Search Result
Results for "
BaF3 cells
" in MedChemExpress (MCE) Product Catalog:
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-18960
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CHZ868
5 Publications Verification
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JAK
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Cancer
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CHZ868 is a type II JAK2 inhibitor with an IC50 of 0.17 μM in EPOR JAK2 WT Ba/F3 cell.
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- HY-104010A
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ABL001 hydrochloride
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Bcr-Abl
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Cancer
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Asciminib (ABL001) hydrochloride is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC50 of 0.25 nM .
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- HY-104010
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ABL001
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Bcr-Abl
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Cancer
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Asciminib (ABL001) is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC50 of 0.25 nM .
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- HY-153724
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BI-2865
1 Publications Verification
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Ras
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Cancer
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BI-2865 is a none-covalent pan-KRAS Inhibitor. BI-2865 binds to WT, G12C, G12D, G12V and G13D mutant KRAS with KDs of 6.9, 4.5, 32, 26, 4.3 nM respectively. BI-2865 inhibits the proliferation of G12C, G12D or G12V mutant KRAS expressing BaF3 cells (mean IC50: roughly 140 nM) .
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- HY-121874
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JAK
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Cancer
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EP009 is a JAK3 inhibitor that selectively inhibits IL-2-mediated JAK3 tyrosine phosphorylation (IC50=10-20 μM in Kit225 cells) without affecting IL-3-induced JAK2 phosphorylation (up to 50 μM in BaF/3 cells). EP009 significantly reduced Kit225 cell viability (72 h, LD50=5.0 μM) while having no effect on BaF/3 cells. .
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- HY-164397
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Anaplastic lymphoma kinase (ALK)
Apoptosis
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Cancer
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XMU-MP-5 is a selective inhibitor for ALK. XMU-MP-5 inhibits ALK-mutated Ba/F3 cell with IC50s of 4-50 nM, and induces apoptosis in EML4-ALK Ba/F3. XMU-MP-5 exhibits antitumor efficacy in mice .
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- HY-156086
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Trk Receptor
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Cancer
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TRK-IN-24 (compound 10g) is a Trk Receptor inhibitor that inhibits TRKA, TRKC, TRKA G595R, TRKA G667C and TRKA F589L IC50s are 5.21, 4.51, 6.77, 1.42 and 6.13 nM respectively. TRK-IN-24 has antitumor efficacy in BaF3-CD74-NTRK1 G595R and BaF3-CD74-NTRK1 G667C xenograft models. TRK-IN-24 inhibits the proliferation of Ba/F3 cells transfected with single mutants such as SF, GK, and xDFG, with an IC50 of 1.43-47.56 nM .
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- HY-126287
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Trk Receptor
Apoptosis
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Cancer
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JND4135 is a Type II TRK inhibitor with IC50 values of 2.79, 3.19, and 3.01 nM against TRKA, TRKB, TRKC, respectively. JND4135 can overcome resistance from TRK xDFG and other mutant forms in the BaF3 stable model, inhibiting phosphorylation of both WT and xDFG mutant TRKs, along with their downstream signaling molecules. JND4135 can induce G0/G1 phase arrest and apoptosis in BaF3–CD74-TRKA-G667C cells. JND4135 shows tumor growth inhibition activity in the BaF3-CD74-TRKA-G667C mouse xenograft model .
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- HY-162427
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Syk
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Endocrinology
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NMS-0963 (compound 1) is an inhibitor of spleen tyrosine kinase (SYK) with an oral activity and IC50 value of 3 nM. NMS-0963 inhibits BaF3-TEL/SYK cell line proliferative at 27 nM .
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- HY-146210
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EGFR
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Cancer
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EGFR-IN-50 (Compound 9h) is a potent EGFR inhibitor against L858R resistance mutation (TEL-EGFR-L858R-BaF3: GI50=8 nM, TEL-EGFR-T790M-L858R-BaF3: GI50=6.03 μM). EGFR-IN-50 shows anti-proliferative activity to cancer cells .
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- HY-18952A
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FLT3
Apoptosis
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Cancer
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(Z)-SU5614 is a potent FLT3 inhibitor and selectively induces growth arrest, apoptosis, and cell cycle arrest in Ba/F3 and AML cell lines expressing a constitutively activated FLT3 .
