-671. [Abstract]
- J Pharm Sci. 2017 Sep;106(9):2632-2641. [Abstract]
- ACS Chem Biol. 2016 Apr 15;11(4):992-1000. [Abstract]
- Mol Med Rep. 2025 Jun;31(6):165. [Abstract]
- Cancer Med. 2016 Nov;5(11):3223-3234. [Abstract]
- Diseases. 2023 Oct 23;11(4):147. [Abstract]
- Toxicol Lett. 2022 Jul 15:365:11-23. [Abstract]
- PLoS One. 2024 Nov 1;19(11):e0308647. [Abstract]
- Drug Metab Pharmacokinet. 2020 Feb;35(1):102-110. [Abstract]
- Leuk Lymphoma. 2015;56(8):2416-23. [Abstract]
- Biomed Chromatogr. 2019 Dec;33(12):e4674. [Abstract]
- Int J Mass Spectrom. 442 (2019) 44-50.
- Xenobiotica. 2018 Oct;48(10):1059-1071. [Abstract]
- Res Sq. 2026 May 6.
- bioRxiv. 2026 Feb 20.
- Blood Vessel Thromb Hemost. 2025 Nov 17.
- bioRxiv. 2025 Sep 30.
- bioRxiv. 2025 February 26.
- bioRxiv. 2024 Dec 22:2024.12.21.629902. [Abstract]
- Research Square Preprint. 2024 Nov 06.
- bioRxiv. 2024 Dec 20:2024.12.19.629301. [Abstract]
- bioRxiv. 2024 May 8:2024.05.07.592424. [Abstract]
- bioRxiv. January 25, 2022.
- Patent. US20210299273A1.
- Patent. US20190084960A1
- Oncotarget. 2018 Apr 24;9(31):22158-22183. [Abstract]
- Technical University of Munich. 24.01.2018.
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Cell Proliferation/Viability Assay
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Cell Migration/Invasion Assay
-
IHC
-
Bio/Physico-chemical Assay
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Cell Proliferation/Viability Assay
Activité biologique
Bcr-Abl[1]
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
6.63 μM
Compound: 2
|
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
|
[PMID: 23521020] |
| BaF3 | IC50 |
>2000 nM
Compound: Chemical probe: AMN107
|
Cytotoxicity against mouse BaF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by methane-thiosulfonate-based CellTiter96 viability analysis
Cytotoxicity against mouse BaF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by methane-thiosulfonate-based CellTiter96 viability analysis
|
[PMID: 15930265] |
| BaF3 | IC50 |
25 nM
Compound: Tasigna, AMN107
|
Antiproliferative activity against BCR-ABL1 transfected mouse BA/F3 cells
Antiproliferative activity against BCR-ABL1 transfected mouse BA/F3 cells
|
[PMID: 20817538] |
| BaF3 | IC50 |
62 nM
Compound: Tasigna, AMN107
|
Antiproliferative activity against PDGFRbeta transfected mouse BA/F3 cells
Antiproliferative activity against PDGFRbeta transfected mouse BA/F3 cells
|
[PMID: 20817538] |
| BaF3 | IC50 |
>10000 nM
Compound: Tasigna, AMN107
|
Antiproliferative activity mouse BA/F3 cells in presence of interleukin 3
Antiproliferative activity mouse BA/F3 cells in presence of interleukin 3
|
[PMID: 20817538] |
| BaF3 | IC50 |
10 nM
Compound: Nilotinib
|
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 F317L mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 F317L mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
|
[PMID: 21481795] |
| BaF3 | IC50 |
10 nM
Compound: Nilotinib
|
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 V299L mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 V299L mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
|
[PMID: 21481795] |
| BaF3 | IC50 |
120 nM
Compound: Nilotinib
|
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 Y253H mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 Y253H mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
|
[PMID: 21481795] |
| BaF3 | IC50 |
17 nM
Compound: Nilotinib
|
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 T315A mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 T315A mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
|
[PMID: 21481795] |
| BaF3 | IC50 |
190 nM
Compound: Nilotinib
|
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 F359C mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 F359C mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
|
[PMID: 21481795] |
| BaF3 | IC50 |
2.1 nM
Compound: Nilotinib
|
Antiproliferative activity against native mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against native mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
|
[PMID: 21481795] |
| BaF3 | IC50 |
2800 nM
Compound: Nilotinib
|
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 T315I mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 T315I mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
|
[PMID: 21481795] |
| BaF3 | IC50 |
4.2 nM
Compound: Nilotinib
|
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 M351T mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 M351T mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
|
[PMID: 21481795] |
| BaF3 | IC50 |
49 nM
Compound: Nilotinib
|
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 H396P mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 H396P mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
|
[PMID: 21481795] |
| BaF3 | IC50 |
5.1 nM
Compound: Nilotinib
|
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 Q252H mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 Q252H mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
|
[PMID: 21481795] |
| BaF3 | IC50 |
63 nM
Compound: Nilotinib
|
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 Y253F mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 Y253F mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
|
[PMID: 21481795] |
| BaF3 | IC50 |
67 nM
Compound: Nilotinib
|
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 G250E mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 G250E mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
|
[PMID: 21481795] |
| BaF3 | IC50 |
80 nM
Compound: Nilotinib
|
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 E255K mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 E255K mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
|
[PMID: 21481795] |
