Search Result
Results for "
c-Kit inhibitor
" in MedChemExpress (MCE) Product Catalog:
16
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-16749
-
Pexidartinib
Maximum Cited Publications
145 Publications Verification
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. Pexidartinib has limited permeability to the blood-brain barrier, primarily through ABCB1 .
|
-
-
- HY-15463
-
|
STI571; CGP-57148B
|
Bcr-Abl
PDGFR
c-Kit
SARS-CoV
Autophagy
|
Cancer
|
|
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-10208
-
|
GW786034
|
VEGFR
c-Kit
PDGFR
Autophagy
FGFR
|
Cancer
|
|
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-50946
-
-
-
- HY-16749A
-
|
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-10514
-
|
|
PDK-1
IKK
Autophagy
|
Cancer
|
|
BX795 is a potent and selective inhibitor of PDK1, with an IC50 of 6 nM. BX795 is also a potent and relatively specific inhibitor of TBK1 and IKKε, with an IC50 of 6 and 41 nM, respectively. BX795 blocks phosphorylation of S6K1, Akt, PKCδ, and GSK3β, and has lower selectivity over PKA, PKC, c-Kit, GSK3β etc. BX795 modulates autophagy .
|
-
-
- HY-136256
-
|
DCC-3014
|
c-Fms
c-Kit
|
Cancer
|
|
Vimseltinib (DCC-3014) is a c-FMS (CSF-IR) and c-Kit dual inhibitor extracted from patent WO2014145025A2, Compound Example 10, has IC50s of <0.01 μM and 0.1-1 μM, respectively . Vimseltinib has certain oral bioavailability .
|
-
-
- HY-13024
-
|
DCC-2036
|
Bcr-Abl
FLT3
Src
Apoptosis
|
Cancer
|
|
Rebastinib (DCC-2036) is an orally active, non-ATP-competitive Bcr-Abl inhibitor for Abl1 WT and Abl1 T315I with IC50s of 0.8 nM and 4 nM, respectively. Rebastinib also inhibits SRC, KDR, FLT3, and Tie-2, and has low activity to seen towards c-Kit.
|
-
-
- HY-10209
-
|
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
-
|
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-10205
-
|
AZD2171
|
VEGFR
Autophagy
PDGFR
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Cediranib (AZD2171) is a highly potent, orally available and blood-brain barrier permeability VEGFR tyrosine kinase inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.
|
-
-
- HY-132166
-
|
M4205; IDRX-42
|
c-Kit
PDGFR
c-Fms
FLT3
Src
|
Cancer
|
|
Velzatinib (M4205) is a multi-target inhibitor for PDGFRB, PDGFRA, CSF1R, c-Kit, FLT3, and LCK, with an IC50s of 2.6, 50, 5.5, 44, 141 and 141 nM, respectively. Velzatinib exhibits antitumor efficacy in xenograft mouse models .
|
-
-
- HY-10527
-
|
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-13904
-
|
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-12009
-
|
GW786034 Hydrochloride
|
PDGFR
VEGFR
FGFR
c-Kit
c-Fms
Autophagy
|
Cancer
|
|
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.
|
-
-
- HY-108713
-
|
SHR1020
|
VEGFR
PDGFR
Apoptosis
|
Cancer
|
|
Famitinib (SHR1020), an orally active multi-targeted kinase inhibitor, inhibits the activity of c-kit, VEGFR-2 and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM and 6.6 nM, respectively . Famitinib exerts powerful antitumor activity in human gastric cancer cells and xenografts. Famitinib triggers apoptosis .
|
-
-
- HY-156619
-
|
EVT-8565072; THB335
|
c-Kit
PDGFR
|
Metabolic Disease
Inflammation/Immunology
|
|
Labuxtinib (EVT-8565072; THB335) is a potent dual inhibitor of c-Kit and PDGFR. Labuxtinib exhibits potent inhibitory activity against wild-type c-Kit (IC50 = 0.005 μM). Labuxtinib inhibits SCF-dependent and PDGF-dependent cell proliferation, and blocks the proliferation of cells dependent on c-Kit or PDGFR signaling pathways. In animal models of skin allergy, Labuxtinib depletes skin mast cells and significantly alleviates anaphylactic shock responses. Labuxtinib can be used in research on mast cell-related diseases, respiratory diseases, inflammatory diseases, fibrotic diseases, metabolic diseases, and other related conditions .
|
-
-
- HY-10251
-
|
AC480
|
EGFR
|
Cancer
|
|
BMS-599626 (AC480) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. BMS-599626 displays ~8-fold less potent to HER4 (IC50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. BMS-599626 inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy .
|
-
-
- HY-10408
-
Ki20227
4 Publications Verification
|
c-Fms
VEGFR
c-Kit
PDGFR
|
Inflammation/Immunology
|
|
Ki20227 is an orally active and highly selective c-Fms tyrosine kinase (CSF1R) inhibitor with IC50s of 2 nM, 12 nM, 451 and 217 nM for CSF1R, VEGFR2 (vascular endothelial growth factor receptor-2), c-Kit (stem cell factor receptor) and PDGFRβ (platelet-derived growth factor receptor β). Ki20227 suppresses osteoclast differentiation and osteolytic bone destruction .
|
-
-
- HY-15240
-
-
-
- HY-112615
-
|
|
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-109190
-
|
GB002; PK10571
|
PDGFR
c-Fms
c-Kit
|
Cardiovascular Disease
|
|
Seralutinib (GB002) is an inhaled PDGFRα and PDGFRβ inhibitor. Seralutinib also targets to CSF1R and c-KIT with IC50s of 8 nM and 14 nM, respectively. Seralutinib (GB002) is used in the study for pulmonary arterial hypertension .
|
-
-
- HY-10207
-
|
CHIR-258 lactate; TKI-258 lactate
|
FLT3
c-Kit
FGFR
VEGFR
PDGFR
|
Cancer
|
|
Dovitinib lactate (TKI258 lactate) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively .
|
-
-
- HY-10202
-
|
MLN518; CT53518
|
FLT3
c-Kit
PDGFR
Apoptosis
|
Cancer
|
|
Tandutinib (MLN518) is a potent and selective inhibitor of the FLT3 with an IC50 of 0.22 μM, and also inhibits c-Kit and PDGFR with IC50s of 0.17 μM and 0.20 μM, respectively. Tandutinib can be used for acute myelogenous leukemia (AML) . Tandutinib has the ability to cross the blood-brain barrier .
|
-
-
- HY-13894
-
|
AG1296
|
PDGFR
c-Kit
FLT3
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Tyrphostin AG1296 is a potent and selective inhibitor of platelet-derived growth factor receptor (PDGFR), with an IC50 of 0.8 μM. Tyrphostin AG1296 inhibits signaling of human PDGF α- and β-receptors as well as of the related stem cell factor receptor (c-Kit). Tyrphostin AG1296 is also a potent inhibitor of FLT3, with an IC50 in the micromolar range .
|
-
-
- HY-10206
-
|
MP470; HPK 56
|
c-Kit
PDGFR
RAD51
FLT3
c-Met/HGFR
RET
Apoptosis
|
Cancer
|
|
Amuvatinib (MP470) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib (MP470) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair . Antineoplastic activity .
|
-
-
- HY-124526
-
|
Ibcasertib; CS2164
|
PDGFR
c-Fms
Aurora Kinase
VEGFR
c-Kit
Mitosis
|
Cancer
|
|
Chiauranib (CS2164) is an orally active multi-target inhibitor against tumor angiogenesis. Chiauranib potently inhibits the angiogenesis-related kinases (VEGFR1, VEGFR2, VEGFR3, PDGFRα and c-Kit), mitosis-related kinase Aurora B, and chronic inflammation-related kinase CSF-1R, with IC50 values ranging from 1-9 nM. Chiauranib has strongly anticancer effects .
|
-
-
- HY-101443
-
|
|
c-Kit
|
Inflammation/Immunology
|
|
ISCK03 is a SCF/c-Kit and CD117-specific inhibitor. ISCK03 significantly inhibits c-Kit phosphorylation at 10 μM .
|
-
-
- HY-112802
-
|
|
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-13049
-
|
AZD-2171 maleate
|
VEGFR
Autophagy
PDGFR
|
Cancer
|
|
Cediranib maleate (AZD-2171 maleate) is a highly potent, orally available VEGFR inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.
|
-
-
- HY-13905
-
|
HHGV678 mesylate
|
Bcr-Abl
c-Kit
PDGFR
|
Cancer
|
|
Flumatinib (HHGV678) mesylate is an orally active and selective inhibitor of Bcr-Abl. Flumatinib mesylate inhibits c-Abl, PDGFRβ and c-Kit with IC50 values of 1.2, 307.6 and 665.5 nM, respectively. Flumatinib mesylate inhibits Bcr-Abl autophosphorylation and Stat5 and Erk1/2 phosphorylation. Flumatinib mesylate inhibits tumor growth in chronic myelogenous leukemia model .
|
-
-
- HY-112616
-
|
|
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-103032
-
|
|
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-15463S1
-
|
STI571 d4; CGP-57148B d4
|
Bcr-Abl
PDGFR
c-Kit
SARS-CoV
Autophagy
|
Cancer
|
|
Imatinib-d4 (STI571-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 .
|
-
-
- HY-13904S
-
|
HHGV678-d3
|
Isotope-Labeled Compounds
Bcr-Abl
c-Kit
PDGFR
|
Cancer
|
|
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 .
|
-
-
- HY-12010
-
|
AC480 Hydrochloride
|
EGFR
|
Cancer
|
|
BMS-599626 Hydrochloride (AC480 Hydrochloride) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. BMS-599626 Hydrochloride displays ~8-fold less potent to HER4 (IC50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. BMS-599626 Hydrochloride inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy .
|
-
-
- HY-18302
-
|
|
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-15463S
-
|
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 .
|
-
-
- HY-13342AS
-
|
YN968D1-d8 free base
|
Src
VEGFR
Autophagy
c-Kit
RET
|
Cancer
|
|
Apatinib-d8 (free base) is the deuterium labeled Apatinib free base . 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 .
|
-
-
- HY-18179
-
|
|
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-10202A
-
|
MLN518 hydrochloride; CT53518 hydrochloride
|
FLT3
c-Kit
PDGFR
Apoptosis
|
Cancer
|
|
Tandutinib hydrochloride (MLN518 hydrochloride) is a potent and selective inhibitor of the FLT3 with an IC50 of 0.22 μM, and also inhibits c-Kit and PDGFR with IC50s of 0.17 μM and 0.20 μM, respectively. Tandutinib hydrochloride can be used for acute myelogenous leukemia (AML) . Tandutinib hydrochloride has the ability to cross the blood-brain barrier .
|
-
-
- HY-13645
-
|
|
VEGFR
c-Kit
PDGFR
|
Cancer
|
|
Henatinib is an orally active small-molecule multikinase inhibitor that has demonstrated broad and potent antitumor activities. Henatinib inhibits the activity of VEGFR-2, c-kit, PDGFR with IC50 values of 0.6 nM, 3.3 nM and 41.5 nM, respectively. Henatinib significantly inhibits VEGFR-2 phosphorylation and its downstream signal pathway in human umbilical vein endothelial cells (HUVECs) .
|
-
-
- HY-10527C
-
|
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-16749R
-
|
PLX-3397 (Standard)
|
c-Fms
c-Kit
Apoptosis
Reference Standards
|
Cancer
|
|
Pexidartinib (Standard) is the analytical standard of Pexidartinib. This product is intended for research and analytical applications. 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 .
|
-
-
- HY-10208S
-
|
GW786034-d6
|
Isotope-Labeled Compounds
VEGFR
c-Kit
PDGFR
Autophagy
FGFR
|
Cancer
|
|
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-108713A
-
|
SHR1020 malate
|
VEGFR
PDGFR
Apoptosis
|
Cancer
|
|
Famitinib (SHR1020) malate, an orally active multi-targeted kinase inhibitor, inhibits the activity of c-kit, VEGFR-2 and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM and 6.6 nM, respectively. Famitinib malate induces cell apoptosis. Famitinib malate exerts powerful antitumor activity in human gastric cancer cells and xenografts, it can be used for the research of cancer .