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- HY-142680
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EGFR
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Cancer
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EGFR-IN-23 is a potent EGFR TKI (tyrosine kinase inhibitor) with an IC50 of 8.05 nM for BaF3/EGFR-DEL19/T790M/C797S cell (WO2021244502A1, compound 8) .
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- HY-155227B
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Anaplastic lymphoma kinase (ALK)
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Cancer
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ALK/EGFR-IN-3 is a dual inhibitor of ALK and EGFR. ALK/EGFR-IN-3 inhibits the cell proliferation of H1975, PC9, and Baf3-EML4-ALK cancer cell lines with IC50s of 0.1360, 0.0332, and 0.0339 μM, respectively .
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- HY-123450
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Bcr-Abl
Apoptosis
PDGFR
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Cancer
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S116836, a potent, orally active BCR-ABL tyrosine kinase inhibitor, blocks both wild-type as well as T315I Bcr-Abl. S116836 arrests the cells in the G0/G1 phase of cell cycle, induces apoptosis, increases ROS production, and decreases GSH production in BaF3/WT and BaF3/T315I cells. S116836 also inhibits SRC, LYN, HCK, LCK and BLK, and receptor tyrosine kinases such as FLT3, TIE2, KIT, PDGFR-β. Antitumor activies . S116836 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-161785
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Apoptosis
EGFR
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Cancer
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EGFR-IN-117 (Compound 8h) exhibits inhibitory activity against EGFR mutation, targets the tumor environment, and induces apoptosis of cancer cells. EGFR-IN-117 inhibits proliferations of H1975, PC-9, and EGFR mutant cells BaF3-EGFR L858R/T790M/C797S and BaF3– C797S/Del19/T790M, with IC50 of 13 nM, 19 nM, 1.2 nM and 1.3 nM, respectively. EGFR-IN-117 exhibits antitumor efficacy in mouse models .
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- HY-110026
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FLT3
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Cancer
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GTP-14564 is a tyrosine kinase inhibitor targeting to internal tandem duplication (ITD) and FLT3. GTP-14564 inhibits FLT3 ligand-dependent growth in Ba/F3 leukemia cells .
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- HY-163620
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FGFR
Apoptosis
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Cancer
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LHQ490 is a selective FGFR2 inhibitor, with an IC50 of 5.2 nM. LHQ490 efficiently inhibits the proliferation of BaF3-FGFR2 cells with an IC50 value of 1.4 nM. LHQ490 inhibits FGFR2-driven cancer cell proliferation and induces apoptosis of FGFR2-driven cancer cells .
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- HY-156467
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- HY-142517
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EGFR
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Cancer
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EGFR-IN-25 is a potent EGFR inhibitor with IC50s of 9 nM and 60 nM for BaF3 cells (EGFR DEL19/T790M/C797S) and A431 cells (WT), respectively .
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- HY-155046
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FGFR
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Cancer
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FGFR4-IN-14 (Compound 27i) is a FGFR4 inhibitor (IC50: 2.4 nM. FGFR4-IN-14 inhibits the proliferation of V550L and N535K mutant strains, with IC50s of 21 nM, 2.5 nM, 171 nM against huh7, BaF3/ETV6-FGFR4-V550L and BaF3/ETV6-FGFR4-N535K cells respectively. FGFR4-IN-14 has potent antitumor efficacy in the Huh7 xenograft model. FGFR4-IN-14 can be used for research of hepatocellular carcinoma (HCC) .
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- HY-104010R
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Bcr-Abl
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Cancer
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Asciminib (Standard) is the analytical standard of Asciminib. This product is intended for research and analytical applications. Asciminib (ABL001) is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC50 of 0.25 nM .
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- HY-147575
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TAM Receptor
c-Met/HGFR
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Cancer
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Axl-IN-8 (NO.1) is a potent AXL inhibitor, with an IC50 of <1 nM. Axl-IN-8 also inhibits c-MET, with an IC50 of 1-10 nM. Axl-IN-8 shows anti-proliferative activity against BaF3/TEL-AXL, MKN45, and EBC-1 cells, with IC50 values of <10, 226.6 and 120.3 nM, respectively .