| BaF3 | IC50 |
930 nM
Compound: Nilotinib
|
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 L248R mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 L248R mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
|
[PMID: 21481795] |
| BaF3 | IC50 |
95 nM
Compound: Nilotinib
|
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 E255V mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against mouse BaF3 cells harbouring BCR-ABL1 E255V mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
|
[PMID: 21481795] |
| BaF3 | IC50 |
9500 nM
Compound: Nilotinib
|
Antiproliferative activity against parent mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs in presence of IL-3 by MTT assay
Antiproliferative activity against parent mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs in presence of IL-3 by MTT assay
|
[PMID: 21481795] |
| BaF3 | IC50 |
1.54 nM
Compound: 2, AMN107
|
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M244V mutant after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M244V mutant after 72 hrs by CCK-8 assay
|
[PMID: 23088644] |
| BaF3 | IC50 |
10.3 nM
Compound: 2, AMN107
|
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M351T mutant after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl M351T mutant after 72 hrs by CCK-8 assay
|
[PMID: 23088644] |
| BaF3 | IC50 |
150 nM
Compound: 2, AMN107
|
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Q252H mutant after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Q252H mutant after 72 hrs by CCK-8 assay
|
[PMID: 23088644] |
| BaF3 | IC50 |
159 nM
Compound: 2, AMN107
|
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F359V mutant after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F359V mutant after 72 hrs by CCK-8 assay
|
[PMID: 23088644] |
| BaF3 | IC50 |
21 nM
Compound: 2, AMN107
|
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F486S mutant after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl F486S mutant after 72 hrs by CCK-8 assay
|
[PMID: 23088644] |
| BaF3 | IC50 |
292 nM
Compound: 2, AMN107
|
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255K mutant after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255K mutant after 72 hrs by CCK-8 assay
|
[PMID: 23088644] |
| BaF3 | IC50 |
314 nM
Compound: 2, AMN107
|
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253H mutant after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253H mutant after 72 hrs by CCK-8 assay
|
[PMID: 23088644] |
| BaF3 | IC50 |
38.6 nM
Compound: 2, AMN107
|
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl G250E mutant after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl G250E mutant after 72 hrs by CCK-8 assay
|
[PMID: 23088644] |
| BaF3 | IC50 |
40750 nM
Compound: 2, AMN107
|
Antiproliferative activity against mouse BA/F3 cells after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BA/F3 cells after 72 hrs by CCK-8 assay
|
[PMID: 23088644] |
| BaF3 | IC50 |
473 nM
Compound: 2, AMN107
|
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255V mutant after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E255V mutant after 72 hrs by CCK-8 assay
|
[PMID: 23088644] |
| BaF3 | IC50 |
6.34 nM
Compound: 2, AMN107
|
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396P mutant after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396P mutant after 72 hrs by CCK-8 assay
|
[PMID: 23088644] |
| BaF3 | IC50 |
60.7 nM
Compound: 2, AMN107
|
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253F mutant after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl Y253F mutant after 72 hrs by CCK-8 assay
|
[PMID: 23088644] |
| BaF3 | IC50 |
65.2 nM
Compound: 2, AMN107
|
Antiproliferative activity against mouse BA/F3 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BA/F3 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay
|
[PMID: 23088644] |
| BaF3 | IC50 |
775 nM
Compound: 2, AMN107
|
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 72 hrs by CCK-8 assay
|
[PMID: 23088644] |
| BaF3 | IC50 |
8.38 nM
Compound: 2, AMN107
|
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E355G mutant after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl E355G mutant after 72 hrs by CCK-8 assay
|
[PMID: 23088644] |
| BaF3 | IC50 |
87.2 nM
Compound: 2, AMN107
|
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396R mutant after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl H396R mutant after 72 hrs by CCK-8 assay
|
[PMID: 23088644] |
| BaF3 | IC50 |
0.003 μM
Compound: 2
|
Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL M351T mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL M351T mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
|
[PMID: 23301703] |
| BaF3 | IC50 |
0.0095 μM
Compound: 2
|
Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F486S mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F486S mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
|
[PMID: 23301703] |
| BaF3 | IC50 |
0.022 μM
Compound: 2
|
Cytotoxicity against mouse BA/F3 cells expressing wild type BCR-ABL assessed as growth inhibition after 72 hrs by CCK-8 assay
Cytotoxicity against mouse BA/F3 cells expressing wild type BCR-ABL assessed as growth inhibition after 72 hrs by CCK-8 assay
|
[PMID: 23301703] |
| BaF3 | IC50 |
0.12 μM
Compound: 2
|
Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E359V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E359V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
|
[PMID: 23301703] |
| BaF3 | IC50 |
0.12 μM
Compound: 2
|
Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Q252H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Q252H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
|
[PMID: 23301703] |
| BaF3 | IC50 |
0.13 μM
Compound: 2
|
Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E355G mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E355G mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
|
[PMID: 23301703] |
| BaF3 | IC50 |
0.15 μM
Compound: 2
|
Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL G250E mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL G250E mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
|
[PMID: 23301703] |
| BaF3 | IC50 |
0.16 μM
Compound: 2
|
Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317L mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317L mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
|
[PMID: 23301703] |
| BaF3 | IC50 |
0.17 μM
Compound: 2
|
Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255K mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255K mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
|
[PMID: 23301703] |
| BaF3 | IC50 |
1 μM
Compound: 2
|
Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253H mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
|
[PMID: 23301703] |
| BaF3 | IC50 |
1.2 μM
Compound: 2
|
Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL E255V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
|
[PMID: 23301703] |
| BaF3 | IC50 |
1.4 μM
Compound: 2
|
Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253F mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL Y253F mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
|
[PMID: 23301703] |
| BaF3 | IC50 |
15.1 μM
Compound: 2
|
Cytotoxicity against mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CCK-8 assay
Cytotoxicity against mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CCK-8 assay
|
[PMID: 23301703] |
| BaF3 | IC50 |
16 μM
Compound: 2
|
Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
|
[PMID: 23301703] |
| BaF3 | IC50 |
2.9 μM
Compound: 2
|
Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL F317V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
|
[PMID: 23301703] |
| BaF3 | IC50 |
21.1 μM
Compound: 2
|
Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL H396R mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL H396R mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
|
[PMID: 23301703] |
| BaF3 | IC50 |
3 μM
Compound: 2
|
Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL L248V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL L248V mutant assessed as growth inhibition after 72 hrs by CCK-8 assay
|
[PMID: 23301703] |
| BaF3 | IC50 |
>1 μM
Compound: 1
|
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 72 hrs by CCK-8 assay
|
[PMID: 26195136] |
| BaF3 | GI50 |
>10 μM
Compound: Nilotinib
|
Inhibition of BCR/ABL p210-T315I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
Inhibition of BCR/ABL p210-T315I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
|
[PMID: 26789553] |
| BaF3 | GI50 |
0.004 μM
Compound: Nilotinib
|
Inhibition of BCR/ABL p210 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
Inhibition of BCR/ABL p210 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
|
[PMID: 26789553] |
| BaF3 | GI50 |
0.017 μM
Compound: Nilotinib
|
Inhibition of BCR/ABL p210-M351T mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
Inhibition of BCR/ABL p210-M351T mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
|
[PMID: 26789553] |
| BaF3 | GI50 |
0.021 μM
Compound: Nilotinib
|
Inhibition of BCR/ABL p210-E255K mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
Inhibition of BCR/ABL p210-E255K mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
|
[PMID: 26789553] |
| BaF3 | GI50 |
0.023 μM
Compound: Nilotinib
|
Inhibition of BCR/ABL p210-Q252H mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
Inhibition of BCR/ABL p210-Q252H mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
|
[PMID: 26789553] |
| BaF3 | GI50 |
0.025 μM
Compound: Nilotinib
|
Inhibition of BCR/ABL p210-H369P mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
Inhibition of BCR/ABL p210-H369P mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
|
[PMID: 26789553] |
| BaF3 | GI50 |
0.0546 μM
Compound: Nilotinib
|
Inhibition of BCR/ABL p210-F317I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
Inhibition of BCR/ABL p210-F317I mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
|
[PMID: 26789553] |
| BaF3 | GI50 |
0.202 μM
Compound: Nilotinib
|
Inhibition of BCR/ABL p210-F317L mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
Inhibition of BCR/ABL p210-F317L mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
|
[PMID: 26789553] |
| BaF3 | GI50 |
0.47 μM
Compound: Nilotinib
|
Inhibition of TEL-SRC (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
Inhibition of TEL-SRC (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
|
[PMID: 26789553] |
| BaF3 | GI50 |
0.87 μM
Compound: Nilotinib
|
Inhibition of TEL-LCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
Inhibition of TEL-LCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
|
[PMID: 26789553] |
| BaF3 | GI50 |
1.093 μM
Compound: Nilotinib
|
Inhibition of BCR/ABL p210-Y253F mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
Inhibition of BCR/ABL p210-Y253F mutant (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
|
[PMID: 26789553] |
| BaF3 | GI50 |
1.1 μM
Compound: Nilotinib
|
Inhibition of TEL-DDR1 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
Inhibition of TEL-DDR1 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
|
[PMID: 26789553] |
| BaF3 | GI50 |
1.3 μM
Compound: Nilotinib
|
Inhibition of TEL-BLK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
Inhibition of TEL-BLK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
|
[PMID: 26789553] |
| BaF3 | GI50 |
1.4 μM
Compound: Nilotinib
|
Inhibition of TEL-DDR2 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
Inhibition of TEL-DDR2 (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