|
-
-
- HY-15463R
-
|
STI571 (Standard); CGP-57148B (Standard)
|
Reference Standards
Bcr-Abl
PDGFR
c-Kit
SARS-CoV
Autophagy
|
Cancer
|
|
Imatinib (Standard) is the analytical standard of Imatinib. This product is intended for research and analytical applications. 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-101219
-
|
|
VEGFR
c-Kit
EGFR
|
Cancer
|
|
VEGFR-IN-1 (compound 3) is a potent angiogenesis inhibitor with IC50s of 0.02, 0.18, 0.24 7.3, and 7 µM for KDR, Flt-1, c-Kit, EGF-R, and c-Src, respectively .
|
-
-
- HY-B0062
-
|
TKI258 lactate hydrate; CHIR-258 lactate hydrate
|
FLT3
c-Kit
FGFR
VEGFR
PDGFR
|
Cancer
|
|
Dovitinib lactate hydrate (TKI258 lactate hydrate) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively .
|
-
-
- HY-10206A
-
|
MP470 hydrochloride; HPK 56 hydrochloride
|
c-Kit
PDGFR
RAD51
FLT3
c-Met/HGFR
RET
|
Cancer
|
|
Amuvatinib hydrochloride (MP470 hydrochloride) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib hydrochloride (MP470 hydrochloride) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair . Antineoplastic activity .
|
-
- HY-10230S
-
|
PKC412-d5; CGP 41251-d5
|
Isotope-Labeled Compounds
PKC
Syk
Akt
PKA
c-Kit
|
Cancer
|
|
Midostaurin-d5 (PKC412-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 .
|
-
- HY-13894R
-
|
AG1296 (Standard)
|
PDGFR
c-Kit
FLT3
Apoptosis
Reference Standards
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Tyrphostin AG1296 (Standard) is the analytical standard of Tyrphostin AG1296. This product is intended for research and analytical applications. Tyrphostin AG1296 is a potent and selective inhibitor of platelet-derived growth factor receptor (PDGFR), with an IC50 of 0.8 μM. Tyrphostin AG1296 inhibits signaling of human PDGF α- and β-receptors as well as of the related stem cell factor receptor (c-Kit). Tyrphostin AG1296 is also a potent inhibitor of FLT3, with an IC50 in the micromolar range .
|
-
- HY-110272
-
|
PTK787 succinate; ZK-222584 succinate; CGP-79787 succinate
|
VEGFR
|
Cancer
|
|
Vatalanib (PTK787) succinate is a potent and orally active VEGFR inhibitor with IC50s of 37 nM, 77 nM, 270 nM, 660 nM, 730 nM, 1400 nM, and 580 nM for KDR, Flt-1, Flk, Flt-4, c-Kit, c-Fms, and PDGFR-β, respectively .
|
-
- HY-128589
-
|
|
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-10209R
-
|
AB1010 (Standard)
|
Reference Standards
c-Kit
PDGFR
Src
FGFR
FAK
Apoptosis
|
Cancer
|
|
Masitinib (Standard) is the analytical standard of Masitinib. This product is intended for research and analytical applications. 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-P990851
-
|
|
c-Kit
|
Inflammation/Immunology
Cancer
|
|
Anti-c-Kit/CD117 Antibody (SR-1) is a kind of mouse IgG2a κ chimeric antibody inhibitor, targeting to human c-Kit/CD117. Anti-c-Kit/CD117 Antibody (SR-1) binds to the extracellular domain of human c-Kit (also known as CD117) and blocks stem cell factor (SCF) binding to CD117. Anti-c-Kit/CD117 Antibody (SR-1) can be used for the researches of cancer and immunology, such as gastrointestinal stromal tumor (GIST) and xenograft .
|
-
- HY-16749AR
-
|
PLX-3397 hydrochloride (Standard)
|
c-Fms
c-Kit
Apoptosis
Reference Standards
|
Cancer
|
|
Pexidartinib (hydrochloride) (Standard) is the analytical standard of Pexidartinib (hydrochloride). This product is intended for research and analytical applications. 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-10209AR
-
|
AB-1010 mesylate (Standard)
|
Reference Standards
c-Kit
PDGFR
Src
FGFR
Apoptosis
|
Cancer
|
|
Masitinib (mesylate) (Standard) is the analytical standard of Masitinib (mesylate). This product is intended for research and analytical applications. 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-50946R
-
|
STI571 Mesylate (Standard); CGP-57148B Mesylate (Standard)
|
Reference Standards
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 an orally active tyrosine kinases inhibitor that inhibits c-Kit, Bcr-Abl, and PDGFR (IC50=100 nM) tyrosine kinases.
|
-
- HY-10527R
-
|
Bay 57-9352 (Standard)
|
Reference Standards
c-Kit
PDGFR
VEGFR
|
Cancer
|
|
Telatinib (Standard) is the analytical standard of Telatinib. This product is intended for research and analytical applications. 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-117873A
-
|
|
c-Kit
RET
PDGFR
|
Infection
|
KBP-7018 hydrochloride is a tyrosine kinase-selective inhibitor. KBP-7018 hydrochloride has potent inhibitory effects on c-KIT, PDGFR, and RET with IC50 values of 10 nM, 7.6 nM and 25 nM, respectively. KBP-7018 hydrochloride can be used for the research of idiopathic pulmonary fibrosis .
|
-
- HY-10527CR
-
|
Bay 57-9352 mesylate (Standard)
|
Reference Standards
VEGFR
PDGFR
c-Kit
|
Cancer
|
|
Telatinib (mesylate) (Standard) is the analytical standard of Telatinib (mesylate). This product is intended for research and analytical applications. 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-117873
-
|
|
c-Kit
RET
PDGFR
|
Infection
|
KBP-7018 is a tyrosine kinase-selective inhibitor. KBP-7018 has potent inhibitory effects on c-KIT, PDGFR, and RET with IC50 values of 10 nM, 7.6 nM and 25 nM, respectively. KBP-7018 can be used for the research of idiopathic pulmonary fibrosis .
