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Results for "

BaF3 mutant

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (4) Anaplastic lymphoma kinase (ALK) (2) Apoptosis (8) Bcr-Abl (5) c-Kit (6) EGFR (12) Epigenetic Reader Domain (1) ERK (4) FAK (2) FGFR (1) FLT3 (3) HDAC (1) JAK (1) p38 MAPK (2) PROTACs (7) Ras (2) RET (2) Src (1) STAT (1) Trk Receptor (3)
By Research Areas:	Cancer (34) Endocrinology (1) Inflammation/Immunology (1)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-153724

BI-2865 10+ Cited Publications	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-129550

BI-4020	EGFR	Cancer
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 .

HY-157229

STX-721 1 Publications Verification	EGFR ERK	Cancer
STX-721 is an orally active, irreversible, covalent EGFR exon 20 insertion (ex20ins) inhibitor that selectively targets ex20ins-mutant dynamic protein states. STX-721 potently inhibits the kinase activity of EGFR ex20ins mutants (NPG, ASV, SVD). STX-721 inhibits phosphorylation of EGFR (pEGFR Y1068) and downstream ERK (pERK Thr202/Tyr204), and suppresses proliferation of ex20ins-mutant Ba/F3 cells and human NSCLC cell lines (NCI-H2073 ASV KI, CUTO-14 ASV). STX-721 induces tumor regression in EGFR ex20ins-mutant PDX/CDX models. STX-721 can be used for the study of non-small cell lung cancer (NSCLC) harboring EGFR or HER2 ex20ins mutations .

HY-134877

BAY 2476568	EGFR ERK Akt	Cancer
BAY 2476568 is a potent and mutant-selective inhibitor targeting EGFR exon20 insertion variants. BAY 2476568 potently inhibits the kinase activity of EGFR exon20 insertion mutants (insASV, insSVD, insNPG) with IC₅₀ values of 0.09 nM, 0.21 nM, and 0.11 nM, respectively. BAY 2476568 inhibits EGFR (Y1068) phosphorylation and reduces the phosphorylation of ERK1/2 and Akt (S473) in Ba/F3 cells expressing EGFR exon20 insertion mutants (insASV, insSVD). BAY 2476568 can be used for the study of non-small cell lung cancer (NSCLC) driven by EGFR exon20 insertion mutations .

HY-118144

PD166326	Src Bcr-Abl p38 MAPK	Cancer
PD166326 is an orally active tyrosine kinase inhibitor with a IC₅₀ of 8 nM against abl tyrosine kinase and a IC₅₀ of 6 nM against src tyrosine kinase. PD166326 blocks Bcr/Abl kinase activity. PD166326 inhibits Bcr/Abl-dependent proliferation and cell cycle progression. PD166326 reduces peripheral blood granulocytosis, alleviates splenomegaly and prolongs survival in a mouse model of chronic myeloid leukemia. PD166326 can be used in research related to chronic myeloid leukemia .

HY-139997

DDC-01-163	PROTACs EGFR	Cancer
DDC-01-163 is an allosteric PROTAC degrader targeting EGFR. DDC-01-163 is dependent on the ubiquitin–proteasome system. DDC-01-163 can selectively inhibit the proliferation of L858R/T790M (L/T) mutant Ba/F3 cells. DDC-01-163 is effective against Osimertinib (HY-15772)-resistant cells with L/T/C797S and L/T/L718Q EGFR mutations. DDC-01-163 exhibits enhanced anti-proliferative activity against L858R/T790M EGFR-Ba/F3 cells when combined with the ATP-site EGFR inhibitor Osimertinib. DDC-01-163 can be used for the study of non-small cell lung cancer .

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-161633

PROTAC EGFR degrader 11	PROTACs EGFR FAK	Cancer
PROTAC EGFR degrader 11 (Compound B71) is a PROTAC degrader for epidermal growth factor receptor (EGFR), with DC₅₀ <100 nM. PROTAC EGFR degrader 11 binds CRBN-DDB1 with a K_i of 36 nM. PROTAC EGFR degrader 11 degrades EGFR, focal adhesion kinase (FAK), and RSK1, inhibits the proliferation of BaF3 wild type and EGFR mutants, with IC₅₀ <100 nM.

HY-159591

YK-8S	Ras Akt ERK	Cancer
YK-8S is a dual-targeted K-Ras (G12D/G12C) covalent inhibitor. YK-8S shows no significant binding to wild-type K-Ras and other mutants (G12R, G13D, Q61R/K). YK-8S exhibits anti-proliferative activity against H358 (G12C) and AGS (G12D) cells. YK-8S inhibits the phosphorylation of p-AKT/p-ERK in BaF3/G12D and G12C cells. YK-8S can be used for pancreatic cancer, colorectal cancer and other tumors with high incidence of G12D .

