Imatinib Mesylate
Based on 127 publication(s) in Google Scholar
Imatinib Mesylate (STI571 Mesylate) is an orally active tyrosine kinases inhibitor that inhibits c-Kit, Bcr-Abl, and PDGFR (IC50=100 nM) tyrosine kinases.
For research use only. We do not sell to patients.
- Purity: 99.93%
- CAS No.: 220127-57-1
- Formula: C30H35N7O4S
- Molecular Weight:589.71
-
Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) Imatinib Mesylate
More- Signal Transduct Target Ther. 2023 Mar 1;8(1):90. [Abstract]
- Cell Metab. 2022 Mar 1;34(3):424-440.e7. [Abstract]
- Cancer Commun (Lond). 2025 Nov 10. [Abstract]
- Nat Immunol. 2023 Sep;24(9):1443-1457. [Abstract]
- Nat Biomed Eng. 2018 Aug;2(8):578-588. [Abstract]
- Cancer Res. 2025 Jan 2;85(1):101-117. [Abstract]
- Bone Res. 2024 Apr 10;12(1):24. [Abstract]
- Nat Commun. 2025 Jul 24;16(1):6777. [Abstract]
- Nat Commun. 2025 Feb 14;16(1):1631. [Abstract]
- Exp Hematol Oncol. 2024 Dec 18;13(1):121. [Abstract]
- Sci Immunol. 2023 Mar 17;8(81):eade4656. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Nucleic Acids Res. 2021 Jan 8;49(D1):D1113-D1121. [Abstract]
- Theranostics. 2021 Jan 1;11(6):2691-2705. [Abstract]
- Adv Sci (Weinh). 2024 Sep;11(33):e2402107. [Abstract]
- Cell Rep Med. 2026 Mar 17;7(3):102686. [Abstract]
- Cell Rep Med. 2025 Apr 15;6(4):102053. [Abstract]
- Cell Death Dis. 2026 Apr 24;17(1):548. [Abstract]
- Cell Death Dis. 2022 Apr 20;13(4):384. [Abstract]
- Cancer Lett. 2026 Aug 10:653:218551. [Abstract]
- Cancer Lett. 2019 Apr 10:447:105-114. [Abstract]
- Mol Ther. 2023 Feb 1;31(2):503-516. [Abstract]
- Phytomedicine. 2024 Nov:134:155937. [Abstract]
- Clin Cancer Res. 2025 May 1;31(9):1686-1699. [Abstract]
- Clin Cancer Res. 2020 Aug 15;26(16):4349-4359. [Abstract]
- Acta Pharmacol Sin. 2023 May;44(5):984-998. [Abstract]
- J Transl Med. 2024 Dec 20;22(1):1119. [Abstract]
- Oncogene. 2024 Jun;43(27):2078-2091. [Abstract]
- Oncogene. 2022 Mar;41(12):1821-1834. [Abstract]
- Cell Chem Biol. 2018 Aug 16;25(8):996-1005.e4. [Abstract]
- BMC Med. 2022 Aug 24;20(1):257 [Abstract]
- EMBO J. 2025 Nov 3. [Abstract]
- Sensor Actuat B-Chem. 2021, 128991.
- Clin Chem. 2019 Dec;65(12):1522-1531. [Abstract]
- Clin Transl Med. 2025 Feb;15(2):e70231. [Abstract]
- EMBO Mol Med. 2021 Apr 9;13(4):e13144. [Abstract]
- ACS Appl Mater Interfaces. 2025 Jan 15;17(2):2884-2898. [Abstract]
- Inflamm Regen. 2022 Sep 26;42(1):44. [Abstract]
- Clin Sci. 2021 Jul 30;135(14):1751-1765. [Abstract]
- J Med Chem. 2021 Mar 11;64(5):2725-2738. [Abstract]
- J Med Chem. 2019 Jul 11;62(13):6083-6101. [Abstract]
- J Med Chem. 2019 May 23;62(10):5006-5024. [Abstract]
- J Med Chem. 2016 Sep 22;59(18):8456-72. [Abstract]
- Sci Signal. 2019 Jul 16;12(590):eaav7259. [Abstract]
- Pharmaceutics. 2023 Sep 12;15(9):2305. [Abstract]
- CNS Neurosci Ther. 2025 Dec;31(12):e70715. [Abstract]
- Ecotoxicol Environ Saf. 2025 Nov 15:307:119433. [Abstract]
- Cell Biosci. 2024 Jun 29;14(1):87. [Abstract]
- Biochem Pharmacol. 2023 Mar:209:115442. [Abstract]
- Cell Biosci. 2020 Feb 12:10:16. [Abstract]
- Gastric Cancer. 2023 Sep;26(5):677-690. [Abstract]
- Drug Des Devel Ther. 2022 Aug 4;16:2545-2557. [Abstract]
- J Biomed Inform. 2023 Jun:142:104383. [Abstract]
- Commun Biol. 2026 Feb 3;9(1):355. [Abstract]
- Commun Biol. 2024 Jul 10;7(1):843. [Abstract]
- Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
- Eur J Pharmacol. 2021 Dec 15:913:174633. [Abstract]
- Eur J Pharmacol. 2021 Sep 5:906:174217. [Abstract]
- Eur J Pharmacol. 2021 Apr 15:897:173944. [Abstract]
- Cancer Biol Ther. 2019;20(6):877-885. [Abstract]
- Int Immunopharmacol. 2026 Jul 1:180:116725. [Abstract]
- Int J Mol Sci. 2023 Feb 2;24(3):2849. [Abstract]
- Biomolecules. 2022 Jun 11;12(6):819. [Abstract]
- Stem Cell Reports. 2017 Dec 12;9(6):1948-1960. [Abstract]
- Microchem J. 2025 Apr.