|
-
- HY-13049R
-
|
AZD-2171 maleate (Standard)
|
VEGFR
Autophagy
PDGFR
Reference Standards
|
Cancer
|
|
Cediranib (maleate) (Standard) is the analytical standard of Cediranib (maleate). This product is intended for research and analytical applications. Cediranib maleate (AZD-2171 maleate) is a highly potent, orally available VEGFR inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.
|
-
- HY-12009R
-
|
GW786034 Hydrochloride (Standard)
|
Reference Standards
PDGFR
VEGFR
FGFR
c-Kit
c-Fms
Autophagy
|
Cancer
|
|
Pazopanib (Hydrochloride) (Standard) is the analytical standard of Pazopanib (Hydrochloride). This product is intended for research and analytical applications. 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.
|
-
- HY-10205R
-
|
AZD2171 (Standard)
|
Reference Standards
VEGFR
Autophagy
PDGFR
|
Cancer
|
|
Cediranib (Standard) is the analytical standard of Cediranib. This product is intended for research and analytical applications. Cediranib (AZD2171) is a highly potent, orally available VEGFR tyrosine kinase inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.
|
-
- HY-10208R
-
|
GW786034 (Standard)
|
Reference Standards
VEGFR
c-Kit
PDGFR
Autophagy
FGFR
|
Cancer
|
|
Pazopanib (Standard) is the analytical standard of Pazopanib. This product is intended for research and analytical applications. 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-10202B
-
|
|
FLT3
c-Kit
PDGFR
Apoptosis
|
Cancer
|
|
Tandutinib (MLN518) sulfate is a potent and selective inhibitor of the FLT3 with an IC50 of 0.22 μM, and also inhibits c-Kit and PDGFR with IC50s of 0.17 μM and 0.20 μM, respectively. Tandutinib sulfate can be used for acute myelogenous leukemia (AML) . Tandutinib sulfate has the ability to cross the blood-brain barrier .
|
-
- HY-W705479
-
|
GW786034-d3 hydrochloride
|
Isotope-Labeled Compounds
Autophagy
PDGFR
FGFR
c-Fms
VEGFR
c-Kit
|
Cancer
|
|
Pazopanib-d3 (hydrochloride) (GW786034-d3 (hydrochloride)) is deuterium labeled Pazopanib (Hydrochloride). 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.
|
-
- HY-10208S2
-
|
GW786034-d3
|
Isotope-Labeled Compounds
Autophagy
VEGFR
c-Kit
PDGFR
FGFR
|
Cancer
|
|
Pazopanib-d3 (GW786034-d3) is 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-108713R
-
|
SHR1020 (Standard)
|
Reference Standards
VEGFR
PDGFR
Apoptosis
|
Cancer
|
|
Famitinib (Standard) is the analytical standard of Famitinib. This product is intended for research and analytical applications. Famitinib (SHR1020), an orally active multi-targeted kinase inhibitor, inhibits the activity of c-kit, VEGFR-2 and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM and 6.6 nM, respectively . Famitinib exerts powerful antitumor activity in human gastric cancer cells and xenografts. Famitinib triggers apoptosis .
|
-
- HY-177287
-
-
- HY-10202R
-
|
MLN518 (Standard); CT53518 (Standard)
|
Reference Standards
FLT3
c-Kit
PDGFR
Apoptosis
|
Cancer
|
|
Tandutinib (Standard) is the analytical standard of Tandutinib. This product is intended for research and analytical applications. Tandutinib (MLN518) is a potent and selective inhibitor of the FLT3 with an IC50 of 0.22 μM, and also inhibits c-Kit and PDGFR with IC50s of 0.17 μM and 0.20 μM, respectively. Tandutinib can be used for acute myelogenous leukemia (AML) . Tandutinib has the ability to cross the blood-brain barrier .
|
-
- HY-10202AR
-
|
MLN518 hydrochloride (Standard); CT53518 hydrochloride (Standard)
|
Reference Standards
FLT3
c-Kit
PDGFR
Apoptosis
|
Cancer
|
|
Tandutinib (hydrochloride) (Standard) is the analytical standard of Tandutinib (hydrochloride). This product is intended for research and analytical applications. Tandutinib hydrochloride (MLN518 hydrochloride) is a potent and selective inhibitor of the FLT3 with an IC50 of 0.22 μM, and also inhibits c-Kit and PDGFR with IC50s of 0.17 μM and 0.20 μM, respectively. Tandutinib hydrochloride can be used for acute myelogenous leukemia (AML) . Tandutinib hydrochloride has the ability to cross the blood-brain barrier .
|
-
- HY-10207R
-
|
CHIR-258 lactate (Standard); TKI-258 lactate (Standard)
|
Reference Standards
FLT3
c-Kit
FGFR
VEGFR
PDGFR
|
Cancer
|
|
Dovitinib (lactate) (Standard) is the analytical standard of Dovitinib (lactate). This product is intended for research and analytical applications. Dovitinib lactate (TKI258 lactate) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively .
|
-
- HY-P990020
-
|
FSI-174
|
c-Kit
|
Others
|
|
Eglatoprutug is an humanized immunoglobulin G1-kappa, anti-c-Kit monoclonal antibody .
|
-
- HY-10206R
-
|
MP470 (Standard); HPK 56 (Standard)
|
Reference Standards
c-Kit
PDGFR
RAD51
FLT3
c-Met/HGFR
RET
Apoptosis
|
Cancer
|
|
Amuvatinib (Standard) is the analytical standard of Amuvatinib. This product is intended for research and analytical applications. Amuvatinib (MP470) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib (MP470) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair . Antineoplastic activity .
|
-
- HY-177286
-
|
|
c-Kit
|
Inflammation/Immunology
Cancer
|
|
c-Kit-IN-11 (Compound A7) is a c-Kit inhibitor with an IC50 of 76 nM for Mo7e cells. c-Kit-IN-11 can be used for inflammatory like asthma and malignant cancers research .
