Search Result

Results for "

Inhibitor _Kit

" in MedChemExpress (MCE) Product Catalog:

By Targets:	c-Kit (91) Akt (2) Anaplastic lymphoma kinase (ALK) (1) Apoptosis (31) Aurora Kinase (2) Autophagy (23) Bcr-Abl (14) c-Fms (16) c-Met/HGFR (9) c-Myc (1) Casein Kinase (1) CDK (1) Checkpoint Kinase (Chk) (1) Discoidin Domain Receptor (3) Drug Metabolite (11) Drug-Linker Conjugates for ADC (2) EGFR (3) FAK (1) Ferroptosis (3) FGFR (21) FLT3 (25) IKK (1) Isotope-Labeled Compounds (6) JAK (1) NAMPT (1) NO Synthase (1) PDGFR (65) PDK-1 (1) Pim (1) PKA (1) PKC (2) RAD51 (2) Raf (10) RET (16) SARS-CoV (4) Src (7) Syk (1) TAM Receptor (4) Tie (3) Trk Receptor (3) VEGFR (55) Wnt (1)
By Research Areas:	Cancer (116) Cardiovascular Disease (2) Infection (1) Inflammation/Immunology (10) Neurological Disease (2)

By Targets:

c-Kit (91)

Akt (2)

Anaplastic lymphoma kinase (ALK) (1)

Apoptosis (31)

Aurora Kinase (2)

Autophagy (23)

Bcr-Abl (14)

c-Fms (16)

c-Met/HGFR (9)

c-Myc (1)

Casein Kinase (1)

CDK (1)

Checkpoint Kinase (Chk) (1)

Discoidin Domain Receptor (3)

Drug Metabolite (11)

Drug-Linker Conjugates for ADC (2)

EGFR (3)

FAK (1)

Ferroptosis (3)

FGFR (21)

FLT3 (25)

IKK (1)

Isotope-Labeled Compounds (6)

JAK (1)

NAMPT (1)

NO Synthase (1)

PDGFR (65)

PDK-1 (1)

Pim (1)

PKA (1)

PKC (2)

RAD51 (2)

Raf (10)

RET (16)

SARS-CoV (4)

Src (7)

Syk (1)

TAM Receptor (4)

Tie (3)

Trk Receptor (3)

VEGFR (55)

Wnt (1)

By Research Areas:

Cancer (116)

Cardiovascular Disease (2)

Infection (1)

Inflammation/Immunology (10)

Neurological Disease (2)

132

Inhibitors & Agonists

Inhibitory Antibodies

Isotope-Labeled Compounds

Targets Recommended: c-Kit

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-132166

M4205

c-Kit Cancer

M4205 is a c-KIT inhibitor, with an IC₅₀ of 10 nM for c-KIT V654A. M4205 has high activity on c-KIT mutations in exon 11, 13, 17.
HY-15240

c-Kit-IN-1

c-Kit c-Met/HGFR Cancer

c-Kit-IN-1 is a potent inhibitor of c-Kit and c-Met with IC₅₀s of <200 nM.

M4205	c-Kit	Cancer
M4205 is a *c-KIT* inhibitor, with an IC₅₀ of 10 nM for c-KIT V654A. M4205 has high activity on c-KIT mutations in exon 11, 13, 17.

c-Kit-IN-1	c-Kit c-Met/HGFR	Cancer
c-Kit-IN-1 is a potent inhibitor of *c-Kit* and c-Met with IC₅₀s of <200 nM.

HY-18302

c-Kit-IN-5-1	c-Kit	Inflammation/Immunology
c-Kit-IN-5 is potent inhibitor of *c-Kit, with IC₅₀s of 22 nM and 16 nM in kinase assay and cell assay, respectively. c-Kit-IN-5 shows more than 200-fold selectivity for c-Kit* over KDR, p38, Lck, and Src. c-Kit-IN-5 also exhibits desirable pharmacokinetic properties .

HY-112802

AZD3229

c-Kit Cancer

AZD3229 is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors. AZD3229 inhibits c-KIT with an IC₅₀ value of 223.3 nM .

AZD3229	c-Kit	Cancer
AZD3229 is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors. AZD3229 inhibits c-KIT with an IC₅₀ value of 223.3 nM .