- Sci Rep. 2025 May 30;15(1):18978. [Abstract]
- Sci Rep. 2025 Feb 8;15(1):4779. [Abstract]
- Curr Res Toxicol. 2024 Jul 14:7:100187. [Abstract]
- Mol Cell Biochem. 2020 Jan;463(1-2):67-78. [Abstract]
- Bioengineering (Basel). 2025 Oct 19;12(10):1121. [Abstract]
- Ther Adv Med Oncol. 2019 May 17:11:1758835919849757. [Abstract]
- J Tradit Complement Med. 2023 Nov 22;14(3):321-334. [Abstract]
- Viruses. 2021 May 31;13(6):1035. [Abstract]
- J Bioenerg Biomembr. 2012 Feb;44(1):155-61. [Abstract]
- PLoS Negl Trop Dis. 2019 Aug 20;13(8):e0007681. [Abstract]
- ChemMedChem. 2026 Jun 26;21(12):e70328. [Abstract]
- Mol Carcinog. 2026 Apr;65(4):407-421. [Abstract]
- Mol Carcinog. 2024 Jul;63(7):1334-1348. [Abstract]
- Mol Carcinog. 2024 Jan;63(1):75-93. [Abstract]
- Arch Pharm (Weinheim). 2022 Oct 10;e2200367. [Abstract]
- Cancer Med. 2019 Sep;8(11):5352-5366. [Abstract]
- Breast Cancer Res Treat. 2025 Jun;211(2):467-478. [Abstract]
- Toxicol Lett. 2022 Jul 15:365:11-23. [Abstract]
- Toxicol Lett. 2022 Jun 15:363:11-26. [Abstract]
- J Cell Biochem. 2023 Sep;124(9):1404-1422. [Abstract]
- Microvasc Res. 2025 Jul:160:104816. [Abstract]
- Hum Cell. 2025 Jan 3;38(2):38. [Abstract]
- PLoS One. 2024 Nov 1;19(11):e0308647. [Abstract]
- PLoS One. 2017 Jun 1;12(6):e0178619. [Abstract]
- Biochem Biophys Res Commun. 2025 Jul 22:771:152027. [Abstract]
- J Chromatogr B Analyt Technol Biomed Life Sci. 2025 Apr 1:1255:124526. [Abstract]
- J Chromatogr B Analyt Technol Biomed Life Sci. 2024 Apr 15:1237:124100. [Abstract]
- Med Sci Monit. 2017 Aug 6:23:3808-3816. [Abstract]
- Bioanalysis. 2018 Jul;10(14):1099-1113. [Abstract]
- Anticancer Drugs. 2014 Jul;25(6):673-82. [Abstract]
- In Vivo. 2024 Sep-Oct;38(5):2310-2317. [Abstract]
- Biomed Chromatogr. 2019 Dec;33(12):e4674. [Abstract]
- Res Sq. 2026 Jun 19.
- Res Sq. 2026 May 6.
- Res Sq. 2026 Apr 3.
- bioRxiv. 2026 Feb 20.
- Blood Vessel Thromb Hemost. 2025 Nov 17.
- bioRxiv. 2025 Sep 30.
- Biomed Pharmacother. 2025 Aug:189:118246. [Abstract]
- bioRxiv. 2025 Jul 12:2025.07.08.663754. [Abstract]
- University of Heidelberg. 2025.
- bioRxiv. 2025 Jun 13:2025.06.13.659082. [Abstract]
- Res Sq. 2025 Apr 14.
- bioRxiv. 2025 February 26.
- bioRxiv. 2024 Dec 20:2024.12.19.629301. [Abstract]
- Patent. US20240325538A1.
- Patent. US20240238271A1.
- Heliyon. 2024 Aug 22;10(16):e36640. [Abstract]
- bioRxiv. 2024 June 09.
- Biomed Pharmacother. 2024 Jan:170:115778. [Abstract]
- Research Square Preprint. 2023 Nov 20.
- Patent. US20230226111A1.
- Patent. US20230158019A1.
- J Pers Med. 2023 Jan 11;13(1):146. [Abstract]
- Patent. US20220288064A1.
- Patent. US20220242943A1.
- Patent. US20220064117A1.
- Research Square Preprint. 2021 May.
- Patent. US20200276189A1.
- Oncotarget. 2018 Apr 24;9(31):22158-22183. [Abstract]
- Oncotarget. 2017 Nov 15;8(67):111110-111118. [Abstract]
- Oncotarget. 2016 Jul 19;7(29):45562-45574. [Abstract]
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Biological Activity
IC50: ~100 nM (c-Kit, Bcr-Abl, and PDGFR)[1]
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
1.87 μM
Compound: Imatinib mesylate
|
Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by xCELLigence RTCA
Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by xCELLigence RTCA
|
[PMID: 32866755] |
| Bel-7402 | IC50 |
55.52 μM
Compound: Imatinib mesylate
|
Antiproliferative activity against human Bel-7402 cells assessed as reduction in cell viability incubated for 48 hrs by xCELLigence RTCA
Antiproliferative activity against human Bel-7402 cells assessed as reduction in cell viability incubated for 48 hrs by xCELLigence RTCA
|
[PMID: 32866755] |
| GIST882 | IC50 |
1.7 μM
Compound: Gleevec
|
Growth inhibition of human GIST882 cells expressing c-Kit after 96 hrs by SRB assay
Growth inhibition of human GIST882 cells expressing c-Kit after 96 hrs by SRB assay
|
[PMID: 24900212] |
| K562 | EC50 |
0.09 μM
Compound: 1, Gleevec
|
Antiproliferative activity against K562 cells expressing Bcr-Abl
Antiproliferative activity against K562 cells expressing Bcr-Abl
|
[PMID: 16678414] |
| K562 | IC50 |
0.21 μM
Compound: 1, gleevec
|
Cytotoxicity against human K562 cells after 24 hrs by MTT assay
Cytotoxicity against human K562 cells after 24 hrs by MTT assay
|
[PMID: 22000207] |
| K562 | IC50 |
0.31 μM
Compound: Imatinib mesylate
|
Cytotoxicity against human K562 cells measured after 72 hrs by MTT assay
Cytotoxicity against human K562 cells measured after 72 hrs by MTT assay
|
[PMID: 28075592] |
| KBM5 | IC50 |
152.2 nM
Compound: IM
|
Cytotoxicity against Imatinib mesylate sensitive wild-type human KBM5 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
Cytotoxicity against Imatinib mesylate sensitive wild-type human KBM5 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
|
[PMID: 34052717] |
| KBM5 | IC50 |
310.6 nM
Compound: IM
|
Cytotoxicity against imatinib mesylate resistant wild-type human KBM5 cells expressing T315I mutant assessed as cell growth inhibition measured after 48 hrs by MTT assay
Cytotoxicity against imatinib mesylate resistant wild-type human KBM5 cells expressing T315I mutant assessed as cell growth inhibition measured after 48 hrs by MTT assay
|
[PMID: 34052717] |
| KU812 cell line | EC50 |
0.6 μM