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- HY-142922
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Bcr-Abl
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Cancer
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BCR-ABL-IN-4 is a BCR-ABL inhibitor with anticancer effects. BCR-ABL-IN-4 inhibits the cancer cell growth with IC50 values of 0.67 nM and 16 nM for K562 cells and BCR-ABL T315I transfected Ba/F3 cells, respectively (WO2021143927A1; compound 11) .
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- HY-155227A
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Anaplastic lymphoma kinase (ALK)
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Cancer
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ALK/EGFR-IN-2 is a potent dual inhibitor of ALK and EGFR. ALK/EGFR-IN-2 induces apoptosis and G0/G1 cell cycle arrest in cancer cells. ALK/EGFR-IN-2 significantly inhibits the cell proliferation of H1975, PC9, and Baf3-EML4-ALK cancer cell lines with IC50s of 0.0034, 0.0065, and 0.0018 μM, respectively .
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- HY-13491
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Trk Receptor
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Cancer
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GNF-5837 is a potent, selective, and orally bioavailable pan-tropomyosin receptor kinase (TRK) inhibitor which display antiproliferative effects in cellular Ba/F3 assays ( IC50 values of 7 nM, 9 nM and 11 nM for cells containing the fusion proteins Tel-TrkC, Tel-TrkB and Tel-TrkA, respectively) .
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- HY-12291
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HMSL 10017-101-1
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Raf
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Cancer
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HG6-64-1 is a potent and selective B-Raf inhibitor extracted from patent WO 2011090738 A2, example 9 (XI-1); has a IC50 of 0.09 μM on B-raf V600E transformed Ba/F3 cells.
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- HY-163453
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EGFR
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Cancer
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HER2-IN-19 (Compound 10e) is a potent inhibitor of HER2 and EGFR with IC50 values of 0.87 respectively and 3.5 nM. HER2-IN-19 has potent inhibitory activity against tumor cells, IC50 NCI-N87 = 1.63 nM, IC50 BT474= 15.17 nM, IC50 BaF3-HER2YVMA = 1.49 nM .
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- HY-163417
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EGFR
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Cancer
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HER2-IN-15 (Compound 1) is an inhibitor for HER2, which inhibits the Her YVMA exon 20 insertion mutation (HER2 YVMA) with an IC50 <200 nM. HER2-IN-15 inhibits proliferation of HER2 YVMA mutated BaF3 cells with an IC50 <200 nM and amliorates non-small-cell lung cancer (NSCLC) .
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- HY-163418
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EGFR
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Cancer
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HER2-IN-17 (Compound 2) is an inhibitor for HER2, which inhibits the Her YVMA exon 20 insertion mutation (HER2 YVMA) with an IC50 <200 nM. HER2-IN-17 inhibits proliferation of HER2 YVMA mutated BaF3 cells with an IC50 <200 nM and amliorates non-small-cell lung cancer (NSCLC) .
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- HY-163420
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EGFR
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Cancer
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HER2-IN-16 (Compound 14) is an inhibitor for HER2, which inhibits the Her YVMA exon 20 insertion mutation (HER2 YVMA) with an IC50 <200 nM. HER2-IN-16 inhibits proliferation of HER2 YVMA mutated BaF3 cells with an IC50 <200 nM and amliorates non-small-cell lung cancer (NSCLC) .
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- HY-156410
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FLT3
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Cancer
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FLT3-IN-23 (compound 15) is an inhibitor of JFMS-like tyrosine kinase 3 (FLT3) with an IC50 of 7.42 nM. FLT3-IN-23 has antiproliferative activities against BaF3 cells carrying various FLT3-TKD and FLT3-ITD-TKD mutations .
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- HY-156467A
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Anaplastic lymphoma kinase (ALK)
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Cancer
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ALK-IN-27 TFA is the TFA form of ALK-IN-27 (HY-156467). ALK-IN-27 (compound 1) is a potent ALK inhibitor. ALK-IN-27 shows antitumor activity. ALK-IN-27 has an IC50 of 2.7 nM for Ba/F3 CLIP1-LTK cells .