HY-101443

ISCK03 2 Publications Verification	c-Kit	Inflammation/Immunology
ISCK03 is a *SCF/c-Kit* and CD117-specific inhibitor. ISCK03 significantly inhibits c-Kit phosphorylation at 10 μM .

HY-128589

CHMFL-KIT-033

c-Kit Cancer

CHMFL-KIT-033 is a potent and selective inhibitor of c-KIT T670I mutant for gastrointestinal stromal tumors (GISTs), with an IC₅₀ of 0.045 μM .
HY-156619

Labuxtinib

c-Kit Cancer

Labuxtinib is c-kit tyrosine kinase inhibitor .

CHMFL-KIT-033	c-Kit	Cancer
CHMFL-KIT-033 is a potent and selective inhibitor of *c-KIT* T670I mutant for gastrointestinal stromal tumors (GISTs), with an IC₅₀** of 0.045 μM .

Labuxtinib	c-Kit	Cancer
Labuxtinib is c-kit tyrosine kinase inhibitor .

HY-112452

SU11652	VEGFR FGFR PDGFR c-Kit Apoptosis	Cancer
SU11652 is a potent receptor tyrosine kinase (RTK) inhibitor. SU11652 also inhibits several members of the split kinase family of RTKs, including VEGFR, FGFR, PDGFR, and *Kit. SU11652 can be uesd for spontaneous cancers expressing Kit* mutations research .

HY-P99462

Barzolvolimab CDX 0159	c-Kit	Inflammation/Immunology
Barzolvolimab (CDX 0159) is a humanized anti-KIT IgG1 monoclonal antibody. Barzolvolimab specificity and potently inhibits KIT activation by SCF. Barzolvolimab can reduce skin mast cells and disease activity in chronic inducible urticaria .

HY-112802A

AZD3229 Tosylate

c-Kit Cancer

AZD3229 Tosylate is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors.

AZD3229 Tosylate	c-Kit	Cancer
AZD3229 Tosylate is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors.

HY-10873

N-Desethyl Sunitinib 5 Publications Verification SU-12662	Drug Metabolite	Cancer
N-Desethyl Sunitinib (SU-12662) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and *KIT* inhibitor with K_i values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively .

HY-138813

N-Desethyl Sunitinib hydrochloride 5 Publications Verification SU-12662 hydrochloride	Drug Metabolite	Cancer
N-Desethyl Sunitinib (SU-12662) (hydrochloride) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and *KIT* inhibitor with K_i values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively .

HY-128602

c-Kit-IN-2	c-Kit	Cancer
c-Kit-IN-2 is a *c-KIT* inhibitor with an IC₅₀ of 82 nM, shows superior antiproliferative activities against all the three GIST cell lines, GIST882, GIST430, and GIST48, with GI₅₀s of 3, 1, and 2 nM, respectively .

HY-101034

CHMFL-ABL/KIT-155 CHMFL-ABL-KIT-155
CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor (IC₅₀s of 46 nM and 75 nM, respectively), and it also presents significant inhibitory activities to BLK (IC₅₀=81 nM), CSF1R (IC₅₀=227 nM), DDR1 (IC₅₀=116 nM), DDR2 (IC₅₀=325 nM), LCK (IC₅₀=12 nM) and PDGFRβ (IC₅₀=80 nM) kinases. CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) arrests cell cycle progression and induces apoptosis .

HY-50946

Imatinib Mesylate 65+ Cited Publications STI571 Mesylate; CGP-57148B Mesylate	c-Kit Bcr-Abl PDGFR Autophagy	Cancer
Imatinib Mesylate (STI571 Mesylate) is a tyrosine kinases inhibitor that inhibits *c-Kit, Bcr-Abl, and PDGFR* (IC₅₀=100 nM) tyrosine kinases.

HY-112616

NAMPT inhibitor-linker 2	NAMPT Drug-Linker Conjugates for ADC	Cancer
NAMPT inhibitor-linker 2 is a agent-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-4 consists of an NAMPT inhibitor-linker 2 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526, with IC₅₀s of <7 pM and 40 pM, respectively.

HY-112615

NAMPT inhibitor-linker 1	Drug-Linker Conjugates for ADC	Cancer
NAMPT inhibitor-linker 1 is a agent-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-3 consists of an NAMPT inhibitor-linker 1 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526 cells, with IC₅₀s of <3 pM and 9 pM, respectively.