Compound: Imatinib mesylate
|
Cytotoxicity against human KU812 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against human KU812 cells assessed as reduction in cell viability after 48 hrs by MTT assay
|
[PMID: 29778892] |
| KU812 cell line | IC50 |
311.2 nM
Compound: IM
|
Cytotoxicity against Bcr-Abl expressing human KU812 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
Cytotoxicity against Bcr-Abl expressing human KU812 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
|
[PMID: 34052717] |
| LAMA-84 | IC50 |
100 nM
Compound: IM
|
Antiproliferative activity against human LAMA-84 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
Antiproliferative activity against human LAMA-84 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
|
[PMID: 28523104] |
| LAMA-84 | IC50 |
100 nM
Compound: IM
|
Antiproliferative activity against human LAMA-84 cells overexpressing BCR/ABL assessed as cell growth inhibition
Antiproliferative activity against human LAMA-84 cells overexpressing BCR/ABL assessed as cell growth inhibition
|
[PMID: 28523104] |
| MCF7 | IC50 |
0.83 μM
Compound: 1, gleevec
|
Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay
Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay
|
[PMID: 22000207] |
| MDA-MB-231 | IC50 |
1.8 μM
Compound: 1, gleevec
|
Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay
|
[PMID: 22000207] |
| MKN-45 | IC50 |
12.18 μM
Compound: Imatinib mesylate
|
Antiproliferative activity against human MKN-45 cells assessed as reduction in cell viability incubated for 48 hrs by xCELLigence RTCA
Antiproliferative activity against human MKN-45 cells assessed as reduction in cell viability incubated for 48 hrs by xCELLigence RTCA
|
[PMID: 32866755] |
| SGC-7901 | IC50 |
0.208 μM
Compound: Imatinib mesylate
|
Antiproliferative activity against human SGC7901 cells assessed as reduction in cell viability incubated for 48 hrs by xCELLigence RTCA
Antiproliferative activity against human SGC7901 cells assessed as reduction in cell viability incubated for 48 hrs by xCELLigence RTCA
|
[PMID: 32866755] |
| Vero C1008 | CC50 |
>100 μM
Compound: 13
|
Cytotoxicity against African green monkey Vero E6 cells
Cytotoxicity against African green monkey Vero E6 cells
|
[PMID: 33539089] |
| Vero C1008 | CC50 |
>30.86 μM
Compound: Imatinib Mesylate
|
CC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells
CC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells
|
10.1101/2020.03.25.008482 |
| Vero C1008 | CC50 |
>30.86 μM
Compound: Imatinib Mesylate
|
CC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells
CC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells
|
10.1101/2020.03.25.008482 |
| Vero C1008 | IC50 |
3.24 μM
Compound: Imatinib Mesylate
|
IC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells
IC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells
|
10.1101/2020.03.25.008482 |
| Vero C1008 | IC50 |
5.32 μM
Compound: Imatinib Mesylate
|
IC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells
IC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells
|
10.1101/2020.03.25.008482 |
Imatinib (STI571) Mesylate inhibits c-Kit autophosphorylation, activation of MAPK, and activation of Akt without altering total protein levels of c-kit, MAPK, or Akt. The concentration that produces 50% inhibition for these effects is approximately 100 nM[1]. Imatinib (STI571) mesylate is very effective (in vitro IC50 of 25 nM) against the chronic myeloid leukemia-causing kinase Bcr-Abl. Imatinib also efficiently inhibits Kit (in vitro IC50, 410 nM) and PDGFR (in vitro IC50, 380 nM)[2]. Imatinib (STI571) mesylate is a multi-target inhibitor of v-Abl, c-Kit and inhibits Bcr/Abl, v-Abl, Tel/Abl, the native PDGFβ receptor, and c-Kit, but it does not inhibit Src family kinases, c-Fms, Flt3, the EGFR or multiple other tyrosine kinases. Imatinib inhibits tyrosine phosphorylation and cell growth of Ba/F3 cells expressing Bcr/Abl, Tel/Abl, Tel/PDGFβR, and Tel/Arg with an IC50 of approximately 0.5 μM in each case, but it has no effect on untransformed Ba/F3 cells growing in IL-3 or on Ba/F3 cells transformed by Tel/JAK2[3]. Imatinib mesylate selectively inhibits the activity of Bcr/Abl, c-Kit and PDGFR kinases. Imatinib mesylate reveals distinct and rapid antileukemic activity in chronic myelogenous leukemia (CML) and Philadelphia-positive (Ph+) acute lymphoblastic leukemia (ALL)[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 220127-57-1
-
Appearance Solid
-
Molecular Weight 589.71
-
Formula C30H35N7O4S
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Color White to off-white
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SMILES
O=S(O)(C)=O.O=C(NC1=CC=C(C(NC2=NC=CC(C3=CC=CN=C3)=N2)=C1)C)C4=CC=C(CN5CCN(CC5)C)C=C4
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Synonyms
STI571 Mesylate; CGP-57148B Mesylate
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Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (127)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
TSPAN32 suppresses chronic myeloid leukemia pathogenesis and progression by stabilizing PTEN. [Abstract]2023 Mar 1;8(1):90. PMID: 36854750 -
Cell Metab