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- HY-112378
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FLT3
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Cancer
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D-65476 is an inhibitor of type Ⅲ receptor tyrosine kinase (Flt3). In the absence of IL-3, D-65476 inhibits the proliferation of TEL-Flt3 transfected BA/F3 cells (IC50= 0.2 μM), which can be used in the study of Flt3-driven leukemia .
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- HY-12083
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Bcr-Abl
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Cancer
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PPY-A is a potent T315I mutant and wild-type Abl kinases inhibitor with IC50s of 9 and 20 nM, respectively. PPY-A inhibits Ba⁄F3 cells transformed with wild-type Abl and Abl T315I mutantl with IC50s of 390 and 180 nM, respectively. PPY-A can be used for the research of chronic myeloid leukemia (CML) .
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- HY-159147
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PROTACs
ROS Kinase
Apoptosis
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Cancer
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SIAIS039 is an orally active c-ros oncogene 1 (ROS1)-specific PROTAC with DC50s of 154.46 nM, 126.47 nM, 143.69 nM for HCC78 cells, Ba/F3 expressing the CD74-ROS1 fusion and Ba/F3 expressing the SDC4-ROS1 fusion, respectively. SIAIS039 suppresses cell proliferation, induces cell cycle arrest and apoptosis, and inhibits clonogenicity against ROS1-positive cells. SIAIS039 demonstrates anti-tumour effects against ROS1-driven tumor growth vivo. SIAIS039 is composed of the ALK inhibitor Brigatinib (HY-12857), a linker EM-12 (HY-138793), and a VHL ligand E3 ubiquitin ligase 1-Butyne (Red: Brigatinib; Blue: VHL ligand; Black: linker) .
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- HY-155227
-
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Anaplastic lymphoma kinase (ALK)
EGFR
Apoptosis
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Cancer
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ALK/EGFR-IN-1 (Compound 8l) is an ALK/EGFR dual inhibitor that blocks the phosphorylation of EGFR and ALK. ALK/EGFR-IN-1 inhibits ALK/EGFR mutants respectively, with IC50 of 4.3 nM for EGFR L858R T790M in H1975 cells and EML4-ALK in BaF3 cells, respectively. and 3.6 nM. ALK/EGFR-IN-1 may be used in NSCLC research .
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- HY-162103
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TAM Receptor
Apoptosis
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Cancer
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Axl-IN-18 (compound 25c) is a potent and selective type II AXL inhibitor. Axl-IN-18 shows excellent AXL inhibitory activity (IC50=1.1 nM) and 343-fold selectivity over the highly homologous kinase MET in biochemical assays (IC50=377 nM). Axl-IN-18 significantly inhibits AXL-driven cell proliferation, dose-dependently suppresses 4T1 cell migration and invasion, and induces apoptosis. Axl-IN-18 shows noticeable antitumor efficacy in a BaF3/TEL-AXL xenograft model .
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-
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- HY-133551
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RET
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Cancer
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WF-47-JS03 is a potent and selective RET kinase inhibitor with IC50s of 1.7 nM and 5.3 nM for KIF5B-RET transfected Ba/F3 cells and CCDC6-RET transfected LC-2/ad lung cancer cells, respectively. WF-47-JS03 demonstrates >500-fold selectivity against kinase insert domain receptor (KDR). Effective brain penetration .
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- HY-131906
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JAK
FLT3
Apoptosis
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Cancer
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JAK2-IN-7 is a selective JAK2 inhibitor with IC50s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3 V617F cells, respectively. JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3. JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities .
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- HY-125845
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VH032-NH2; VHL ligand 1
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Ligands for E3 Ligase
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Cancer
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(S,R,S)-AHPC (VH032-NH2) is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells .
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- HY-101763B
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VH032-NH2 dihydrochloride; VHL ligand 1 dihydrochloride
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Ligands for E3 Ligase
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Cancer
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(S,R,S)-AHPC (VH032-NH2) dihydrochloride is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC dihydrochloride can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells .
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- HY-155302
-
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FLT3
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Cancer
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FLT3-IN-22 (compound 22f) is a potent FLT3 inhibitor with IC50 values of 0.941 nM and 0.199 nM for FLT3 and FLT3/D835Y, respectively. FLT3-IN-22 exhibits strong antiproliferative activity against MV4-11 cells and the mutant FLT kinase expressed Ba/F3 cell lines, including FLT-D835Y and FLT3-F691L .
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- HY-125834
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PROTACs
Bcr-Abl
Apoptosis
STAT
JAK
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Cancer
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GMB-475 is a potent BCR-ABL1 PROTAC based on Von Hippel-Lindau (VHL). GMB-475 targets the nutmeg pocket of ABL1 in an ectopic manner and degrades BCR-ABL1 protein through the ubiquitin proteasome pathway. GMB-475 inhibits the proliferation of human K562 cells and mouse Ba/F3 cells, and is used for the study of chronic myeloid leukemia. (Blue: VHL ligand (HY-125845); Black: Linker; Pink: BCR-ABL1 ligand (HY-11007)) .
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- HY-110402
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VH032-NH2 TFA; VHL ligand 1 TFA
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Ligands for E3 Ligase
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Cancer
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(S,R,S)-AHPC (VH032-NH2) TFA is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC TFA can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells .
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- HY-155358
-
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EGFR
Apoptosis
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Cancer
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Os30, a potent fourth-generation EGFR inhibitor, is a potent EGFRC797S-TK inhibitor with IC50 values of 18 nM and 113 nM for EGFRDel19/T790M/C797S TK and EGFRL858R/T790M/C797S TK, respectively. Os30 can suppress EGFR phosphorylation, arrest at G1 phase and induce the apoptosis of KC-0116 (BaF3-EGFRDel19/T790M/C797S) cells. Os30 shows potent antitumor efficacy on non-small cell lung cancer (NSCLC) with EGFmRC797S mutation .
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- HY-129550
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EGFR
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Cancer
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BI-4020 is a fourth-generation, orally active, and non-covalent EGFR tyrosine kinase inhibitor. BI-4020 inhibits not only the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines) but also the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC50=1 nM). BI-4020 also shows activity against EGFR wt (IC50=190 nM). BI-4020 shows high kinome selectivity and good DMPK properties .
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- HY-143445
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EGFR
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Cancer
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EGFR-IN-48 is a potent and orally active EGFR inhibitor with IC50s of 0.193 nM, 0.251 nM, 10.4 nM for EGFR d19/TM/CS, EGFR LR/TM/CS, EGFR WT, respectively. EGFR-IN-48 inhibits the proliferation of BaF3 EGFR del19/T790M/C797S and PC-9 EGFR del19/T790M/C797S cells with IC50s of 1.526, 66.7 nM, respectively .
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- HY-146807
-
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Trk Receptor
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Cancer
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Type II TRK inhibitor 1 is a potent TRK inhibitor, which inhibits various TRK fusion protein variants and wild type. Type II TRK inhibitor 1 exhibits antiproliferative activity against Ba/F3 cells harboring CD74-TRKA G667C and ETV6-TRKC G696C fusion proteins with IC50s of 6 nM and 1.7 nM, respectively . Type II TRK inhibitor 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-149965
-
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Trk Receptor
Apoptosis
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Cancer
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TRK-IN-23 (compound 24b) is a potent and orally active TRK inhibitor with IC50 values of 0.5 nM, 9 nM, 14 nM, 4.4 nM, and 4.8 nM against TRKA, TRKC, TRKA G595R, TRKA F589L, and TRKA G667C, respectively. TRK-IN-23 indues apoptosis of Ba/F3-TRKAG595Rand Ba/F3-TRKAG667C cells .
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- HY-163004
-
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Trk Receptor
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Cancer
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Type II TRK inhibitor 2 (compound 40l) is a selective type II TRK inhibitor with plasma stability and moderate hepatic microsomal stability. Type II TRK inhibitor 2 significantly inhibits Km-12, Ba/F3-TRKA G595R and Ba/F3-TRKA G667C cell proliferation (IC50: 4.1 nM, 41.5 nM, 1.4 nM). Type II TRK inhibitor 2 can be used to study NTRK fusion cancers .