HY-122849

CHMFL-KIT-031	c-Kit	Cancer
CHMFL-KIT-031 is a highly selective KIT V559D inhibitor, with an IC₅₀ of 28 nM. CHMFL-KIT-031 potently affects KIT V559D mutant’s phosphorylation at Y703/719/823 sites. CHMFL-KIT-031 inhibits the tumor growth in BaF3-TEL-KIT-V559D cell inoculated mouse model .

HY-161632

PROTAC EGFR degrader 10	PROTACs EGFR FAK	Cancer
PROTAC EGFR degrader 10 (Compound B56) is a PROTAC degrader for epidermal growth factor receptor (EGFR), with DC₅₀ <100 nM. PROTAC EGFR degrader 10 binds CRBN-DDB1 with a K_i of 37 nM. PROTAC EGFR degrader 10 degrades EGFR, focal adhesion kinase (FAK), and RSK1, inhibits the proliferation of BaF3 wild type and EGFR mutants, with IC₅₀ <150 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-178057

EGFR-IN-176	EGFR Akt Anaplastic lymphoma kinase (ALK) Apoptosis	Cancer
EGFR-IN-176 is an orally active and ATP-competitive EGFR mutant inhibitor (particularly C797S-mediated EGFR triple mutant). EGFR-IN-176 effectively inhibits subsequent AKT signaling and induces apoptosis in Ba/F3 and PC-9 cells expressing EGFR ^{19del/T790M/C797S} and EGFR ^{L858R/T790M/C797S}. EGFR-IN-176 selectively inhibits EGFR signaling in cell lines harboring EGFR triple mutation and shows no inhibitory effect against A431 cells that express wild-type EGFR. EGFR-IN-176 can effectively inhibit the enzymatic activity of ALK (IC₅₀ < 0.5 nM). EGFR-IN-176 can be used for the study of non-small cell lung cancer (NSCLC) .

HY-175864

EGFR-IN-173	EGFR Apoptosis p38 MAPK ERK Akt STAT	Inflammation/Immunology Cancer
EGFR-IN-173 is an orally active, pan-mutant EGFR tyrosine kinase inhibitor that targets EGFR 19del, L858R/T790M and C797S triple-mutations, potently inhibiting EGFR ^{19del/T790M/C797S} with an IC₅₀ of 1.19 nM while showing over 100-fold selectivity for mutant over wild-type EGFR (IC₅₀ = 19.362 μM against WT). EGFR-IN-173 significantly inhibits cell migration, induces apoptosis in non-small cell lung cancer (NSCLC) cells. EGFR-IN-173 inhibits EGFR phosphorylation and suppresses the downstream pathways (MAPK/ERK, AKT, STAT3). EGFR-IN-173 exhibits antitumor efficacy in NSCLC and Ba/F3 xenograft models. EGFR-IN-173 can be used for NSCLC research .

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-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-175610

PROTAC FLT3/JAK2/BRD4 Degrader-1	PROTACs FLT3 JAK Epigenetic Reader Domain	Cancer
PROTAC FLT3/JAK2/BRD4 Degrader-1 is a PROTAC degrader that target FLT3, JAK2, and BRD4 with DC₅₀ values of 5.23, 0.678, and 1.17 nM, respectively. PROTAC FLT3/JAK2/BRD4 Degrader-1 exhibits potent antiproliferative activity against MV4;11 cells (IC₅₀ = 0.79 nM) and FLT3 mutant-transformed Ba/F3 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 induces apoptosis in MV4;11 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 demonstrates significant anti-tumor efficacy in the MV4;11 xenograft model established in NOD SCID mice. PROTAC FLT3/JAK2/BRD4 Degrader-1 can be used for the study of acute myeloid leukemia (AML). (Pink: FLT3/JAK2/BRD4 ligand (HY-175611), Blue: CRBN Ligand (HY-W087383), Black: Linker, E3 ligase ligand-linker conjugate (HY-W897939)) .

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-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-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-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-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-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-175302

TRK-IN-32	Trk Receptor Apoptosis	Cancer
TRK-IN-32 is a potent TRK inhibitor. TRK-IN-32 potently inhibits TRK ^WT, TRK ^G595R and TRK ^G667C with IC₅₀ values of 0.08 nM, 2.14 nM and 0.68 nM, respectively. TRK-IN-32 also demonstrates antiproliferative activity against a panel of Ba/F3 cell lines transformed with wild type, xDFG, solvent-front as well as gatekeeper mutant TRK fusion proteins. TRK-IN-32 induces apoptosis of Ba/F3-TRKA ^WT and Ba/F3-TRKA ^G667C cells.TRK-IN-32 can be used for the study of various cancers (such as thyroid cancer, secretory breast carcinoma) .