HY-13838

PLX647	c-Fms c-Kit	Cancer
PLX647 is an orally active, highly specific dual FMS and *KIT* kinase inhibitor, with IC₅₀s of 28 and 16 nM, respectively. PLX647 shows selectivity for FMS and KIT over a panel of 400 kinases at a concentration of 1 μM except FLT3 and KDR (IC₅₀s=91 and 130 nM, respectively) .

HY-10873S

N-Desethyl Sunitinib-d5	Isotope-Labeled Compounds Drug Metabolite	Cancer
N-Desethyl Sunitinib-d₅ is the deuterium labeled N-Desethyl Sunitinib. N-Desethyl Sunitinib (SU-12662) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively[1].

HY-13838A

PLX647 dihydrochloride	c-Fms c-Kit	Inflammation/Immunology Cancer
PLX647 dihydrochloride is an orally active, highly specific dual FMS and *KIT* kinase inhibitor, with IC₅₀s of 28 and 16 nM, reapectively. PLX647 dihydrochloride shows selectivity for FMS and KIT over a panel of 400 kinases at a concentration of 1 μM except FLT3 and KDR (IC₅₀s=91 and 130 nM, respectively) .

HY-G0017

N-Desmethyl imatinib Norimatinib; Imatinib metabolite N-Desmethyl imatinib	Drug Metabolite	Others
N-Desmethyl imatinib (Norimatinib) is a metabolite of Imatinib (HY-15463). Imatinib is a multi-target inhibitor of v-Abl, c-Kit and PDGFR .

HY-G0017A

N-Desmethyl imatinib mesylate Norimatinib mesylate; Imatinib metabolite N-Desmethyl imatinib mesylate	Drug Metabolite	Others
N-Desmethyl imatinib mesylate (Norimatinib mesylate) is a metabolite of Imatinib (HY-15463). Imatinib is a multi-target inhibitor of v-Abl, c-Kit and PDGFR .

HY-110071

APcK110

c-Kit Cancer

APcK110 is a potent Kit inhibitor that can be used for the research of acute myeloid leukemia (AML). APcK110 induces AML cell apoptosis .

APcK110	c-Kit	Cancer
APcK110 is a potent *Kit* inhibitor that can be used for the research of acute myeloid leukemia (AML). APcK110 induces AML cell apoptosis .

HY-10209

Masitinib 5 Publications Verification AB1010	c-Kit PDGFR Src FGFR FAK Apoptosis	Cancer
Masitinib (AB1010) is a potent, orally bioavailable, and selective inhibitor of *c-Kit* (IC₅₀=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC₅₀s=540/800 nM), Lyn (IC₅₀= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib (AB1010) has anti-proliferative, pro-apoptotic activity and low toxicity .

HY-10209A

Masitinib mesylate 5 Publications Verification AB-1010 mesylate	c-Kit PDGFR Src FGFR Apoptosis	Cancer
Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of *c-Kit* (IC₅₀=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC₅₀s=540/800 nM), Lyn (IC₅₀= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib mesylate (AB-1010 mesylate) has anti-proliferative, pro-apoptotic activity and low toxicity .

HY-148794

Risvodetinib IkT-148009	c-Met/HGFR	Cancer
Risvodetinib is a potent protein tyrosine kinase inhibitor. Risvodetinib involves in synthesis of Abelson protein kinases (c-Abl1, c-Abl2, and c-kit) inhibitor .

HY-10501

SU14813 1 Publications Verification	PDGFR VEGFR c-Kit	Cancer
SU14813 is a multi-targeted receptor tyrosine kinases inhibitor with IC₅₀s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and *KIT*.

HY-10501A

SU14813 maleate 1 Publications Verification	PDGFR VEGFR c-Kit	Cancer
SU14813 maleate is a multi-targeted receptor tyrosine kinases inhibitor with IC₅₀s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and *KIT*.

HY-10981

Lenvatinib 35+ Cited Publications E7080	VEGFR FGFR PDGFR c-Kit RET	Cancer
Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, *KIT, and RET*, shows potent antitumor activities .

HY-10981A

Lenvatinib mesylate 35+ Cited Publications E7080 mesylate	VEGFR FGFR PDGFR RET c-Kit	Cancer
Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, *KIT, and RET*, shows potent antitumor activities .