Imatinib and methazolamide ameliorate COVID-19-induced metabolic complications via elevating ACE2 enzymatic activity and inhibiting viral entry. [Abstract]2022 Mar 1;34(3):424-440.e7. PMID: 35150639 -
Cancer Commun (Lond)
Unfolded protein response kinase PERK supports survival and metastasis of circulating tumor cell clusters via SAM synthesis and H3K4me3-dependent PDGFB signaling. [Abstract]2025 Nov 10. PMID: 41212905 -
Nat Immunol
Fibrosis induced by resident macrophages has divergent roles in pancreas inflammatory injury and PDAC. [Abstract]2023 Sep;24(9):1443-1457. PMID: 37563309 -
Nat Biomed Eng
TLR7/8-agonist-loaded nanoparticles promote the polarization of tumour-associated macrophages to enhance cancer immunotherapy. [Abstract]2018 Aug;2(8):578-588. PMID: 31015631 -
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 -
Bone Res
Sorafenib inhibits ossification of the posterior longitudinal ligament by blocking LOXL2-mediated vascularization. [Abstract]2024 Apr 10;12(1):24. PMID: 38594260 -
Nat Commun
PEAK1 maintains tight junctions in intestinal epithelial cells and resists colitis by inhibiting autophagy-mediated ZO-1 degradation. [Abstract]2025 Jul 24;16(1):6777. PMID: 40707483 -
Nat Commun
2025 Feb 14;16(1):1631. PMID: 39952934 -
Exp Hematol Oncol
Chiglitazar diminishes the warburg effect through PPARγ/mTOR/PKM2 and increases the sensitivity of imatinib in chronic myeloid leukemia. [Abstract]2024 Dec 18;13(1):121. PMID: 39696470 -
Sci Immunol
Targeting the chromatin effector Pygo2 promotes cytotoxic T cell responses and overcomes immunotherapy resistance in prostate cancer. [Abstract]2023 Mar 17;8(81):eade4656. PMID: 36897957 -
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 -
Nucleic Acids Res
COVID19 Drug Repository: text-mining the literature in search of putative COVID19 therapeutics. [Abstract]2021 Jan 8;49(D1):D1113-D1121. PMID: 33166390 -
Theranostics
KDM6A promotes imatinib resistance through YY1-mediated transcriptional upregulation of TRKA independently of its demethylase activity in chronic myelogenous leukemia. [Abstract]2021 Jan 1;11(6):2691-2705. PMID: 33456567 -
Adv Sci (Weinh)
Overcoming the Tumor Collagen Barriers: A Multistage Drug Delivery Strategy for DDR1-Mediated Resistant Colorectal Cancer Therapy. [Abstract]2024 Sep;11(33):e2402107. PMID: 38953306 -
Cell Rep Med
FBXO3-mediated DUSP9 ubiquitination promotes leukemia stem cell maintenance and tyrosine kinase inhibitor resistance in chronic myeloid leukemia. [Abstract]2026 Mar 17;7(3):102686. PMID: 41850237 -
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 15;6(4):102053. PMID: 40187357 -
Cell Death Dis
RHBDL2 drives lipid metabolic reprogramming in osteosarcoma via USP3-mediated deubiquitination of PPT1. [Abstract]2026 Apr 24;17(1):548. PMID: 42031733 -
Cell Death Dis
Mitochondrial oxidative phosphorylation is dispensable for survival of CD34+ chronic myeloid leukemia stem and progenitor cells. [Abstract]2022 Apr 20;13(4):384. PMID: 35444236 -
Cancer Lett
2026 Aug 10:653:218551. PMID: 42066836 -
Cancer Lett
Repurposing cabozantinib to GISTs: Overcoming multiple imatinib-resistant cKIT mutations including gatekeeper and activation loop mutants in GISTs preclinical models. [Abstract]2019 Apr 10:447:105-114. PMID: 30684595 -
Mol Ther
Imatinib facilitates gemcitabine sensitivity by targeting epigenetically activated PDGFC signaling in pancreatic cancer. [Abstract]2023 Feb 1;31(2):503-516. PMID: 36384875 -
Phytomedicine
Celastrol induces DNA damage and cell death in BCR-ABL T315I-mutant CML by targeting YY1 and HMCES. [Abstract]2024 Nov:134:155937. PMID: 39255723 -
Clin Cancer Res
Predicting c-KIT Inhibitor Efficacy in Patient-Derived Models of Sinonasal Mucosal Melanomas through Integrated Histogram Analysis of Whole-Tumor DKI, IVIM, and DCE-MRI. [Abstract]2025 May 1;31(9):1686-1699. PMID: 39937224 -
Clin Cancer Res
AXL Mediates Cetuximab and Radiation Resistance Through Tyrosine 821 and the c-ABL Kinase Pathway in Head and Neck Cancer. [Abstract]2020 Aug 15;26(16):4349-4359. PMID: 32439698 -
Acta Pharmacol Sin
Circulating small extracellular vesicles promote proliferation and migration of vascular smooth muscle cells via AXL and MerTK activation. [Abstract]2023 May;44(5):984-998. PMID: 36450791 -
J Transl Med
ABL1‒YAP1 axis in intestinal stem cell activated by deoxycholic acid contributes to hepatic steatosis. [Abstract]2024 Dec 20;22(1):1119. PMID: 39707364 -
Oncogene
RAF1 facilitates KIT signaling and serves as a potential treatment target for gastrointestinal stromal tumor. [Abstract]2024 Jun;43(27):2078-2091. PMID: 38760447 -
Oncogene
2022 Mar;41(12):1821-1834. PMID: 35140331 -
Cell Chem Biol
Overcoming Resistance to Targeted Anticancer Therapies through Small-Molecule-Mediated MEK Degradation. [Abstract]2018 Aug 16;25(8):996-1005.e4. PMID: 29909991
Imatinib Mesylate purchased from MedChemExpress. Usage Cited in: Cell Chem Biol. 2018 Aug 16;25(8):996-1005.e4. [Abstract]
Negligible increases in caspase-3 activity or PARP-1 cleavage is observed in PC-9 GR NSCLC cells treated with DMSO, single agent PAC-1 (5 mM), or Osimertinib (Osi). In cells treated with PAC-1+Osimertinib, dramatic increases in caspase-3 activity is observed as early as 36 hr post treatment.