HY-170497

EGFR-IN-140	EGFR	Cancer
EGFR-IN-140 (Compound 31) is the inhibitor for EGFR, that inhibits EGFR wildtype and EGFR L858R/T790M/C797S mutant with K_i of 0.95 nM and 2.1 nM, and inhibits EGFR del19/T790M/C797S in Ba/F3 with an IC₅₀ of 56.9 nM. EGFR-IN-140 exhibits antitumor efficacy in mouse model .

HY-169076

FLT3/HDAC-IN-1	FLT3 HDAC Apoptosis	Cancer
FLT3/HDAC-IN-1 is a dual inhibitor of FLT3/HDAC, with IC₅₀ values of 30.4, 52.4, and 14.7 nM for FLT3, HDAC1, and HDAC3, respectively. FLT3/HDAC-IN-1 can induce apoptosis in MV-4-11 cells and has anti-proliferative effects on FLT3 mutant-transformed BaF3 cells. FLT3/HDAC-IN-1 is being researched for its potential in treating hard-to-treat solid tumors and hematological malignancies .

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 .

HY-180981

P19As	PROTACs Bcr-Abl	Cancer
P19As is a BCR-ABL PROTAC degrader based on Asciminib (HY-104010), with a DC₅₀ value of approximately 200 nM for the wild-type BCR-ABL protein. P19As can degrade the T315I mutant and exhibits potent anti-proliferative activity in BaF3-BCR-ABL (T315I) cells. P19As can be used for the study of chronic myeloid leukemia and acute lymphoblastic leukemia .

HY-182741

RET-IN-32	RET	Endocrinology Cancer
RET-IN-32 is an orally active RET inhibitor with IC₅₀ values of 0.285, 4.602 and 103.5 nM against wild-type, V804M and G810S mutant forms, respectively. RET-IN-32 inhibits the autophosphorylation of Tyr1062. RET-IN-32 completely suppresses tumor growth induced by BAF3-KIF3B-RET-WT xenografts. RET-IN-32 can be used in the research of thyroid cancer and lung cancer .

HY-180979

P22D	PROTACs Bcr-Abl	Cancer
P22D is a BCR-ABL PROTAC degrader based on Dasatinib (HY-10181), with a DC₅₀ value of approximately 10 nM for the wild-type BCR-ABL protein. P22D cannot degrade the BCR-ABL T315I mutant. P22D has inhibitory activity against K562 cells (wild type), but is ineffective against BaF3-BCR-ABL (T315I) cells. P22D can be used for research on chronic myeloid leukemia and acute lymphocytic leukemia .

HY-179563

c-Kit-IN-12	c-Kit	Cancer
C-Kit-IN-12 (Compound 2a) is a potent c-Kit inhibitor, with its IC₅₀ value for c-Kit being less than 10 nM in four KIT mutant cell models (BAF3 KIT EX11 DEL, EX11 DEL/D816H, EX11 DEL/T670I, EX11 DEL/V654A). C-Kit-IN-12 can be used for studying diseases or disorders related to c-Kit, such as cancer .

HY-171884

BI-8128	EGFR	Cancer
BI-8128 is a potent EGFR inhibitor, with IC₅₀ values of 12, 6.7, 22, 10, and 3 nM against wild-type, T790M, C797S, T790M/C797S, and L858R/T790M/C797S mutant EGFR, respectively. BI-8128 significantly inhibits the proliferation of Ba/F3 and PC-9 drug-resistant mutant cells. BI-8128 is applicable for the research of non-small cell lung cancer .

HY-179563A

(S)-c-Kit-IN-12	c-Kit	Cancer
(S)-c-Kit-IN-12 (Compound 2b) is a potent c-Kit inhibitor, with its IC₅₀ value for c-Kit being less than 10 nM in four KIT mutant cell models (BAF3 KIT EX11 DEL, EX11 DEL/D816H, EX11 DEL/T670I, EX11 DEL/V654A). (S)-c-Kit-IN-12 can be used for studying diseases or disorders related to c-Kit, such as cancer .

HY-180977

P19P	PROTACs Bcr-Abl	Cancer
P19P is a BCR-ABL PROTAC degrader based on Ponatinib (HY-12047), with a DC₅₀ value of approximately 20 nM for the wild-type BCR-ABL protein. P19P can effectively degrade various drug-resistant mutants such as T315I, E255K, H396R, and V468F, and exhibits potent anti-proliferative activity in BaF3-BCR-ABL (T315I) cells. P19P maintains strong inhibitory activity against ABL (T315I), with a IC₅₀ of 13.1 nM. P19P does not inhibit the formation of vascular lumens in HUVEC. P19P can be used for research on chronic myeloid leukemia and acute lymphoblastic leukemia .

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BaF3 mutant

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