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- HY-144451
-
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Trk Receptor
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Cancer
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TRK-IN-12 (Compound 9e) is a potent inhibitor of TRK (TRK G595R IC50 = 13.1 nM). TRK-IN-12 is a macrocyclic derivative compound. TRK-IN-12 shows significant antiproliferative activity in the Ba/F3-LMNA-NTRK1 cell line (IC50 = 0.080 μM). TRK-IN-12 has shown a better inhibitory effect (IC50 = 0.646 μM) than control agent LOXO-101 in Ba/F3-LMNA-NTRK1-G595R cell line .
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- HY-157432
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EGFR
Apoptosis
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Cancer
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EGFR-IN-97 (compound 6q) is a EGFR inhibitor. EGFR-IN-97 shows inhibitory activity against Ba/F3-EGFR L858R/T790M/C797S and Ba/F3-EGFR Del19/T790M/C797S cells, with IC50 values of 0.42 μM and 0.41 μM, respectively. EGFR-IN-97 can promote apoptosis of NCI-H1975-EGFR L858R/T790M/C797S cells at the concentration of 0.8 μM .
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- HY-131244
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Anaplastic lymphoma kinase (ALK)
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Cancer
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ALK-IN-9 (compound 40) is a potent ALK inhibitor. ALK-IN-9 inhibits cell proliferation with IC50s of <0.2 nM, <0.2 nM, 0.2 nM for Ba/F3-EML4-ALK, KM 12 (TPM3-TRKA), KG-l cell (OP2-FGFR1), respectively .
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- HY-149451
-
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RET
VEGFR
c-Myc
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Cancer
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SYHA1815 is an orally active RET inhibitor (IC50=0.9 nmol/L) with antitumor activity. SYHA1815 is more selective for RET than KDR (IC50=15.9 nmol/L). SYHA1815 arrests the G1 cell cycle and inhibits RET-driven cell proliferation by downregulating c-Myc .
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- HY-126619
-
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Others
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Infection
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Aspochalasin D is a co-metabolite originally isolated from A. microcysticus with aspochalasins A, B, and C, that is initially thought to be inactive. It has antibacterial activity against Gram-positive and Gram-negative bacteria at a concentration of 1 mg/ml.2 Aspochalasin D is more cytotoxic, via apoptosis, to Ba/F3-V12 cells in an IL-3-free medium than in an IL-3-containing medium (IC50s=0.49 and 1.9 μg/mL, respectively).
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- HY-161269
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EGFR
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Cancer
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EGFR-IN-101 (I-10) is a 2-phenylamino pyrimidine derivative. EGFR-IN-101 is a EGFR inhibitor. The IC50 values for EGFR L858R/T790M/C797S and Ba/F3-EGFR L858R/T790M/C797S are 33.26 and 106.4 nM, respectively. EGFR-IN-101 can be used IN the study of non-small cell lung cancer (NSCLC) .
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- HY-121852
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SCH-225336
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Cannabinoid Receptor
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Inflammation/Immunology
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SCH 336 is a potent, selective, inverse and orally active CB2 agonist. SCH 336 inhibits BaF3/CB2 migration. SCH 336 significantly inhibits the migration of leukocytes in vivo. SCH 336 blocks ovalbumin-induced lung eosinophilia in mice .
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Cat. No. |
Product Name |
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Classification |
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- HY-159147
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Azide
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SIAIS039 is an orally active c-ros oncogene 1 (ROS1)-specific PROTAC with DC50s of 154.46 nM, 126.47 nM, 143.69 nM for HCC78 cells, Ba/F3 expressing the CD74-ROS1 fusion and Ba/F3 expressing the SDC4-ROS1 fusion, respectively. SIAIS039 suppresses cell proliferation, induces cell cycle arrest and apoptosis, and inhibits clonogenicity against ROS1-positive cells. SIAIS039 demonstrates anti-tumour effects against ROS1-driven tumor growth vivo. SIAIS039 is composed of the ALK inhibitor Brigatinib (HY-12857), a linker EM-12 (HY-138793), and a VHL ligand E3 ubiquitin ligase 1-Butyne (Red: Brigatinib; Blue: VHL ligand; Black: linker) .
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