|
-
- HY-168580
-
|
|
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-168579
-
|
|
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-168581
-
|
|
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-128602
-
|
|
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-170228
-
|
|
c-Kit
|
Inflammation/Immunology
|
|
Kit-IN-9 (Compound D9) is an inhibitor of c-Kit. c-Kit-IN-9 inhibits the inflammatory responses in J774A.1, RAW264.7, MPMs cells and lung tissues by blocking the activation of the NF-κB pathway induced by LPS (HY-D1056). Meanwhile, c-Kit-IN-9 exhibits good anti-inflammatory activities in acute lung injury and sepsis mouse models. c-Kit-IN-9 can be used in the research of acute lung injury and related inflammatory diseases .
|
-
- HY-111947
-
|
|
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-149019
-
|
|
c-Kit
Apoptosis
|
Cancer
|
|
Antitumor agent-70 (compound 8b) has anti-tumor activity and can induce cell apoptosis. Antitumor agent-70 inhibits multiple myeloma with an IC50 value of 0.12 μM. Antitumor agent-70 is a potential multi-targeted kinase inhibitor especially for c-Kit .
|
-
- HY-147864
-
|
|
c-Fms
c-Kit
Apoptosis
|
Cancer
|
|
c-Fms-IN-12 (Compound 4g) is an FMS kinase inhibitor. c-Fms-IN-12 can also inhibits c-KIT. c-Fms-IN-12 is a potential broad-spectrum anticancer agent against multiple cancer types. c-Fms-IN-12 induces A549 cell apoptosis .
|
-
- HY-W011873R
-
|
|
Reference Standards
Endogenous Metabolite
|
Neurological Disease
|
|
Pazopanib (Hydrochloride) (Standard) is the analytical standard of Pazopanib (Hydrochloride). This product is intended for research and analytical applications. 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.
|
-
- HY-12009S
-
|
GW786034-13C,d3 hydrochloride
|
VEGFR
PDGFR
Autophagy
c-Fms
FGFR
c-Kit
|
Cancer
|
|
Pazopanib- 13C,d3 (hydrochloride) is the deuterium and 13C labeled Pazopanib hydrochloride . 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 .
|
-
- HY-15463S2
-
|
STI571-d3 hydrochloride; CGP-57148B-d3 hydrochloride
|
Autophagy
Bcr-Abl
c-Kit
SARS-CoV
PDGFR
|
Cancer
|
|
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-10208S1
-
|
GW786034-13C,d3
|
VEGFR
PDGFR
Autophagy
FGFR
c-Kit
|
Cancer
|
|
Pazopanib- 13C,d3 is the deuterium and 13C 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-131275
-
|
|
Drug Metabolite
|
Others
|
|
Imatinib Impurity E is the impurity of Imatinib. Imatinib 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-18187
-
|
|
Apoptosis
|
Cancer
|
|
Ki 23057 is a competitive, orally active inhibitor for tyrosine kinase, which inhibits the phosphorylation of K-samII/FGF-R2, VEGF-R1, VEGF-R2, PDGF-Rβ and c-Kit, with IC50s of 88, 69, 83, 100 and 480 nM. Ki 23057 inhibits the proliferation of sclerogastric cancer cells OCUM-2MD3 and OCUM-8, and induces apoptosis. Ki 23057 exhibits antitumor efficacy in mouse models .
|
-
- HY-179563
-
|
|
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-179563A
-
|
|
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-13645A
-
|
|
VEGFR
c-Kit
PDGFR
|
Cancer
|
|
Henatinib maleate is an orally active small-molecule multikinase inhibitor that has demonstrated broad and potent antitumor activities. Henatinib maleate inhibits the activity of VEGFR-2, c-kit, PDGFR with IC50 values of 0.6 nM, 3.3 nM and 41.5 nM, respectively. Henatinib maleate significantly inhibits VEGFR-2 phosphorylation and its downstream signal pathway .
|
-
- HY-181518
-
|
|
c-Kit
|
Cancer
|
|
c-Kit-IN-15 is a c-Kit inhibitor. c-Kit-IN-15 inhibits the c-Kit signaling pathway and suppresses cancer cell proliferation. c-Kit-IN-15 can be used in research related to hepatocellular carcinoma and breast cancer .
|
-
- HY-180653
-
|
|
c-Kit
|
Inflammation/Immunology
|
|
c-Kit-IN-14 (Compound 1) is a c-kit kinase inhibitor. c-Kit-IN-14 inhibits the phosphorylation of wild-type c-kit, with an IC50 of 0.4 nM for pKIT. c-Kit-IN-14 inhibits Exon 11 KIT, with an IC50 of 0.4 nM. c-Kit-IN-14 can be used in the research of mast cell-mediated diseases such as urticaria .
|
-
- HY-180652
-
|
|
c-Kit
|
Inflammation/Immunology
|
|
c-Kit-IN-13 (Compound I) is a c-kit kinase inhibitor. c-Kit-IN-13 inhibits the autophosphorylation of wild-type c-kit, with an IC50 of 0.3 nM for pKIT. c-Kit-IN-13 inhibits Exon 11 KIT, with an IC50 of 0.9 nM. c-Kit-IN-13 can be used in the research of mast cell-mediated diseases such as urticaria .
|
-
- HY-18909
-
|
|
Src
Bcr-Abl
Pyk2
p38 MAPK
c-Kit
|
Others
|
|
Multi-kinase-IN-11 (Compound 1a) is a DFG-out conformation-targeted multi-kinase inhibitor, including SRC, LCK, ABL, PYK2, CSK, HCK, P38 and C-KIT. Multi-kinase-IN-11 serves as a scaffold for the preparation of fluorescently labeled binding probes and affinity matrices .
|
-
- HY-103032R
-
|
|
Reference Standards
PDGFR
c-Kit
Bcr-Abl
|
Cancer
|
|
Multi-kinase inhibitor 1 (Standard) is the analytical standard of Multi-kinase inhibitor 1 (HY-103032). This product is intended for research and analytical applications. 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-50905S
-
|
|
FLT3
c-Kit
FGFR
VEGFR
PDGFR
c-Fms
|
Cancer
|
|
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 .
|
-
- HY-18949
-
|
|
FLT3
JAK
c-Kit
|
Cancer
|
|
JI6 is a potent, selective and orally active FLT3 inhibitor, with IC50s of ~40, 8, and 4 nM for FLT3-WT, FLT3-D835Y, and FLT3-D835H, respectively. JI6 also inhibits JAK3 and c-Kit, with IC50s of ~250 and ~500 nM, respectively. JI6 can be used for the research of acute myeloid leukemia .