HY-15198

KG5	Raf PDGFR FLT3 c-Kit	Cancer
KG5 is an orally active dual PDGFRβ and B-Raf allosteric inhibitor. KG5 also inhibits Flt3, *KIT* and c-Raf. KG5 has anticancer, antiangiogenic activities .

HY-13904

Flumatinib HHGV678	Bcr-Abl c-Kit PDGFR	Cancer
Flumatinib (HHGV678) is an orally available, selective inhibitor of Bcr-Abl. Flumatinib inhibits c-Abl, PDGFRβ and *c-Kit* with IC₅₀s of 1.2 nM, 307.6 nM and 665.5 nM, respectively .

HY-111947

c-Fms-IN-6	c-Fms	Inflammation/Immunology
c-Fms-IN-6 is a potent inhibitor of c-FMS, with an IC₅₀ of ≤10 nM for unphosphorylated c-FMS, also weakly inhibits unphosphorylated c-KIT and PDGFR (IC₅₀, > 1 μM). Used in the research of autoimmune diseases .

HY-50946R

Imatinib Mesylate (Standard) STI571 Mesylate (Standard); CGP-57148B Mesylate (Standard)	c-Kit Bcr-Abl PDGFR Autophagy	Cancer
Imatinib (Mesylate) (Standard) is the analytical standard of Imatinib (Mesylate). This product is intended for research and analytical applications. Imatinib Mesylate (STI571 Mesylate) is a tyrosine kinases inhibitor that inhibits *c-Kit, Bcr-Abl, and PDGFR* (IC₅₀=100 nM) tyrosine kinases.

HY-16749A

Pexidartinib hydrochloride 65+ Cited Publications PLX-3397 hydrochloride	c-Fms c-Kit Apoptosis	Cancer
Pexidartinib hydrochloride (PLX-3397 hydrochloride) is a potent, orally active, selective, and ATP-competitive colony stimulating factor 1 receptor (CSF1R or M-CSFR) and *c-Kit* inhibitor, with IC₅₀s of 20 and 10 nM, respectively. Pexidartinib hydrochloride exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. Pexidartinib hydrochloride induces cell apoptosis and has anti-cancer activity .

HY-15463S

Imatinib-d8 1 Publications Verification STI571-d₈; CGP-57148B-d₈	Bcr-Abl PDGFR c-Kit SARS-CoV Autophagy	Cancer
Imatinib-d₈ is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity[1][2].

HY-15463S1

Imatinib-d4 STI571 d₄; CGP-57148B d₄	Bcr-Abl PDGFR c-Kit SARS-CoV Autophagy	Cancer
Imatinib-d₄ is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity[1][2].

HY-18317

JNJ-38158471	VEGFR RET c-Kit	Cancer
JNJ-38158471 is a well tolerated, orally available, highly selective VEGFR-2 inhibitor, with an IC₅₀ of 40 nM. JNJ-38158471 also inhibits Ret and *Kit* with IC₅₀s of 180 and 500 nM, respectively .

HY-152839

Elenestinib BLU-263	c-Kit	Cancer
Elenestinib (BLU-263) is a potent and orally active tyrosine kinase inhibitor. Elenestinib has the potential for the research of systemic mastocytosis (SM). Elenestinib inhibits KIT D816V with an IC₅₀ value of 0.2 nM .

HY-10527

Telatinib 1 Publications Verification Bay 57-9352	c-Kit PDGFR VEGFR	Cancer
Telatinib (Bay 57-9352) is an orally active, small molecule inhibitor of VEGFR2, VEGFR3, PDGFα, and *c-Kit* with IC₅₀s of 6, 4, 15 and 1 nM, respectively.

HY-10527C

Telatinib mesylate 1 Publications Verification Bay 57-9352 mesylate	VEGFR PDGFR c-Kit	Cancer
Telatinib mesylate (Bay 57-9352 mesylate) is a potent and orally active VEGFR2, VEGFR3, PDGFα, and *c-Kit* inhibitor with IC₅₀s of 6 nM, 4 nM, 15 nM and 1 nM, respectively .

HY-101561

Avapritinib 5 Publications Verification BLU-285	c-Kit PDGFR	Cancer
Avapritinib (BLU-285) is a highly potent, selective, and orally active *KIT* and PDGFRA activation loop mutant kinases inhibitor with IC₅₀s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2 .