|
[PMID: 26789553] |
| BaF3 | GI50 |
2.1 μM
Compound: Nilotinib
|
Antiproliferative activity against mouse BA/F3 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay
Antiproliferative activity against mouse BA/F3 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay
|
[PMID: 26789553] |
| BaF3 | GI50 |
4.1 μM
Compound: Nilotinib
|
Inhibition of TEL-HCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
Inhibition of TEL-HCK (unknown origin) expressed in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo or CCK-8 assay
|
[PMID: 26789553] |
| BaF3 | IC50 |
2.7 μM
Compound: Nilotinib
|
Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant after 72 hrs by MTT assay
Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant after 72 hrs by MTT assay
|
[PMID: 26814890] |
| BaF3 | IC50 |
>100 nM
Compound: Nilotinib
|
Cytotoxicity against mouse BAF3 cells expressing BCR-ABL T315I mutant assessed as inhibition of cell growth measured after 48 hrs by trypan blue assay
Cytotoxicity against mouse BAF3 cells expressing BCR-ABL T315I mutant assessed as inhibition of cell growth measured after 48 hrs by trypan blue assay
|
[PMID: 34011155] |
| BaF3 | IC50 |
11.8 nM
Compound: Nilotinib
|
Cytotoxicity against mouse BAF3 cells expressing native BCR-ABL assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Cytotoxicity against mouse BAF3 cells expressing native BCR-ABL assessed as inhibition of cell growth measured after 72 hrs by MTT assay
|
[PMID: 34011155] |
| BJ | IC50 |
12.8 μM
Compound: Tasigna
|
Antiproliferative activity against human BJ cells after 72 hrs by PrestoBlue colorimetric assay
Antiproliferative activity against human BJ cells after 72 hrs by PrestoBlue colorimetric assay
|
[PMID: 24835982] |
| CHO | IC50 |
4.7 μM
Compound: nilotinib
|
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
|
[PMID: 23812503] |
| Daoy | IC50 |
6 μM
Compound: Nilotinib
|
Antiproliferative activity against human Daoy cells assessed as inhibition of cell growth incubated for 72 hrs by Alamar blue dye based fluorescence spectrophotometric assay
Antiproliferative activity against human Daoy cells assessed as inhibition of cell growth incubated for 72 hrs by Alamar blue dye based fluorescence spectrophotometric assay
|
[PMID: 33636537] |
| GIST882 | IC50 |
151 nM
Compound: Tasigna, AMN107
|
Antiproliferative activity against human GIST882 cells
Antiproliferative activity against human GIST882 cells
|
[PMID: 20817538] |
| H9c2 | IC50 |
21.33 μM
Compound: Nilotinib
|
Cytotoxicity against rat H9c2 cells incubated for 48 hrs and measured by MTT assay
Cytotoxicity against rat H9c2 cells incubated for 48 hrs and measured by MTT assay
|
[PMID: 36283251] |
| HCT-116 | IC50 |
2.39 μM
Compound: 2
|
Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay
Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay
|
[PMID: 23521020] |
| HCT-116 | IC50 |
5.75 μM
Compound: Nilotinib
|
Antiproliferative activity against human HCT-116 cells overexpressing DDR1 assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells overexpressing DDR1 assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
|
[PMID: 33246255] |
| HEK293 | IC50 |
3.7 nM
Compound: Tasigna, AMN107
|
Inhibition of autophosphorylation of DDR1 expressed in HEK293 cells by ELISA
Inhibition of autophosphorylation of DDR1 expressed in HEK293 cells by ELISA
|
[PMID: 20817538] |
| HEK293 | IC50 |
5.2 nM
Compound: Tasigna, AMN107
|
Inhibition of autophosphorylation of DDR2 expressed in HEK293 cells by ELISA
Inhibition of autophosphorylation of DDR2 expressed in HEK293 cells by ELISA
|
[PMID: 20817538] |
| HEK293 | IC50 |
677 nM
Compound: Tasigna, AMN107
|
Inhibition of autophosphorylation of CSF1R expressed in HEK293 cells by ELISA
Inhibition of autophosphorylation of CSF1R expressed in HEK293 cells by ELISA
|
[PMID: 20817538] |
| HEK293 | IC50 |
0.5 μM
Compound: nilotinib
|
Inhibition of the Organic Cation Transporter 3 (OCT3, SLC22A3) as assessed by a phenotypic impedance-based assay detecting changes in cell morphology by MPP+ uptake in HEK-293 JumpIN-SLC22A3 cells
Inhibition of the Organic Cation Transporter 3 (OCT3, SLC22A3) as assessed by a phenotypic impedance-based assay detecting changes in cell morphology by MPP+ uptake in HEK-293 JumpIN-SLC22A3 cells
|
[PMID: 35163125] |
| HEK293 | IC50 |
0.5 μM
Compound: nilotinib
|
Inhibition of the Organic Cation Transporter 3 (OCT3, SLC22A3) as assessed by a phenotypic impedance-based assay detecting changes in cell morphology by MPP+ uptake in HEK-293 JumpIN-SLC22A3 cells (PubChem AID: 1745861)
Inhibition of the Organic Cation Transporter 3 (OCT3, SLC22A3) as assessed by a phenotypic impedance-based assay detecting changes in cell morphology by MPP+ uptake in HEK-293 JumpIN-SLC22A3 cells (PubChem AID: 1745861)
|
[PMID: 35163125] |
| HEK293 | IC50 |
0.128 μM
Compound: 38
|
Cytotoxicity against HEK293 cells expressing ABCG2-482-R in presence of methotrexate
Cytotoxicity against HEK293 cells expressing ABCG2-482-R in presence of methotrexate
|
[PMID: 35944339] |
| HEK293 | IC50 |
0.147 μM
Compound: 38
|
Cytotoxicity against HEK293 cells expressing ABCG2-482-T7 in presence of methotrexate
Cytotoxicity against HEK293 cells expressing ABCG2-482-T7 in presence of methotrexate
|
[PMID: 35944339] |
| HEK293 | IC50 |
8.3 μM
Compound: AMN107
|
Cytotoxicity against HEK293 cells assessed as reduction in cell viability measured after 48 hrs by alamar blue assay
Cytotoxicity against HEK293 cells assessed as reduction in cell viability measured after 48 hrs by alamar blue assay
|
[PMID: 35944901] |
| HEK293 | IC50 |
8.4 μM
Compound: Nilotinib
|
Cytotoxicity against HEK293 cells incubated for 48 hrs and measured by MTT assay
Cytotoxicity against HEK293 cells incubated for 48 hrs and measured by MTT assay
|
[PMID: 36283251] |