|
-
- HY-10230
-
|
PKC412; CGP 41251
|
PKC
VEGFR
c-Kit
NO Synthase
Apoptosis
|
Cancer
|
|
Midostaurin (PKC412; CGP 41251) is an orally active, reversible multi-targeted protein kinase inhibitor. Midostaurin 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 . Midostaurin also upregulates endothelial nitric oxide synthase (eNOS) gene expression. Midostaurin shows powerful anticancer effects .
|
-
- HY-10201AR
-
|
Bay 43-9006 tosylate (Standard)
|
Reference Standards
Raf
VEGFR
FLT3
Autophagy
Ferroptosis
Apoptosis
|
Cancer
|
|
Sorafenib tosylate (Standard) is the analytical standard of Sorafenib tosylate. This product is intended for research and analytical applications. Sorafenib tosylate (Bay 43-9006 tosylate) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib tosylate 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 tosylate induces autophagy and apoptosis. Sorafenib Tosylate has anti-tumor activity. Sorafenib tosylate is a ferroptosis activator .
|
-
- HY-10201S2
-
|
Bay 43-9006-13C,d3
|
Raf
VEGFR
FLT3
Autophagy
Apoptosis
Ferroptosis
|
Cancer
|
|
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 .
|
-
- HY-10201R
-
|
Bay 43-9006 (Standard)
|
Reference Standards
Raf
VEGFR
FLT3
Autophagy
Apoptosis
Ferroptosis
|
Cancer
|
|
Sorafenib (Standard) is the analytical standard of Sorafenib. This product is intended for research and analytical applications. 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 .
|
-
- HY-15463S3
-
|
STI571-13C,d3; CGP-57148B-13C,d3
|
Isotope-Labeled Compounds
Autophagy
SARS-CoV
Bcr-Abl
PDGFR
c-Kit
|
Cancer
|
|
Imatinib- 13C,d3 (STI571- 13C,d3) is 13C 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-178219
-
|
|
Drug-Linker Conjugates for ADC
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Bis-sulfone-(PEG24)-Glu-Val-Cit-PAB-MMAE is a drug-linker conjugate for ADC. Bis-sulfone-(PEG24)-Glu-Val-Cit-PAB-MMAE contains a linker and bioactive small molecule toxins MMAE (HY-15162). Bis-sulfone-(PEG24)-Glu-Val-Cit-PAB-MMAE can conjugate with NN2101 (HY-P991293) (anti c-Kit) for synthesizing NN3201. NN3201 rapidly internalizes and inhibits SCF-driven signaling, thereby delivering its payload to induce cell cycle arrest and apoptosis. NN3201 exhibits significant c-Kit-dependent anti-tumor efficacies in various tumor models, such as small cell lung cancer (SCLC) and gastrointestinal stromal tumor (GIST) .
|
-
- HY-150026
-
|
|
VEGFR
PDGFR
FGFR
c-Kit
Akt
Src
Apoptosis
|
Cancer
|
|
Multi-kinase-IN-2 (compound 7h) is an orally active and potent angiokinase inhibitor. Multi-kinase-IN-2 exhibits excellent inhibitory activity against angiokinases including VEGFR-1/2/3, PDGFRα/β, and FGFR-1, as well as LYN and c-KIT kinases. Multi-kinase-IN-2 significantly attenuates phosphorylation of AKT and ERK proteins. Multi-kinase-IN-2 induces cell apoptosis. Multi-kinase-IN-2 shows anticancer activity .
|
-
- HY-50905
-
|
CHIR-258; TKI258
|
FLT3
c-Kit
FGFR
VEGFR
PDGFR
c-Fms
|
Cancer
|
|
Dovitinib (CHIR-258) is an orally active, potent multi-targeted tyrosine kinase (RTK) inhibitor with IC50s of 1, 2, 36, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, CSF-1R, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively. Dovitinib has potent antitumor activity .
|
-
- HY-10230R
-
|
PKC412 (Standard); CGP 41251 (Standard)
|
Reference Standards
PKC
VEGFR
c-Kit
NO Synthase
Apoptosis
|
Cancer
|
|
Midostaurin (Standard) is the analytical standard of Midostaurin. This product is intended for research and analytical applications. Midostaurin (PKC412; CGP 41251) is an orally active, reversible multi-targeted protein kinase inhibitor. Midostaurin 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 . Midostaurin also upregulates endothelial nitric oxide synthase (eNOS) gene expression. Midostaurin shows powerful anticancer effects .
|
-
- HY-10514R
-
|
|
Reference Standards
PDK-1
IKK
Autophagy
|
Cancer
|
|
BX795 (Standard) is the analytical standard of BX795 (HY-10514). This product is intended for research and analytical applications. BX795 is a potent and selective inhibitor of PDK1, with an IC50 of 6 nM. BX795 is also a potent and relatively specific inhibitor of TBK1 and IKKε, with an IC50 of 6 and 41 nM, respectively. BX795 blocks phosphorylation of S6K1, Akt, PKCδ, and GSK3β, and has lower selectivity over PKA, PKC, c-Kit, GSK3β etc. BX795 modulates autophagy .
|
-
- HY-143895
-
|
|
FLT3
|
Cancer
|
|
FLT3-IN-12 is a potent, selective and orally active FLT3 kinase inhibitor with IC50s of 1.48 nM and 2.87 nM for FLT3-WT and FLT3-D835Y, respectively. FLT3-IN-12 possesses high selectivity over c-KIT (>1000-fold). FLT3-IN-12 has an excellent anti-AML (acute myeloid leukemia) activity (MV4-11, IC50 of 0.75 nM) .
|
-
- HY-10408R
-
|
|
Reference Standards
c-Fms
VEGFR
c-Kit
PDGFR
|
Inflammation/Immunology
|
|
Ki20227 (Standard) is the analytical standard of Ki20227 (HY-10408). This product is intended for research and analytical applications. Ki20227 is an orally active and highly selective c-Fms tyrosine kinase (CSF1R) inhibitor with IC50s of 2 nM, 12 nM, 451 and 217 nM for CSF1R, VEGFR2 (vascular endothelial growth factor receptor-2), c-Kit (stem cell factor receptor) and PDGFRβ (platelet-derived growth factor receptor β). Ki20227 suppresses osteoclast differentiation and osteolytic bone destruction .
|
-
- HY-10201S4
-
|
Donafenib tosylate; Bay 43-9006-d3 tosylate
|
Isotope-Labeled Compounds
Raf
VEGFR
FLT3
Autophagy
Apoptosis
Ferroptosis
|
Cancer
|
|
Sorafenib-d3 (Donafenib-d3) tosylate is the deuterium labeled Sorafenib (HY-10201). Sorafenib is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib-d3tosylate 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-d3tosylate induces autophagy and apoptosis. Sorafenib-d3tosylate has anti-tumor activity. Sorafenib is a ferroptosis activator .
|
-
- HY-143894
-
|
|
FLT3
|
Cancer
|
|
FLT3-IN-11 (compound 30) is a potent, selective and orally active FLT3 kinase inhibitor with IC50s of 7.22 nM and 4.95 nM for wild-type FLT3 and FLT3-D835Y, respectively. FLT3-IN-11 high selectivity for FLT3 over c-KIT (>1000-fold). FLT3-IN-11has excellent anti-acute myeloid leukemia (AML) activity (MV4-11 cells, IC50 of 3.2 nM) .
|
-
- HY-W751179
-
|
PKC412-13C6; CGP 41251-13C6
|
Isotope-Labeled Compounds
Apoptosis
VEGFR
PKC
c-Kit
NO Synthase
|
Cancer
|
|
Midostaurin- 13C6 (PKC412- 13C6) is the 13C-labeled Midostaurin (HY-10230). Midostaurin (PKC412; CGP 41251) is an orally active, reversible multi-targeted protein kinase inhibitor. Midostaurin 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 . Midostaurin also upregulates endothelial nitric oxide synthase (eNOS) gene expression. Midostaurin shows powerful anticancer effects .
|
-
- HY-50905R
-
|
CHIR-258 (Standard); TKI258 (Standard)
|
FLT3
c-Kit
FGFR
VEGFR
PDGFR
c-Fms
Reference Standards
|
Cancer
|
|
Dovitinib (Standard) is the analytical standard of Dovitinib. This product is intended for research and analytical applications. Dovitinib (CHIR-258) is an orally active, potent multi-targeted tyrosine kinase (RTK) inhibitor with IC50s of 1, 2, 36, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, CSF-1R, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively. Dovitinib has potent antitumor activity .
|
-
- HY-N0419
-
|
Quercetin-7-O-β-D-glucopyranoside
|
Glycosidase
c-Kit
MMP
VEGFR
Aurora Kinase
|
Metabolic Disease
Cancer
|
|
Quercimeritrin (Quercetin-7-O-β-D-glucopyranoside) is an orally active α-glucosidase inhibitor (with an IC50 of 79.88 μM against the Saccharomyces cerevisiae enzyme) and a P-gp substrate, with anti-angiogenic and antioxidant activities. Quercimeritrin does not cross the blood-brain barrier and does not inhibit cytochrome P450 enzymes. Quercimeritrin precisely binds to and inhibits the active sites of c-Kit, MMP-2, Aurora-A kinases and α-glucosidase, thereby disrupting target functions. Quercimeritrin effectively regulates postprandial blood glucose and also exhibits significant anti-angiogenic activity, which inhibits endothelial cell proliferation and microvascular growth. Quercimeritrin can be used in the research of diabetes and breast cancer .
|
-
- HY-156470
-
|
|
Trk Receptor
Anaplastic lymphoma kinase (ALK)
c-Kit
EGFR
Pim
Casein Kinase
Checkpoint Kinase (Chk)
CDK
Apoptosis
|
Cancer
|
|
Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that shows good enzyme inhibitory activity against TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. Multi-kinase-IN-6 reveals antiproliferative activity against MCF7, HCT116 and EKVX with IC50 values of 3.36 μM, 1.40 μM and 3.49 μM, respectively. Multi-kinase-IN-6 shows cell cycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells with good apoptotic effect .
|
-
- HY-179497
-
|
|
FLT3
VEGFR
Akt
STAT
ERK
Apoptosis
|
Cancer
|
FLT3-IN-37 (Compound 6z) is a potent inhibitor of FLT3-ITD, with IC50 values of 1.5 and 3.4 nM for FLT3-ITD and TEL-VEGFR2, respectively. FLT3-IN-37 exhibits high selectivity for wild-type FLT3 (WT) and c-Kit. FLT3-IN-37 inhibits FLT3 phosphorylation and downregulates the expression of p-Akt, p-STAT5, and p-ERK. FLT3-IN-37 exerts anti-leukemia effects by blocking the cell cycle and inducing apoptosis (apoptosis). FLT3-IN-37 can be used for research on acute myeloid leukemia (AML) .
|
-
- HY-179382
-
|
|
FLT3
Apoptosis
|
Cancer
|
|
HSB401 is an orally active FLT3 inhibitor (IC50: 28, 5, 72, 51 nM for FLT3-WT, FLT3-D835Y, FLT3-ITD-F691L, FLT3-ITD, respectively). HSB401 downregulates FLT3 signaling and induces cell cycle arrest and apoptosis. HSB401 spares c-KIT inhibition, thereby reducing the risk of myelosuppression. HSB401 significantly suppresses tumor growth in the MV4-11 xenograft mouse model. HSB401 can be used for the research of acute myeloid leukemia .