HY-18179

AZD2932	PDGFR VEGFR FLT3 c-Kit	Cancer
AZD2932 is a potent and multi-targeted kinase inhibitor VEGFR2, PDGFβ, Flt-3 and *c-Kit* with IC₅₀s of 8, 4, 7 and 9 nM in cell assay, respectively.

HY-13493

AC710

PDGFR c-Kit FLT3 Cancer

AC710 is a potent PDGFR inhibitor with K_ds of 0.6, 1.57, 1, 1.3, 1.0 nM for FLT3, CSF1R, KIT, PDGFRα and PDGFRβ, respectively.
HY-13493A

AC710 Mesylate

PDGFR Cancer

AC710 Mesylate is a potent PDGFR inhibitor with K_ds of 0.6, 1.57, 1, 1.3, 1.0 nM for FLT3, CSF1R, KIT, PDGFRα and PDGFRβ, respectively.

AC710	PDGFR c-Kit FLT3	Cancer
AC710 is a potent PDGFR inhibitor with K_ds of 0.6, 1.57, 1, 1.3, 1.0 nM for FLT3, CSF1R, KIT, PDGFRα and PDGFRβ, respectively.

AC710 Mesylate	PDGFR	Cancer
AC710 Mesylate is a potent PDGFR inhibitor with K_ds of 0.6, 1.57, 1, 1.3, 1.0 nM for FLT3, CSF1R, KIT, PDGFRα and PDGFRβ, respectively.

HY-145557

Bezuclastinib CGT9486; PLX 9486	c-Kit	Cancer
Bezuclastinib (CGT9486) is an orally active, highly selective tyrosine kinase inhibitor with potent activity against KIT D816V. Bezuclastinib can be used for the research of nonadvanced systemic mastocytosis (NonAdvSM) .

HY-103032

Multi-kinase inhibitor 1	PDGFR c-Kit Bcr-Abl	Cancer
Multi-kinase inhibitor 1 is a potent multi-kinase inhibitor. Multi-kinase inhibitor 1 has the potential for diseases or disorders associated with abnormal or deregulated tyrosine kinase activity, particularly diseases associated with the activity of PDGF-R, *c-Kit* and Bcr-abl .

HY-160765

WNTinib APS-8-100-2	Wnt Apoptosis	Cancer
WNTinib (APS-8-100-2) is a multi-kinase inhibitor that selectively antagonizes β-catenin (CTNNB1) mutated hepatocellular carcinoma (HCC). WNTinib downregulates oncogenicWntsignaling by inhibiting KIT/MAPK and downstream EZH2 activation .

HY-112306

Ripretinib DCC-2618	c-Kit PDGFR FLT3 VEGFR Apoptosis	Cancer
Ripretinib (DCC-2618) is an orally bioavailable, selective *KIT* and PDGFRA switch-control inhibitor. Ripretinib (DCC-2618) targets and binds to both wild-type and mutant forms of KIT and PDGFRA specifically at their switch pocket binding sites, thereby preventing the switch from inactive to active conformations of these kinases and inactivating their wild-type and mutant forms. Ripretinib (DCC-2618) also inhibits multiple other kinase targets, such as FLT3 and KDR (or VEGFR-2) . DCC-2618 exerts antineoplastic effect and induces apoptosis .

HY-16749

Pexidartinib 65+ Cited Publications PLX-3397	c-Fms c-Kit Apoptosis	Cancer
Pexidartinib (PLX-3397) is a potent, orally active, selective, and ATP-competitive colony stimulating factor 1 receptor (CSF1R or M-CSFR) and *c-Kit* inhibitor, with IC₅₀s of 20 and 10 nM, respectively. Pexidartinib (PLX-3397) exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. Pexidartinib (PLX-3397) induces cell apoptosis and has anti-tumor activity .

Cat. No.	Product Name	Chemical Structure

HY-10873S

N-Desethyl Sunitinib-d5
N-Desethyl Sunitinib-d₅ is the deuterium labeled N-Desethyl Sunitinib. N-Desethyl Sunitinib (SU-12662) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively[1].

HY-15463S

Imatinib-d8 1 Publications Verification
Imatinib-d₈ is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity[1][2].

HY-15463S1

Imatinib-d4
Imatinib-d₄ is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity[1][2].