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BMC Med
2022 Aug 24;20(1):257 PMID: 35999600 -
EMBO J
Tyrosine kinase targeting uncovers oncogenic pathway plasticity in Tasmanian devil transmissible cancers. [Abstract]2025 Nov 3. PMID: 41184587 -
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Clin Chem
Discovering Cross-Reactivity in Urine Drug Screening Immunoassays through Large-Scale Analysis of Electronic Health Records. [Abstract]2019 Dec;65(12):1522-1531. PMID: 31578215 -
Clin Transl Med
SHP2 inhibition and adjuvant therapy synergistically target KIT-mutant GISTs via ERK1/2-regulated GSK3β/cyclin D1 pathway. [Abstract]2025 Feb;15(2):e70231. PMID: 39981588 -
EMBO Mol Med
Upfront admixing antibodies and EGFR inhibitors preempts sequential treatments in lung cancer models. [Abstract]2021 Apr 9;13(4):e13144. PMID: 33660397 -
ACS Appl Mater Interfaces
Bola-Amphiphilic Dendrimer Enhances Imatinib to Target Metastatic Ovarian Cancer via β-Catenin-HRP2 Signaling Axis. [Abstract]2025 Jan 15;17(2):2884-2898. PMID: 39752231 -
Inflamm Regen
Imatinib inhibits pericyte-fibroblast transition and inflammation and promotes axon regeneration by blocking the PDGF-BB/PDGFRβ pathway in spinal cord injury. [Abstract]2022 Sep 26;42(1):44. PMID: 36163271 -
Clin Sci
A novel epigenetic drug conjugating flavonoid and HDAC inhibitor confer suppression of acute myeloid leukemogenesis. [Abstract]2021 Jul 30;135(14):1751-1765. PMID: 34282832 -
J Med Chem
Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration. [Abstract]2021 Mar 11;64(5):2725-2738. PMID: 33619967 -
J Med Chem
Discovery of 2-(4-Chloro-3-(trifluoromethyl)phenyl)- N-(4-((6,7-dimethoxyquinolin-4-yl)oxy)phenyl)acetamide (CHMFL-KIT-64) as a Novel Orally Available Potent Inhibitor against Broad-Spectrum Mutants of c-KIT Kinase for Gastrointestinal Stromal Tumors. [Abstract]2019 Jul 11;62(13):6083-6101. PMID: 31250638 -
J Med Chem
Discovery of ( E)- N1-(3-Fluorophenyl)- N3-(3-(2-(pyridin-2-yl)vinyl)-1 H-indazol-6-yl)malonamide (CHMFL-KIT-033) as a Novel c-KIT T670I Mutant Selective Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs). [Abstract]2019 May 23;62(10):5006-5024. PMID: 31046271 -
J Med Chem
Discovery of N-((1-(4-(3-(3-((6,7-Dimethoxyquinolin-3-yl)oxy)phenyl)ureido)-2-(trifluoromethyl)phenyl)piperidin-4-yl)methyl)propionamide (CHMFL-KIT-8140) as a Highly Potent Type II Inhibitor Capable of Inhibiting the T670I "Gatekeeper" Mutant of cKIT Kinase. [Abstract]2016 Sep 22;59(18):8456-72. PMID: 27545040
Imatinib Mesylate purchased from MedChemExpress. Usage Cited in: J Med Chem. 2016 Sep 22;59(18):8456-72. [Abstract]
Effect of compounds 1 (Imatinib), 2 (Sunitinib), and 35 on cKIT mediated signaling pathways in GIST-T1 and GIST-5R cancer cell lines.
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Sci Signal
Application of a MYC degradation screen identifies sensitivity to CDK9 inhibitors in KRAS-mutant pancreatic cancer. [Abstract]2019 Jul 16;12(590):eaav7259. PMID: 31311847 -
Pharmaceutics
A Nucleus-Targeting WT1 Antagonistic Peptide Encapsulated in Polymeric Nanomicelles Combats Refractory Chronic Myeloid Leukemia. [Abstract]2023 Sep 12;15(9):2305. PMID: 37765274 -
CNS Neurosci Ther
High Shear Stress-Induced Endothelial Piezo1 Downregulation Promotes Intracranial Aneurysm Formation via the PDGF-BB/PDGFRβ Paracrine Signaling Pathway. [Abstract]2025 Dec;31(12):e70715. PMID: 41457305 -
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 -
Cell Biosci
Entry of ZSWIM4 to the nucleus is crucial for its inhibition of KIT and BMAL1 in gastrointestinal stromal tumors. [Abstract]2024 Jun 29;14(1):87. PMID: 38951864 -
Biochem Pharmacol
AMPK inhibition induces MCL1 mRNA destabilization via the p38 MAPK/miR-22/HuR axis in chronic myeloid leukemia cells. [Abstract]2023 Mar:209:115442. PMID: 36720359 -
Cell Biosci
Loss of PI3 kinase association improves the sensitivity of secondary mutation of KIT to Imatinib. [Abstract]2020 Feb 12:10:16. PMID: 32082541 -