| HEK293 | IC50 |
8.2 μM
Compound: Nilotinib
|
Cytotoxicity against HEK293 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against HEK293 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
|
[PMID: 38006642] |
| HEL | GI50 |
3.9 μM
Compound: Nilotinib
|
Antiproliferative activity against human HEL cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay
Antiproliferative activity against human HEL cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay
|
[PMID: 26789553] |
| Jurkat | IC50 |
>1000 nM
Compound: Nilotinib
|
Cytotoxicity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Cytotoxicity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
|
[PMID: 34011155] |
| K562 | IC50 |
21 nM
Compound: Tasigna, AMN107
|
Antiproliferative activity against human K562 cells
Antiproliferative activity against human K562 cells
|
[PMID: 20817538] |
| K562 | IC50 |
42 nM
Compound: Tasigna, AMN107
|
Inhibition of BCR-ABL1 autophosphorylation in human K562 cells
Inhibition of BCR-ABL1 autophosphorylation in human K562 cells
|
[PMID: 20817538] |
| K562 | IC50 |
260 nM
Compound: Nilotinib
|
Antiproliferative activity against human imatinib-resistant K562 cells
Antiproliferative activity against human imatinib-resistant K562 cells
|
[PMID: 21376587] |
| K562 | IC50 |
6.5 nM
Compound: Nilotinib
|
Antiproliferative activity against human K562 cells
Antiproliferative activity against human K562 cells
|
[PMID: 21376587] |
| K562 | IC50 |
0.015 μM
Compound: 2
|
Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay
Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay
|
[PMID: 23521020] |
| K562 | IC50 |
89.13 μM
Compound: Nilotinib
|
Antiproliferative activity against human K562 cells after 48 hrs by MTT assay
Antiproliferative activity against human K562 cells after 48 hrs by MTT assay
|
[PMID: 23538233] |
| K562 | IC50 |
2.4 μM
Compound: Tasigna
|
Antiproliferative activity against apoptosis-resistant, Philadelphia chromosome-positive human K562 cells after 72 hrs by PrestoBlue colorimetric assay
Antiproliferative activity against apoptosis-resistant, Philadelphia chromosome-positive human K562 cells after 72 hrs by PrestoBlue colorimetric assay
|
[PMID: 24835982] |
| K562 | IC50 |
0.022 μM
Compound: 1
|
Antiproliferative activity against human K562 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay
Antiproliferative activity against human K562 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay
|
[PMID: 26195136] |
| K562 | GI50 |
0.002 μM
Compound: Nilotinib
|
Antiproliferative activity against human K562 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay
Antiproliferative activity against human K562 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay
|
[PMID: 26789553] |
| K562 | IC50 |
0.0039 μM
Compound: Nilotinib
|
Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by MTT assay
Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by MTT assay
|
[PMID: 26814890] |
| K562 | IC50 |
<100 nM
Compound: Nilotinib
|
Inhibition of kinobead binding to DDR1 in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method
Inhibition of kinobead binding to DDR1 in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method
|
[PMID: 28280261] |
| K562 | IC50 |
1.8 μM
Compound: Nilotinib
|
Inhibition of kinobead binding to NQO2 in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method
Inhibition of kinobead binding to NQO2 in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method
|
[PMID: 28280261] |
| K562 | IC50 |
28 nM
Compound: Nilotinib
|
Inhibition of kinobead binding to ABL in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method
Inhibition of kinobead binding to ABL in human K562 cells incubated for 30 mins by iTRAQ reagent-based mass spectrometric method
|
[PMID: 28280261] |
| K562 | IC50 |
1.8 nM
Compound: Nilotinib
|
Cytotoxicity against human K562 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Cytotoxicity against human K562 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
|
[PMID: 34011155] |
| K562 | GI50 |
26 nM
Compound: AMN107
|
Growth inhibition of human K562 cells measured after 48 hrs by alamarblue assay
Growth inhibition of human K562 cells measured after 48 hrs by alamarblue assay
|
[PMID: 35944901] |
| K562 | GI50 |
>1000 nM
Compound: AMN107
|
Growth inhibition of human K562 cells expressing BCR-ABL T315I mutant measured after 48 hrs by alamarblue assay
Growth inhibition of human K562 cells expressing BCR-ABL T315I mutant measured after 48 hrs by alamarblue assay
|
[PMID: 35944901] |
| KBM5 | IC50 |
12 nM
Compound: NLT
|
Cytotoxicity against human KBM5 cells expressing IM- sensitive wild type Bcr/Abl assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human KBM5 cells expressing IM- sensitive wild type Bcr/Abl assessed as reduction in cell viability incubated for 48 hrs by MTT assay
|
[PMID: 31727471] |
| KBM5 | IC50 |
2421 nM
Compound: NLT
|
Cytotoxicity against human KBM5 cells expressing IM-resistant Bcr/Abl T315I mutant assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human KBM5 cells expressing IM-resistant Bcr/Abl T315I mutant assessed as reduction in cell viability incubated for 48 hrs by MTT assay
|
[PMID: 31727471] |
| KU812 cell line | IC50 |
3.4 nM
Compound: Nilotinib
|
Antiproliferative activity against human KU812 cells
Antiproliferative activity against human KU812 cells
|
[PMID: 21376587] |
| KU812 cell line | GI50 |
0.001 μM
Compound: Nilotinib
|
Antiproliferative activity against human KU812 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay
Antiproliferative activity against human KU812 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay
|
[PMID: 26789553] |
| KU812 cell line | IC50 |
10 nM
Compound: NLT
|
Cytotoxicity against human KU812 cells expressing IM- sensitive wild type Bcr/Abl assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human KU812 cells expressing IM- sensitive wild type Bcr/Abl assessed as reduction in cell viability incubated for 48 hrs by MTT assay
|
[PMID: 31727471] |
| KU812 cell line | IC50 |
1.8 nM
Compound: Nilotinib
|
Cytotoxicity against human KU812 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Cytotoxicity against human KU812 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
|
[PMID: 34011155] |
| L02 | IC50 |
40.39 μM
Compound: Nilotinib
|
Cytotoxicity against human L02 cells incubated for 48 hrs and measured by MTT assay
Cytotoxicity against human L02 cells incubated for 48 hrs and measured by MTT assay
|
[PMID: 36283251] |
| L02 | IC50 |
37.03 μM
Compound: Nilotinib
|
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
|
[PMID: 38006642] |
| MCF7 | IC50 |
6.92 μM
Compound: 2
|
Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
|
[PMID: 23521020] |
| MDA-MB-231 | IC50 |
7.31 μM
Compound: Nilotinib
|
Antiproliferative activity against human MDA-MB-231 cells overexpressing DDR1 assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells overexpressing DDR1 assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
|
[PMID: 33246255] |
| MDA-MB-435S | IC50 |
2.66 μM
Compound: 2
|
Antiproliferative activity against human MDA-MB-435S cells after 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-435S cells after 72 hrs by MTT assay
|
[PMID: 23521020] |
| MEG-01 | GI50 |
0.016 μM
Compound: Nilotinib
|
Antiproliferative activity against human MEG01 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay
Antiproliferative activity against human MEG01 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay
|
[PMID: 26789553] |
| MOLM-14 | GI50 |
>10 μM
Compound: Nilotinib
|
Antiproliferative activity against human MOLM14 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay
Antiproliferative activity against human MOLM14 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay
|
[PMID: 26789553] |
| MV4-11 | GI50 |
>10 μM
Compound: Nilotinib
|
Antiproliferative activity against human MV4-11 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay
Antiproliferative activity against human MV4-11 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay
|
[PMID: 26789553] |
| NCI-H2286 | IC50 |
1.8 μM
Compound: Nilotinib
|
Antiproliferative activity against human NCI-H2286 cells expressing DDR2 mutant after 72 hrs by alamar blue assay
Antiproliferative activity against human NCI-H2286 cells expressing DDR2 mutant after 72 hrs by alamar blue assay
|
[PMID: 26191369] |
| NCI-H23 | IC50 |
3.05 μM
Compound: 2
|
Antiproliferative activity against human NCI-H23 cells after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H23 cells after 72 hrs by MTT assay
|
[PMID: 23521020] |
| NCI-H460 | IC50 |
14.41 μM
Compound: 2
|
Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay
|
[PMID: 23521020] |
| NFS-60 | IC50 |
838 nM
Compound: Tasigna, AMN107
|
Antiproliferative activity against mouse M-NFS-60 cells
Antiproliferative activity against mouse M-NFS-60 cells
|
[PMID: 20817538] |
| SCH | IC50 |
14.6 μM
Compound: 3; AMN107
|
Antiproliferative activity against human SCH cells assessed as reduction in cell viability
Antiproliferative activity against human SCH cells assessed as reduction in cell viability
|
[PMID: 31923860] |
| Sf21 | IC50 |
0.158 μM
Compound: Nilotinib
|
Inhibition of recombinant human N-terminal GST-tagged c-Kit (544 to end residues) expressed in baculovirus infected Sf21 insect cells using FAM-labelled P22 peptide as substrate preincubated for 10 mins followed by substrate addition and measured after 1
Inhibition of recombinant human N-terminal GST-tagged c-Kit (544 to end residues) expressed in baculovirus infected Sf21 insect cells using FAM-labelled P22 peptide as substrate preincubated for 10 mins followed by substrate addition and measured after 1
|
[PMID: 32051094] |
| SH-SY5Y | IC50 |
38.51 μM
Compound: Nilotinib
|
Cytotoxicity against human SH-SY5Y cells incubated for 48 hrs and measured by MTT assay
Cytotoxicity against human SH-SY5Y cells incubated for 48 hrs and measured by MTT assay
|
[PMID: 36283251] |
| SH-SY5Y | IC50 |
38.69 μM
Compound: Nilotinib
|
Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
|
[PMID: 38006642] |
| T47D | IC50 |
6.08 μM
Compound: 2
|
Antiproliferative activity against human T47D cells after 72 hrs by MTT assay
Antiproliferative activity against human T47D cells after 72 hrs by MTT assay
|
[PMID: 23521020] |
| THP-1 | IC50 |
400 nM
Compound: Nilotinib
|
Antiinflammatory activity against LPS-stimulated human THP-1 cells assessed as TNF-alpha secretion pretreated for 1 hr followed by LPS stimulation and measured upto 24 hrs by ELISA analysis
Antiinflammatory activity against LPS-stimulated human THP-1 cells assessed as TNF-alpha secretion pretreated for 1 hr followed by LPS stimulation and measured upto 24 hrs by ELISA analysis
|
[PMID: 36094045] |
| U-937 | GI50 |
>10 μM
Compound: Nilotinib
|
Antiproliferative activity against human U937 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay
Antiproliferative activity against human U937 cells assessed as cell viability after 72 hrs by CellTiter-Glo or CCK-8 assay
|
[PMID: 26789553] |
| U-937 | IC50 |
>1000 nM
Compound: Nilotinib
|
Cytotoxicity against human U-937 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
Cytotoxicity against human U-937 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
|
[PMID: 34011155] |
Nilotinib (AMN107), selective Abl inhibitor, is designed to interact with the ATP-binding site of BCR-ABL with a higher affinity than imatinib while being significantly more potent compared with imatinib (IC50<30 nM), also maintains activity against most of the BCR-ABL point mutants that confer Imatinib resistance[1].