HY-10981S

Lenvatinib-d4
Lenvatinib-d₄ is the deuterium labeled Lenvatinib. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities[1][2].

HY-10981S1

Lenvatinib-d5
Lenvatinib-d₅ is the deuterium labeled Lenvatinib. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities[1][2].

HY-13904S

Flumatinib-d3
Flumatinib-d₃ is deuterium labeled Flumatinib. Flumatinib (HHGV678) is an orally available, selective inhibitor of Bcr-Abl. Flumatinib inhibits c-Abl, PDGFRβ and c-Kit with IC50s of 1.2 nM, 307.6 nM and 665.5 nM, respectively[1].

HY-13016S1

Cabozantinib-d4
Cabozantinib-d₄ is deuterium labeled Cabozantinib. Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.

HY-13342AS

Apatinib-d8 free base

Apatinib-d₈ (free base) is the deuterium labeled Apatinib free base[1]. Apatinib free base (YN968D1 free base) is an orally bioavailable tyrosine kinase inhibitor, which selectively targets VEGFR-2 (IC50=1 nM). Apatinib free base (YN968D1 free base) is an anti-angiogenic drug for the research of advanced or metastatic gastric cancer. Apatinib free base (YN968D1 free base) potently inhibits Ret, c-Kit and c-Src with IC50s of 13, 429 and 530 nM, respectively. It also inhibits cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ[2][3][4].

HY-13016S

Cabozantinib-d6
Cabozantinib-d₆ is the deuterium labeled Cabozantinib. Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively[1][2][3].

HY-G0017S1

N-Desmethyl imatinib-d4
N-Desmethyl imatinib-d₄ is the deuterium-labeled N-Desmethyl imatinib (HY-G0017). N-Desmethyl imatinib-d₄ (Norimatinib) is a metabolite of Imatinib (HY-15463). Imatinib is a multi-target inhibitor of v-Abl, c-Kit and PDGFR .

HY-10208S

Pazopanib-d6
Pazopanib-d₆ is the deuterium labeled Pazopanib. Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.

HY-15463S2

Imatinib-d3 hydrochloride

Imatinib-d₃ (hydrochloride) is the deuterium labeled Imatinib. Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.

HY-10330S

Toceranib-d8
Toceranib-d₈ is the deuterium labeled Toceranib. Toceranib (SU11654) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. Toceranib (SU11654) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors[1][2].

HY-10230S

Midostaurin-d5
Midostaurin-d₅ is a deuterium labeled Midostaurin. Midostaurin is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM[1].

HY-10331S1

Regorafenib-13C,d3
Regorafenib- ¹³C,d₃ is the ¹³C- and deuterium labeled Regorafenib. Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively.

HY-10208S1

Pazopanib-13C,d3
Pazopanib- ¹³C,d₃ is the deuterium and ¹³C labeled Pazopanib[1]. Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively[2][3].

HY-12009S

Pazopanib-13C,d3 hydrochloride
Pazopanib- ¹³C,d₃ (hydrochloride) is the deuterium and ¹³C labeled Pazopanib hydrochloride[1]. Pazopanib Hydrochloride (GW786034 Hydrochloride) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with an IC50 of 10, 30, 47, 84, 74, 140 and 146 nM, respectively[2][3].

HY-50905S

Dovitinib-d8
Dovitinib-d₈ is the deuterium labeled Dovitinib. Dovitinib (CHIR-258) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively[1][2].

HY-I0678S1

Regorafénib N-oxyde (M2)-13C,d3
Regorafénib N-oxyde (M2)- ¹³C,d₃ is the ¹³C- and deuterium labeled Regorafénib N-oxyde (M2). Regorafénib N-oxyde M2 is an active metabolite of Regorafenib. Regorafenib is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.

HY-I0678S

Regorafénib N-oxyde-d3 (M2)
Regorafénib N-oxyde-d₃(M2) is the deuterium labeled Regorafénib N-oxyde M2[1]. Regorafénib N-oxyde M2 is an active metabolite of Regorafenib. Regorafenib is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively[2].

HY-10201S2

Sorafenib-13C,d3

1 Publications Verification

Sorafenib- ¹³C,d₃ is the ¹³C- and deuterium labeled Sorafenib. Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator[1].

Inquiry Online

Your information is safe with us. * Required Fields.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent: