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Pathways Recommended:	Stem Cell/Wnt Cell Cycle/DNA Damage

Results for "

BaF3 cells

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Anaplastic lymphoma kinase (ALK) (6) Apoptosis (19) Bacterial (1) Bcr-Abl (7) c-Kit (3) c-Met/HGFR (1) c-Myc (1) Cannabinoid Receptor (1) Cytochrome P450 (1) EGFR (18) FGFR (3) FLT3 (8) HDAC (1) JAK (5) Ligands for E3 Ligase (3) PDGFR (1) PROTACs (2) Raf (1) Ras (1) RET (4) ROS Kinase (1) STAT (3) Syk (1) TAM Receptor (2) Trk Receptor (7) VEGFR (1)
By Research Areas:	Cancer (65) Endocrinology (1) Infection (1) Inflammation/Immunology (1)
Click Chemistry:	Azide (1)

Inhibitors & Agonists

Click Chemistry

Targets Recommended: Nuclear Factor of activated T Cells (NFAT) TREM receptor Programmed Cell Death 4 (PDCD4)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-18960

CHZ868 5 Publications Verification	JAK	Cancer
CHZ868 is a type II JAK2 inhibitor with an IC₅₀ of 0.17 μM in EPOR JAK2 WT Ba/F3 cell.

HY-104010A

Asciminib hydrochloride Maximum Cited Publications 8 Publications Verification ABL001 hydrochloride	Bcr-Abl	Cancer
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 .

HY-104010

Asciminib Maximum Cited Publications 8 Publications Verification ABL001	Bcr-Abl	Cancer
Asciminib (ABL001) is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC₅₀ of 0.25 nM .

HY-153724

BI-2865 5 Publications Verification	Ras	Cancer
BI-2865 is a none-covalent pan-KRAS Inhibitor. BI-2865 binds to WT, G12C, G12D, G12V and G13D mutant KRAS with K_Ds 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) .

HY-121874

EP009	JAK	Cancer
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. .

HY-164397

XMU-MP-5	Anaplastic lymphoma kinase (ALK) Apoptosis	Cancer
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 .

HY-156086

TRK-IN-24	Trk Receptor	Cancer
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 .

HY-126287

JND4135	Trk Receptor Apoptosis	Cancer
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 .

HY-162427

NMS-0963	Syk	Endocrinology
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 .

HY-162881

DS06652923	EGFR	Cancer
DS06652923 is an orally active EGFR triple mutation inhibitor. DS06652923 has a growth inhibition effect on Ba/F3 EGFR del19/T90M/C797S cells, with a GI₅₀ value of 9.4 nM. DS06652923 can lead to tumor regression in Ba/F3 xenograft models .

HY-146210

EGFR-IN-50	EGFR	Cancer
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 .

HY-18952A

(Z)-SU5614	FLT3 Apoptosis	Cancer
(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 .

HY-142680

EGFR-IN-23	EGFR	Cancer
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) .

HY-155227B

ALK/EGFR-IN-3	Anaplastic lymphoma kinase (ALK)	Cancer
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 .

HY-123450

S116836	Bcr-Abl Apoptosis PDGFR	Cancer
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.

HY-161785

EGFR-IN-117	Apoptosis EGFR	Cancer
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 .

HY-110026

GTP-14564	FLT3	Cancer
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 .

HY-163620

LHQ490	FGFR Apoptosis	Cancer
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 .

HY-168579

c-Kit-IN-6	c-Kit	Cancer
c-Kit-IN-6 (Compound 101) is an inhibitor of c-Kit with an IC₅₀ value ranging between 100 nM and 1 μM. Additionally, c-Kit-IN-6 can inhibit the proliferation of GIST430 and BaF3 mutant cells .

HY-142517

EGFR-IN-25	EGFR	Cancer
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 .

HY-155046

FGFR4-IN-14	FGFR	Cancer
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) .

HY-104010R

Asciminib (Standard)	Bcr-Abl	Cancer
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 .

HY-168581

c-Kit-IN-8	c-Kit	Cancer
c-Kit-IN-8 (Compound 53) is an inhibitor for c-Kit kinase, that inhibits uKIT kinase with an IC₅₀ > 1 μM. c-Kit-IN-8 inhibits the proliferation of cancer cell GIST430 and BaF3 wildtype and mutants with IC₅₀ > 0.1 μM .

HY-147575

Axl-IN-8	TAM Receptor c-Met/HGFR	Cancer
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 .

HY-142922

BCR-ABL-IN-4	Bcr-Abl	Cancer
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) .

HY-170927

JAK-IN-40	JAK STAT Apoptosis	Cancer
JAK-IN-40 (Compound 46) is the inhibitor for JAK that inhibits JAK1, JAK2 and JAK3 with IC₅₀s of 0.022, 0.759 and 1.601 μM, respectively. JAK-IN-40 inhibits the phosphorylation of STAT3. JAK-IN-40 inhibits the proliferation of cancer cell Ba/F3 and JAK1-TEL Ba/F3 with GI₅₀ of 0.614 μM and 0.193 μM. JAK-IN-40 arrests cell cycle of H1975 and H2087 at G2/M phase, induces apoptosis. JAK-IN-40 exhibits a synergistic antitumor effect with Osimertinib (HY-15772) .

HY-155227A

ALK/EGFR-IN-2	Anaplastic lymphoma kinase (ALK)	Cancer
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 .

HY-12291

HG6-64-1 HMSL 10017-101-1	Raf	Cancer
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.