Nilotinib demonstrates significant antitumor efficacy against GIST xenograft lines and imatinib-resistant GIST cell lines which parent cell lines GK1C and GK3C shows imatinib sensitivity with IC50 of 4.59±0.97 μM and 11.15±1.48 μM, respectively, imatinib-resistant cell lines GK1C-IR and GK3C-IR shows Imatinib resistance with IC50 values of 11.74±0.17 μM (P<0.001) and 41.37±1.07 μM (P<0.001), respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Nilotinib has a significant healing effect on the macroscopic and microscopic pathologic scores and ensures considerable mucosal healing in the indomethacin-induced enterocolitis rat model while decreases the PDGFR α and β levels and apoptotic scores in the colon[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:BALB/cSLc-nu/nu mice with GIST xenograft (GK1X, GK2X and GK3X)[2]
-
Dosage:40 mg/kg
-
Administration:Oral gavage; daily; 4 weeks
-
Result:Inhibited tumor growth by 69.6% in GK1X, 85.3% in GK2X and 47.5% in GK3X xenograft line.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 641571-10-0
-
Appearance Solid
-
Masse moléculaire 529.52
-
Formule C28H22F3N7O
-
Color White to light yellow
-
SMILES
O=C(NC1=CC(C(F)(F)F)=CC(N2C=NC(C)=C2)=C1)C3=CC=C(C)C(NC4=NC=CC(C5=CC=CN=C5)=N4)=C3
-
Synonyms
AMN107
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (50)
-
Journal Impact Factor
-
Most Recent
-
Nat Cancer
A Gremlin 1-expressing splenic niche cell population restrains chronic myeloid leukemia by antagonizing the BMP pathway. [Abstract]2025 Apr;6(4):666-681. PMID: 40097655 -
Cell Mol Immunol
Chaperone- and PTM-mediated activation of IRF1 tames radiation-induced cell death and the inflammatory response. [Abstract]2024 Aug;21(8):856-872. PMID: 38849539 -
Cancer Res
Targeted Degradation of SOS1 Exhibits Potent Anticancer Activity and Overcomes Resistance in KRAS-Mutant Tumors and BCR-ABL-Positive Leukemia. [Abstract]2025 Jan 2;85(1):101-117. PMID: 39437162 -
Nat Commun
2026 Feb 24;17(1):1963. PMID: 41735331 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Biomaterials
2022 Oct:289:121800. PMID: 36166893 -
Cell Rep Med
CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. [Abstract]2025 Apr 2:102053. PMID: 40187357 -
Cancer Lett
Serotonylation in tumor-associated fibroblasts contributes to the tumor-promoting roles of serotonin in colorectal cancer. [Abstract]2024 Aug 1:217150. PMID: 39097134 -
Cell Death Dis
Combination of tyrosine kinase inhibitors and the MCL1 inhibitor S63845 exerts synergistic antitumorigenic effects on CML cells. [Abstract]2021 Sep 25;12(10):875. PMID: 34564697 -
Phytomedicine
Piperine targets SOAT1 to inhibit the progression of esophageal squamous cell carcinoma via ferroptosis. [Abstract]2025 Sep 25:148:157332. PMID: 41061292 -
Cell Syst
A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]2018 Apr 25;6(4):424-443.e7. PMID: 29655704 -
Biomed Pharmacother
Identification of nsp16 inhibitors of SARS -CoV-2, SARS -CoV-1 and MERS-CoV from FDA-approved drugs using in silico and in vitro methods. [Abstract]2025 Jun 20:189:118246. PMID: 40543162 -
Br J Cancer
PCK1 regulates neuroendocrine differentiation in a positive feedback loop of LIF/ZBTB46 signalling in castration-resistant prostate cancer. [Abstract]2022 Mar;126(5):778-790. PMID: 34815524 -
Talanta
A targeted strategy for screening bioactive inhibitors from Morus alba L.: Immobilized PTP1B affinity chromatography. [Abstract]2026 Sep 1:307:129772. PMID: 41955787 -
Ecotoxicol Environ Saf
PPARγ-responsive luciferase reporter system for high-throughput screening of chemical toxins with potential pulmonary fibrosis effects. [Abstract]2025 Nov 15:307:119433. PMID: 41273832 -
Breast Cancer Res
Systematic screening identifies ABCG2 as critical factor underlying synergy of kinase inhibitors with transcriptional CDK inhibitors. [Abstract]2023 May 5;25(1):51. PMID: 37147730 -
Glia
c-Abl-induced Olig2 phosphorylation regulates the proliferation of oligodendrocyte precursor cells. [Abstract]2022 Jun;70(6):1084-1099. PMID: 35156232 -
Stem Cell Reports
2019 May 14;12(5):996-1006. PMID: 31031187 -
Biomolecules
Investigating the Effect of Tyrosine Kinase Inhibitors on the Interaction between Human Serum Albumin by Atomic Force Microscopy. [Abstract]2022 Jun 11;12(6):819. PMID: 35740944 -
Eur J Pharmacol
Discovery of a highly potent kinase inhibitor capable of overcoming multiple imatinib-resistant ABL mutants for chronic myeloid leukemia (CML). [Abstract]2021 Apr 15:897:173944. PMID: 33581133 -
Toxicology
Phosphoproteomics reveals a novel mechanism underlying the proarrhythmic effects of nilotinib, vandetanib, and mobocertinib. [Abstract]2024 May 15:505:153830. PMID: 38754619 -
Cancer Biol Ther
Discovery and characterization of a novel highly potent and selective type II native and drug-resistant V299L mutant BCR-ABL inhibitor (CHMFL-ABL-039) for Chronic Myeloid Leukemia (CML). [Abstract]2019;20(6):877-885. PMID: 30894066
Nilotinib purchased from MedChemExpress. Usage Cited in: Cancer Biol Ther. 2019;20(6):877-885. [Abstract]
Nilotinib (0.1 μM; 15 days). The anti-colony formation effect of CHMFL-ABL-039 against K562, KU812, MEG-01, and BaF3-BCR-ABL-V299L cells was observed.
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Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
Target Oncol
In Vitro Comparison of the Effects of Imatinib and Ponatinib on Chronic Myeloid Leukemia Progenitor/Stem Cell Features. [Abstract]2020 Oct;15(5):659-671. PMID: 32780298 -
J Pharm Sci
Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites. [Abstract]2017 Sep;106(9):2632-2641. PMID: 28479358 -
ACS Chem Biol
2016 Apr 15;11(4):992-1000. PMID: 26741163 -
Mol Med Rep
Identification of the clinical value and biological effects of TTN mutation in liver cancer. [Abstract]2025 Jun;31(6):165. PMID: 40242970
Nilotinib purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2025 Jun;31(6):165. [Abstract]
CCK-8 assays were used to assess the IC50 of Nilotinib (0–20 μM) in JHH7, HepG2, Li7, Huh7, Hep3B, and SNU182 liver cancer cell lines over 48 h.
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Cancer Med
Direct effect of dasatinib on signal transduction pathways associated with a rapid mobilization of cytotoxic lymphocytes. [Abstract]2016 Nov;5(11):3223-3234. PMID: 27726309
Nilotinib purchased from MedChemExpress. Usage Cited in: Cancer Med. 2016 Nov;5(11):3223-3234. [Abstract]
Direct effect of dasatinib on cytotoxic lymphocytes. Mononuclear cells obtained from peripheral blood before taking dasatinib were incubated with dimethylsulfoxide (DMSO) vehicle, 100 nmol/L or 300 nmol/L dasatinib, 2 μmol/L imatinib, or 2 μmol/L Nilotinib, for 1 h.