Gastric Cancer
SPRY4 inhibits and sensitizes the primary KIT mutants in gastrointestinal stromal tumors (GISTs) to imatinib. [Abstract]2023 Sep;26(5):677-690. PMID: 37222910 -
Drug Des Devel Ther
The Flavagline Compound 1-(2-(dimethylamino)acetyl)-Rocaglaol Induces Apoptosis in K562 Cells by Regulating the PI3K/Akt/mTOR, JAK2/STAT3, and MAPK Pathways. [Abstract]2022 Aug 4;16:2545-2557. PMID: 35959422 -
J Biomed Inform
2023 Jun:142:104383. PMID: 37196989 -
Commun Biol
TGFBI promotes liver fibrosis through remodeling the profibrotic microenvironment by a positive feedback regulatory loop. [Abstract]2026 Feb 3;9(1):355. PMID: 41634371 -
Commun Biol
Glutathione determines chronic myeloid leukemia vulnerability to an inhibitor of CMPK and TMPK. [Abstract]2024 Jul 10;7(1):843. PMID: 38987326 -
Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
Eur J Pharmacol
Simvastatin potentiates the cell-killing activity of imatinib in imatinib-resistant chronic myeloid leukemia cells mainly through PI3K/AKT pathway attenuation and Myc downregulation. [Abstract]2021 Dec 15:913:174633. PMID: 34843676 -
Eur J Pharmacol
2021 Sep 5:906:174217. PMID: 34087223 -
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 -
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 -
Int Immunopharmacol
Inhibition of the PDGFRβ/MMP-9 pathway attenuates CUMS-induced blood-brain barrier disruption, neuroinflammation, and depressive-like behaviors. [Abstract]2026 Jul 1:180:116725. PMID: 42035550 -
Int J Mol Sci
Evaluation of In Vitro Distribution and Plasma Protein Binding of Selected Antiviral Drugs (Favipiravir, Molnupiravir and Imatinib) against SARS-CoV-2. [Abstract]2023 Feb 2;24(3):2849. PMID: 36769193 -
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 -
Stem Cell Reports
Inhibition of Farnesyltransferase Potentiates NOTCH-Targeted Therapy against Glioblastoma Stem Cells. [Abstract]2017 Dec 12;9(6):1948-1960. PMID: 29198824 -
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Sci Rep
Neddylation status determines the therapeutic sensitivity of tyrosine kinase inhibitors in chronic myeloid leukemia. [Abstract]2025 May 30;15(1):18978. PMID: 40447744 -
Sci Rep
SOCS2 inhibits the tumorigenesis of GISTs and increases the sensitivity of GISTs to imatinib by suppression of KIT activation. [Abstract]2025 Feb 8;15(1):4779. PMID: 39922931 -
Curr Res Toxicol
Toxicokinetics of a developmental toxicity test in zebrafish embryos and larvae: Relationship with drug exposure in humans and other mammals. [Abstract]2024 Jul 14:7:100187. PMID: 39104612 -
Mol Cell Biochem
Adipose-derived stem cell-conditioned medium protects fibroblasts at different senescent degrees from UVB irradiation damages. [Abstract]2020 Jan;463(1-2):67-78. PMID: 31602539 -
Bioengineering (Basel)
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Ther Adv Med Oncol
Axitinib overcomes multiple imatinib resistant cKIT mutations including the gatekeeper mutation T670I in gastrointestinal stromal tumors. [Abstract]2019 May 17:11:1758835919849757. PMID: 31205508 -
J Tradit Complement Med
Integrating single-cell and spatial transcriptomics to elucidate the crosstalk between cancer-associated fibroblasts and cancer cells in hepatocellular carcinoma with spleen-deficiency syndrome. [Abstract]2023 Nov 22;14(3):321-334. PMID: 38707923 -
Viruses
Bovine Parainfluenza Virus Type 3 (BPIV3) Enters HeLa Cells via Clathrin-Mediated Endocytosis in a Cholesterol- and Dynamin-Dependent Manner. [Abstract]2021 May 31;13(6):1035. PMID: 34072688 -
J Bioenerg Biomembr
Transport and cytotoxicity of the anticancer drug 3-bromopyruvate in the yeast Saccharomyces cerevisiae. [Abstract]2012 Feb;44(1):155-61. PMID: 22359102
Imatinib Mesylate purchased from MedChemExpress. Usage Cited in: J Bioenerg Biomembr. 2012 Feb;44(1):155-61. [Abstract]
Differences in sensitivity of PDR-mutants to 3-BP, Imatinib methanesulfonate, Daunorubicin and Rhodamine 6 G. Minimal medium (YNB) with sucrose.