|
-
- HY-177578
-
|
|
Antibody-Drug Conjugates (ADCs)
c-Kit
Apoptosis
Microtubule/Tubulin
ERK
Akt
Caspase
|
Cancer
|
|
NN3201 is a c-Kit-targeting antibody-drug conjugate (ADC) with high affinity (KD = 0.19 pM). NN3201 is composed of 4-(3-Tosyl-2-(tosylmethyl)propanoyl)benzoic acid-glu(PEG24-Me)-val-cit-NH-benzyloxyformic acid-MMAE (HY-178219) and an anti-c-Kit human monoclonal antibody NN2101 (HY-P991293). NN3201 rapidly internalizes and inhibits stem cell factor (SCF)-driven signaling, thereby delivering its payload to induce cell cycle arrest and apoptosis. NN3201 exhibits no Fc-mediated effector functions antibody-dependent cell-mediated cytotoxicity (ADCC)/complement-dependent cytotoxicity (CDC) due to reduced FcγR binding. NN3201 exhibits significant c-Kit-dependent anti-tumor efficacies in various tumor models. NN3201 can be used in small cell lung cancer (SCLC) and gastrointestinal stromal tumor (GIST) and acute myeloid leukemia (AML) research [1][2].
|
-
- HY-164387
-
|
|
EGFR
PDGFR
VEGFR
|
Cancer
|
|
Sutetinib is an orally active inhibitor for tyrosine kinase, that is associated with tumor growth and angiogenesis, such as VEGFR (Ki= 0.009 µM for VEGFR-1/2/3), PDGFR (Ki= 0.008 µM for PDGFR-α/β) and proto-oncogene cKIT. Sutetinib inhibits the proliferation, migration, and tubular structure formation of endothelial cells and fibroblasts, and exhibits board-spectrum antitumor efficacy in vitro and in vivo .
|
-
- HY-164387A
-
|
|
EGFR
VEGFR
PDGFR
|
Cancer
|
|
Sutetinib maleate is the maleate form of Sutetinib (HY-164387). Sutetinib maleate is an orally active inhibitor for tyrosine kinase, that is associated with tumor growth and angiogenesis, such as VEGFR (Ki= 0.009 µM for VEGFR-1/2/3), PDGFR (Ki= 0.008 µM for PDGFR-α/β) and proto-oncogene cKIT. Sutetinib maleate inhibits the proliferation, migration, and tubular structure formation of endothelial cells and fibroblasts, and exhibits board-spectrum antitumor efficacy in vitro and in vivo .
|
-
- HY-W1117786
-
|
|
ADC Payload
NAMPT
|
Cancer
|
|
Nampt-IN-10 (Compound 4) is an efficient inhibitor of nicotinamide phosphoribosyltransferase (NAMPT). Nampt-IN-10 exhibits nanomolar-level inhibitory activity against cell lines such as MDA-MB453, NCI-N87, and NCI-H526. Nampt-IN-10 can be used as an ADC payload, and the ADC constructed with it as the core demonstrates significant anti-tumor activity .
|
-
- HY-101034
-
|
CHMFL-ABL-Kit-155
|
Bcr-Abl
c-Kit
Apoptosis
PDGFR
Discoidin Domain Receptor
|
Cancer
|
|
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 .
|
-
| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-P990851
-
|
|
c-Kit
|
Inflammation/Immunology
Cancer
|
|
Anti-c-Kit/CD117 Antibody (SR-1) is a kind of mouse IgG2a κ chimeric antibody inhibitor, targeting to human c-Kit/CD117. Anti-c-Kit/CD117 Antibody (SR-1) binds to the extracellular domain of human c-Kit (also known as CD117) and blocks stem cell factor (SCF) binding to CD117. Anti-c-Kit/CD117 Antibody (SR-1) can be used for the researches of cancer and immunology, such as gastrointestinal stromal tumor (GIST) and xenograft .
|
-
(5)
-
- HY-P990020
-
|
FSI-174
|
c-Kit
|
Others
|
|
Eglatoprutug is an humanized immunoglobulin G1-kappa, anti-c-Kit monoclonal antibody .
|
-
(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N0419
-
-
-
- HY-W011873R
-
|
|
Structural Classification
Human Gut Microbiota Metabolites
Microorganisms
Ketones, Aldehydes, Acids
Endogenous metabolite
Source Classification
|
Reference Standards
Endogenous Metabolite
|
|
Pazopanib (Hydrochloride) (Standard) is the analytical standard of Pazopanib (Hydrochloride). This product is intended for research and analytical applications. 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.
|
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-15463S1
-
|
|
|
Imatinib-d4 (STI571-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 .
|
-
-
- HY-13904S
-
|
|
|
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 .
|
-
-
- HY-15463S
-
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 .
|
-
-
- HY-13342AS
-
|
|
|
Apatinib-d8 (free base) is the deuterium labeled Apatinib free base . 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 .
|
-
-
- HY-10201S2
-
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 .
|
-
-
- HY-10208S
-
|
|
|
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-10230S
-
|
|
|
Midostaurin-d5 (PKC412-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 .
|
-
-
- HY-W705479
-
|
|
|
Pazopanib-d3 (hydrochloride) (GW786034-d3 (hydrochloride)) is deuterium labeled Pazopanib (Hydrochloride). 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.
|
-
-
- HY-10208S2
-
|
|
|
Pazopanib-d3 (GW786034-d3) is 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-50905S
-
|
|
|
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 .
|
-
-
- HY-15463S3
-
|
|
|
Imatinib- 13C,d3 (STI571- 13C,d3) is 13C 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-12009S
-
|
|
|
Pazopanib- 13C,d3 (hydrochloride) is the deuterium and 13C labeled Pazopanib hydrochloride . 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 .
|
-
-
- HY-15463S2
-
|
|
|
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-10208S1
-
|
|
|
Pazopanib- 13C,d3 is the deuterium and 13C 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-10201S4
-
|
|
|
Sorafenib-d3 (Donafenib-d3) tosylate is the deuterium labeled Sorafenib (HY-10201). Sorafenib is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib-d3tosylate 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-d3tosylate induces autophagy and apoptosis. Sorafenib-d3tosylate has anti-tumor activity. Sorafenib is a ferroptosis activator .
|
-
-
- HY-W751179
-
|
|
|
Midostaurin- 13C6 (PKC412- 13C6) is the 13C-labeled Midostaurin (HY-10230). Midostaurin (PKC412; CGP 41251) is an orally active, reversible multi-targeted protein kinase inhibitor. Midostaurin 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 . Midostaurin also upregulates endothelial nitric oxide synthase (eNOS) gene expression. Midostaurin shows powerful anticancer effects .
|
-
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