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Diseases
Examining the Effects of Dasatinib, Sorafenib, and Nilotinib on Vascular Smooth Muscle Cells: Insights into Proliferation, Migration, and Gene Expression Dynamics. [Abstract]2023 Oct 23;11(4):147. PMID: 37873791 -
Toxicol Lett
Downregulation of hERG channel expression by tyrosine kinase inhibitors nilotinib and vandetanib predominantly contributes to arrhythmogenesis. [Abstract]2022 Jul 15:365:11-23. PMID: 35680041 -
PLoS One
A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]2024 Nov 1;19(11):e0308647. PMID: 39485774 -
Drug Metab Pharmacokinet
2020 Feb;35(1):102-110. PMID: 31732429 -
Leuk Lymphoma
ETV6/ARG oncoprotein confers autonomous cell growth by enhancing c-Myc expression via signal transducer and activator of transcription 5 activation in the acute promyelocytic leukemia cell line HT93A. [Abstract]2015;56(8):2416-23. PMID: 25373509
Nilotinib purchased from MedChemExpress. Usage Cited in: Leuk Lymphoma. 2015;56(8):2416-23. [Abstract]
Cell cycle analysis of HT93A cells by flow cytometry. Cells are treated with 100 nM Nilotinib and 50 ng/mL G-CSF alone or in combination for 48 h before the cell cycle is analyzed. Nilotinib treatment increases the fraction of cells in G0/G1 phase and decreased the S+G2/M-phase fraction.
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Biomed Chromatogr
UPLC-MS/MS study of the effect of dandelion root extract on the plasma levels of the selected irreversible tyrosine kinase inhibitors dasatinib, imatinib and nilotinib in rats: Potential risk of pharmacokinetic interactions. [Abstract]2019 Dec;33(12):e4674. PMID: 31376170 -
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Xenobiotica
Substrate-dependent effects of molecular-targeted anticancer agents on activity of organic anion transporting polypeptide 1B1. [Abstract]2018 Oct;48(10):1059-1071. PMID: 29034773 -
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bioRxiv
Leukemia escapes immunity by imposing a Type-1 regulatory program on neoantigen-specific CD4+ T cells. [Abstract]2024 Dec 22:2024.12.21.629902. PMID: 39764001 -
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bioRxiv
BRAFV600 and ErbB inhibitors directly activate GCN2 in an off-target manner to limit cancer cell proliferation. [Abstract]2024 Dec 20:2024.12.19.629301. PMID: 39763857 -
bioRxiv
2024 May 8:2024.05.07.592424. PMID: 38766123 -
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Oncotarget
2018 Apr 24;9(31):22158-22183. PMID: 29774130
Nilotinib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2018 Apr 24;9(31):22158-22183. [Abstract]
Primary tumors are dissected at the end of experiment and subjected to immunohistochemistry. Representative images of primary tumor sections stained with anti-PCNA (proliferation), anti-cleaved caspase 3 (apoptosis), and anti-CD31 (angiogenesis).
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Solvant et solubilité
1 M HCl : ≥ 100 mg/mL (188.85 mM)
DMSO : 12.5 mg/mL (23.61 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 4.17 mg/mL (7.88 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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-
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Weisberg E, et al. Beneficial effects of combining nilotinib and imatinib in preclinical models of BCR-ABL+ leukemias. Blood. 2007 Mar 1;109(5):2112-20. [Content Brief]
[2]. Sako H, et al. Antitumor effect of the tyrosine kinase inhibitor Nilotinib on gastrointestinal stromal tumor (GIST) and Imatinib-resistant GIST cells. PLoS One. 2014 Sep 15;9(9):e107613. [Content Brief]
[3]. Dervis Hakim G, et al. Mucosal healing effect of nilotinib in indomethacin-induced enterocolitis: A rat model. World J Gastroenterol. 2015 Nov 28;21(44):12576-85. [Content Brief]
[4]. Fujita KI, et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites. J Pharm Sci. 2017 Sep;106(9):2632-2641. [Content Brief]
[5]. Meirson T, et al. Targeting invadopodia-mediated breast cancer metastasis by using ABL kinase inhibitors. Oncotarget. 2018 Apr 24;9(31):22158-22183. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / 1 M HCl | 1 mM | 1.8885 mL | 9.4425 mL | 18.8850 mL | 47.2126 mL |
| 5 mM | 0.3777 mL | 1.8885 mL | 3.7770 mL | 9.4425 mL | |
| 10 mM | 0.1889 mL | 0.9443 mL | 1.8885 mL | 4.7213 mL | |
| 15 mM | 0.1259 mL | 0.6295 mL | 1.2590 mL | 3.1475 mL | |
| 20 mM | 0.0944 mL | 0.4721 mL | 0.9443 mL | 2.3606 mL | |
| 1 M HCl | 25 mM | 0.0755 mL | 0.3777 mL | 0.7554 mL | 1.8885 mL |
| 30 mM | 0.0630 mL | 0.3148 mL | 0.6295 mL | 1.5738 mL | |
| 40 mM | 0.0472 mL | 0.2361 mL | 0.4721 mL | 1.1803 mL | |
| 50 mM | 0.0378 mL | 0.1889 mL | 0.3777 mL | 0.9443 mL | |
| 60 mM | 0.0315 mL | 0.1574 mL | 0.3148 mL | 0.7869 mL | |
| 80 mM | 0.0236 mL | 0.1180 mL | 0.2361 mL | 0.5902 mL | |
| 100 mM | 0.0189 mL | 0.0944 mL | 0.1889 mL | 0.4721 mL |