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PLoS Negl Trop Dis
Identification of anti-flaviviral drugs with mosquitocidal and anti-Zika virus activity in Aedes aegypti. [Abstract]2019 Aug 20;13(8):e0007681. PMID: 31430351 -
ChemMedChem
Synthesis of Novel d-Glucopyranuronamide-Based Nucleos(t)ide Analogs Bearing (Triazolyl)methyl Phosph(on)ate Motifs With Anticancer and Antibacterial Potential. [Abstract]2026 Jun 26;21(12):e70328. PMID: 42315993 -
Mol Carcinog
AOC3 Loss Promotes Imatinib Resistance in GIST by Stabilizing HK2 and Enhancing H3K18la-Driven Myc Transcription. [Abstract]2026 Apr;65(4):407-421. PMID: 41570175 -
Mol Carcinog
Four and a half LIM domains 2 (FHL2) attenuates tumorigenesis of gastrointestinal stromal tumors (GISTs) by negatively regulating KIT signaling. [Abstract]2024 Jul;63(7):1334-1348. PMID: 38629424 -
Mol Carcinog
DDR1/2 enhance KIT activation and imatinib resistance of primary and secondary KIT mutants in gastrointestinal stromal tumors. [Abstract]2024 Jan;63(1):75-93. PMID: 37737519 -
Arch Pharm (Weinheim)
Synthetic flavagline derivative 1-chloroacetylrocaglaol promotes apoptosis in K562 erythroleukemia cells through miR-17-92 cluster genes. [Abstract]2022 Oct 10;e2200367. PMID: 36216575 -
Cancer Med
Aberrant accumulation of Dickkopf 4 promotes tumor progression via forming the immune suppressive microenvironment in gastrointestinal stromal tumor. [Abstract]2019 Sep;8(11):5352-5366. PMID: 31353847 -
Breast Cancer Res Treat
2025 Jun;211(2):467-478. PMID: 40055251 -
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 -
Toxicol Lett
A new strategy for the rapid identification and validation of direct toxicity targets of psoralen-induced hepatotoxicity. [Abstract]2022 Jun 15:363:11-26. PMID: 35597499 -
J Cell Biochem
Novel chemical scaffold as potential drug against Leishmania donovani: Integrated computational and experimental approaches. [Abstract]2023 Sep;124(9):1404-1422. PMID: 37566640 -
Microvasc Res
The role of the PDGF-BB/PDGFR-β signaling pathway in microcirculatory disturbances and BBB destruction after experimental subarachnoid hemorrhage in mice. [Abstract]2025 Jul:160:104816. PMID: 40345321 -
Hum Cell
Long non-coding RNA MSC-AS1 confers imatinib resistance of gastrointestinal stromal tumor cells by activating FNDC1 and ANLN-mediated PI3K/AKT pathway. [Abstract]2025 Jan 3;38(2):38. PMID: 39751699 -
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 -
PLoS One
Imatinib attenuates cardiac fibrosis by inhibiting platelet-derived growth factor receptors activation in isoproterenol induced model. [Abstract]2017 Jun 1;12(6):e0178619. PMID: 28570599
Imatinib Mesylate purchased from MedChemExpress. Usage Cited in: PLoS One. 2017 Jun 1;12(6):e0178619. [Abstract]
The protein expression of PDGF-A, PDGF-B, PDGF-C, and PDGF-D in hearts from mice treated with vehicle, Imatinib (IMA), ISO, IMA+ISO for one week is tested by Western blot.
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Biochem Biophys Res Commun
Tyrosine kinase inhibitors induce cardiotoxicity by causing Ca2+ overload through the inhibition of phosphoinositide 3-kinase activity. [Abstract]2025 Jul 22:771:152027. PMID: 40403685 -
J Chromatogr B Analyt Technol Biomed Life Sci
Imatinib and norimatinib therapeutic monitoring using dried blood spots: Analytical and clinical validation, and performance comparison of volumetric collection devices. [Abstract]2025 Apr 1:1255:124526. PMID: 39985852 -
J Chromatogr B Analyt Technol Biomed Life Sci
Simultaneous determination of 11 oral targeted antineoplastic drugs and 2 active metabolites by LC-MS/MS in human plasma and its application to therapeutic drug monitoring in cancer patients. [Abstract]2024 Apr 15:1237:124100. PMID: 38547701 -
Med Sci Monit
Platelet Derived Growth Factor Alpha (PDGFRα) Induces the Activation of Cardiac Fibroblasts by Activating c-Kit. [Abstract]2017 Aug 6:23:3808-3816. PMID: 28780584
Imatinib Mesylate purchased from MedChemExpress. Usage Cited in: Med Sci Monit. 2017 Aug 6:23:3808-3816. [Abstract]
The kinase activity of c-Kit is enhanced in an animal model of cardiac fibrosis. The lysates of heart tissues from a mice model treated with vehicle, Imatinib (IMA), ISO, or Imatinib + ISO for one week are analyzed for phosphorylation level of p-c-Kit (Tyr719) and total protein level of c-Kit. The western blotting results from one mouse in each group and the statistical analysis of the western blotting bands are shown.
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Bioanalysis
Ultra-performance LC-MS/MS study of the pharmacokinetic interaction of imatinib with selected vitamin preparations in rats. [Abstract]2018 Jul;10(14):1099-1113. PMID: 30047806 -
Anticancer Drugs
Killing multiple myeloma cells with the small molecule 3-bromopyruvate: implications for therapy. [Abstract]2014 Jul;25(6):673-82. PMID: 24557015 -
In Vivo
Protective Effects of Imatinib on a DSS-induced Colitis Model Through Regulation of Apoptosis and Inflammation. [Abstract]2024 Sep-Oct;38(5):2310-2317. PMID: 39187319 -
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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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 Aug:189:118246. PMID: 40543162 -
bioRxiv
2025 Jul 12:2025.07.08.663754. PMID: 40672312 -
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bioRxiv
2025 Jun 13:2025.06.13.659082. PMID: 40661463 -
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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 -
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Heliyon
Pharmaceutical inhibition of BCL6 ameliorates resistance to imatinib in chronic myeloid leukemia. [Abstract]2024 Aug 22;10(16):e36640. PMID: 39258188 -
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Biomed Pharmacother
C-kit controls blood-brain barrier permeability by regulating caveolae-mediated transcytosis after chronic cerebral hypoperfusion. [Abstract]2024 Jan:170:115778. PMID: 38141279 -
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J Pers Med
Microglia-Derived Spp1 Promotes Pathological Retinal Neovascularization via Activating Endothelial Kit/Akt/mTOR Signaling. [Abstract]2023 Jan 11;13(1):146. PMID: 36675807 -
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Oncotarget
2018 Apr 24;9(31):22158-22183. PMID: 29774130
Imatinib Mesylate 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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Oncotarget
Discovery of a highly selective KIT kinase primary V559D mutant inhibitor for gastrointestinal stromal tumors (GISTs). [Abstract]2017 Nov 15;8(67):111110-111118. PMID: 29340041
Imatinib Mesylate purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Nov 15;8(67):111110-111118. [Abstract]
In cell EC50 determination of CHMFL-KIT-031 with parental Colo320DM (KIT wt) and KIT V559D overexpressed Colo320DM cells.