HY-13491

GNF-5837 3 Publications Verification	Trk Receptor	Cancer
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) .

HY-163453

HER2-IN-19	EGFR	Cancer
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 .

HY-168580

c-Kit-IN-7	c-Kit	Cancer
c-Kit-IN-7 (Compound 104) is a potent inhibitor of c-Kit, with IC₅₀ values of ≤10 nM. c-Kit-IN-7 inhibits the cell proliferation in GIST430 and BaF3 mutants, with IC₅₀ values of ≤100 nM. c-Kit-IN-7 plays an important role in cancer driven by c-KIT kinase mutations research .

HY-170809

RET-IN-29	RET	Cancer
RET-IN-29 (Compound 8W) is a selective RET kinase inhibitor. RET-IN-29 exhibits inhibitory potency against the BaF3 cells harboring CCDC6-RET ^V804M mutation with an IC₅₀ value of 0.715 μM. RET-IN-29 is promising for research of non-small cell lung cancer (NSCLC) .

HY-163418

HER2-IN-17	EGFR	Cancer
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) .

HY-163417

HER2-IN-15	EGFR	Cancer
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) .

HY-163420

HER2-IN-16	EGFR	Cancer
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) .

HY-170926

CQ1373	RET Apoptosis	Cancer
CQ1373 is a potent RET inhibitor, demonstrating cellular potency with IC₅₀ values of 13.0, 25.7 and 28.4 nM against BaF3 cells expressing CCDC6-RET, CCDC6-RET-G810C and CCDC6-RET-G810R, respectively. CQ1373 exhibits good selectivity toward wild-type RET and solvent front mutants G810C/R with IC₅₀ values of 4.2, 7.1 and 32.4 nM, respectively. CQ1373 inhibits RET phosphorylation and downstream signaling through SHC. CQ1373 induces Apoptosis and cell cycle arrest in BaF3 cells. CQ1373 exhibits anti-tumor efficacy and can be used for cancer research .

HY-112378

D-65476	FLT3	Cancer
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 .

HY-156410

FLT3-IN-23	FLT3	Cancer
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 .

HY-170576

FLT3-IN-28	FLT3 STAT Apoptosis	Cancer
FLT3-IN-28 (Compound 12y) is an orally active FLT3 inhibitor with antitumor activity. FLT3-IN-28 selectively inhibits cancer cells harboring the FLT3 internal tandem duplication (ITD) mutation, with IC₅₀ values of 85, 290, 130, 65, and 220 nM for BaF3-FLT3-ITD, BaF3-TEL-VEGFR2, MV4-11, MOLM-13, and MOLM-14 cell lines respectively (MV4-11 and MOLM-13/14 are acute myeloid leukemia (AML) cell lines carrying the FLT3-ITD mutation). Additionally, FLT3-IN-28 can downregulate the phosphorylation levels of FLT3 and STAT5 in MOLM-13 cells and induce cell cycle arrest and Apoptosis. FLT3-IN-28 has an oral bioavailability of 19.2% in SD rats and can prolong survival in a dose-dependent manner in NSG mice xenografted with MOLM-13 cells. FLT3-IN-28 holds promise for research in cancer fields related to FLT3-ITD .

HY-12083

PPY-A	Bcr-Abl	Cancer
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) .

HY-159147

SIAIS039	PROTACs ROS Kinase Apoptosis	Cancer
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) .

HY-155227

ALK/EGFR-IN-1	Anaplastic lymphoma kinase (ALK) EGFR Apoptosis	Cancer
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 .

HY-162103

Axl-IN-18	TAM Receptor Apoptosis	Cancer
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 .

HY-170934

BW710	FGFR	Cancer
BW710 is an orally active fibroblast growth factor receptor 2 (FGFR2) inhibitor. BW710 inhibits the proliferation of BaF3-FGFR2 cells with an IC₅₀ of 2.8 nM. BW710 abolishes FGFR2 enzymatic activity and is selective against other 75 tyrosine kinases including FGFR1, FGFR3, and FGFR4 at 1 μM. BW710 suppresses the FGFR2 signaling and selectively inhibits FGFR2-driven cancer cell proliferation. BW710 displays reasonable pharmacokinetic properties with an oral bioavailability of 29 % in mice .

HY-151048

JBJ-07-149	EGFR	Cancer
JBJ-07-149 is an inhibitor for EGFRL858R/T790M with an IC₅₀ of 1.1 nM. JBJ-07-149 inhibits the proliferation of cell Ba/F3 with IC₅₀ of 4.9 μM and 0.148 μM, without and with presence of Cetuximab (HY-P9905). JBJ-07-149 can be used as ligand for target protein in synthesis of DDC-01-163 (HY-139997) .

HY-133551

WF-47-JS03	RET	Cancer
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 .

HY-131906

JAK2-IN-7	JAK FLT3 Apoptosis	Cancer
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 .

HY-125845

(S,R,S)-AHPC 2 Publications Verification VH032-NH2; VHL ligand 1	Ligands for E3 Ligase	Cancer
(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 .

HY-101763B

(S,R,S)-AHPC dihydrochloride VH032-NH2 dihydrochloride; VHL ligand 1 dihydrochloride	Ligands for E3 Ligase	Cancer
(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 .

HY-155302

FLT3-IN-22	FLT3	Cancer
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 .

Cat. No.	Product Name		Classification

HY-159147

SIAIS039		Azide
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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