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Oncotarget
Discovery and characterization of a novel potent type II native and mutant BCR-ABL inhibitor (CHMFL-074) for Chronic Myeloid Leukemia (CML). [Abstract]2016 Jul 19;7(29):45562-45574. PMID: 27322145
Solvent & Solubility
DMSO : 125 mg/mL (211.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 50 mg/mL (84.79 mM)
* "≥" 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.53 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.53 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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: PBS
Solubility: 100 mg/mL (169.57 mM); Clear solution; Need ultrasonic
Add each solvent one by one: Saline
Solubility: 100 mg/mL (169.57 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
-
-
-
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protocol
Tested A549 cells are placed in 96-well flat-bottom plates at a density of 5×103 cells per well 24 h before the addition of the test compounds. The cells are incubated for 96 h with two different concentrations (10 and 100 nM) of PRI-2191 and concurrently with various concentrations of Imatinib mesylate (10, 100, 1000 and 10,000 ng/mL) and other cytostatic drugs (Docetaxel (DTX) or Idarubicin (ID) : 0.1, 1, 10, 100 ng/mL; Cisplatin (CIS): 1, 10, 100, 1000 ng/mL). The sulforhodamine B (SRB) assay is performed to evaluate the cytotoxic effect. As a result, IC50 is calculated for each separate experiment in Cheburator 0.4, Dmitry Nevozhay software[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[4]
NOD/SCID female mice, 12-16 weeks old, body weight of 20-25 g, are used. Mice are subcutaneously (s.c.) inoculated in the right flank of the abdomen with A549 tumor cells suspension (5×106 cells in 0.2 mL of Hank’s medium per mouse, Day 0) and then are randomized into groups receiving varied combinations of vitamin D analogs and chemotherapeutics. One out of two experimental protocols is applied in the respective experiments: 1. The treatment is started from Day 7 after inoculation of tumor cells (when tumors become palpable). Imatinib mesylate is administered intraperitoneally (i.p.) at a dose of 75 mg/kg/day, daily for 19 days (from Days 7-25). PRI-2191 is administered s.c. or by oral gavage at a dose of 2 μg/kg/day, 3 times a week (on Days 7, 12, 14, 16, 19, 21 and 23). 2. The treatment is started from Day 7 after inoculation of tumor cells (when tumors become palpable). Imatinib mesylate is administered intraperitoneally (i.p.) at a dose of 50 mg/kg/day, daily for 13 days (from Days 7-19). PRI-2191 and PRI-2205 are administered s.c. at doses of 1 or 10 μg/kg/day, respectively, 3 times a week (on Days 7, 10, 12, 14, 17, 19, 21, 24 and 26). At the end of the experiments, blood is collected under anesthesia; then, the mice are sacrificed.
Rats[5]
Male Lewis rats weighing 270 to 320 g are used in the experiments. Imatinib mesylate (50 mg/kg) is injected intraperitoneally in the Imatinib group (n=7), and 0.5 mL of 20% DMSO without Imatinib is administered in the vehicle group (n=7). The dose of 25 mg/kg is preliminarily tested, and it produces a little improvement in lung function without statistical significance. The dose of 50 mg/kg and intraperitoneal administration are adopted based on this result and past reports. The animals undergo left thoracotomy, and the left hilum is occluded with a small metallic clamp. The occlusion is performed 20 minutes after Imatinib or vehicle administration. During clamping, the tidal volume (TV) and respiratory rate (RR) are adjusted to 8 mL/kg and 80 breaths/min, respectively. After 90 minutes of ischemia, the clamp is removed and reperfusion is maintained for 120 minutes. During reperfusion, blood flow and ventilation are restored in the bilateral lung. In the sham group (n=6), the animals are heparinized, thoracotomized, and ventilated for 210 minutes.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (278 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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Heinrich MC, et al. Inhibition of c-kit receptor tyrosine kinase activity by STI 571, a selective tyrosine kinase inhibitor. Blood. 2000 Aug 1;96(3):925-32. [Content Brief]
[2]. Guida T, et al. Sorafenib inhibits imatinib-resistant KIT and platelet-derived growth factor receptor beta gatekeeper mutants. Clin Cancer Res. 2007 Jun 1;13(11):3363-9. [Content Brief]
[3]. Okuda K, et al. ARG tyrosine kinase activity is inhibited by STI571.Blood. 2001 Apr 15;97(8):2440-8 [Content Brief]
[4]. Maj E, et al. Vitamin D Analogs Potentiate the Antitumor Effect of Imatinib Mesylate in a Human A549 Lung Tumor Model. Int J Mol Sci. 2015 Nov 13;16(11):27191-207. [Content Brief]
[5]. Tanaka S, et al. Protective Effects of Imatinib on Ischemia/Reperfusion Injury in Rat Lung. Ann Thorac Surg. 2016 Jul 23. pii: S0003-4975(16)30523-9 [Content Brief]
[6]. 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.6957 mL | 8.4787 mL | 16.9575 mL | 42.3937 mL |
| 5 mM | 0.3391 mL | 1.6957 mL | 3.3915 mL | 8.4787 mL | |
| 10 mM | 0.1696 mL | 0.8479 mL | 1.6957 mL | 4.2394 mL | |
| 15 mM | 0.1130 mL | 0.5652 mL | 1.1305 mL | 2.8262 mL | |
| 20 mM | 0.0848 mL | 0.4239 mL | 0.8479 mL | 2.1197 mL | |
| 25 mM | 0.0678 mL | 0.3391 mL | 0.6783 mL | 1.6957 mL | |
| 30 mM | 0.0565 mL | 0.2826 mL | 0.5652 mL | 1.4131 mL | |
| 40 mM | 0.0424 mL | 0.2120 mL | 0.4239 mL | 1.0598 mL | |
| 50 mM | 0.0339 mL | 0.1696 mL | 0.3391 mL | 0.8479 mL | |
| 60 mM | 0.0283 mL | 0.1413 mL | 0.2826 mL | 0.7066 mL | |
| 80 mM | 0.0212 mL | 0.1060 mL | 0.2120 mL | 0.5299 mL | |
| DMSO | 100 mM | 0.0170 mL | 0.0848 mL | 0.1696 mL | 0.4239 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.