Shopping Cart

Remove All
Your shopping cart is currently empty

Tyrosine Kinase/Adaptors

Discoidin Domain Receptor (DDR)

c-Kit

Proto-oncogene c-KIT is the gene encoding the receptor tyrosine kinase protein known as tyrosine-protein kinase KIT, CD117 (cluster of differentiation 117) or mast/stem cell growth factor receptor (SCFR). Multiple transcript variants encoding different isoforms have been found for this gene.KIT is a cytokine receptor expressed on the surface of hematopoietic stem cells as well as other cell types. Altered forms of this receptor may be associated with some types of cancer. KIT is a receptor tyrosine kinase type III, which binds to stem cell factor (a substance that causes certain types of cells to grow), also known as "steel factor" or "c-kit ligand".

Filter HomeSignaling PathwaysTyrosine Kinase/Adaptorsc-Kit

Lenvatinib

T0520417716-92-8

Lenvatinib (E7080) is a multi-target receptor tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, KIT, PDGFR, and RET, and has oral activity. Lenvatinib has the strongest inhibitory activity on VEGFR2 and VEGFR3 (IC50=4 5.2 nM). Lenvatinib has strong anti-tumor activity.

In Stock

Size

QTY

Cited

Avapritinib

T51091703793-34-3

Avapritinib (BLU-285) is a selective, highly potent, and orally active inhibitor of KIT and PDGFRA activation loop mutant kinases, targeting KIT D816V (IC50:0.27 nM) and PDGFRA D842V (IC50:0.24 nM), and attenuates the transport functions of ABCB1 and ABCG2. It binds to the active conformation of the kinases and exhibits antitumor activity.

In Stock

Size

QTY

Ripretinib

T84821442472-39-0

Ripretinib (DCC-2618) is an orally bioavailable inhibitor of (KIT) and (PDGFRA).

In Stock

Size

QTY

Sorafenib

T0093L284461-73-0

Sorafenib (Bay 43-9006) is a multikinase inhibitor that targets Raf-1, B-Raf, VEGFR2, VEGFR3, VEGFR4, PDGFRβ, FLT3, c-Kit, and others (IC50=6 22 90 15 20 20 57 58 nM) with oral activity. It exhibits antitumor properties and can induce autophagy, apoptosis, and agonistic iron death.

In Stock

Size

QTY

Cited

Pexidartinib

T21151029044-16-3

Pexidartinib (PLX-3397) is a capsule containing a small-molecule receptor tyrosine kinase (RTK) inhibitor targeting KIT, CSF1R, and FLT3, with potential antineoplastic activity.

In Stock

Size

QTY

Cited

Gilteritinib

T44091254053-43-4

Gilteritinib (ASP2215) is a potent inhibitor of FMS-related tyrosine kinase 3 (FLT3) and AXL tyrosine kinase receptors (IC50 = 0.29 nM and <1 nM, respectively). In preclinical studies, gilteritinib demonstrated strong antileukemic and antitumor effects. Gilteritinib is currently in several Phase 3 clinical trials for acute myeloid leukemia.

In Stock

Size

QTY

Cited

Regorafenib

T1792755037-03-7

Regorafenib (BAY 73-4506) is an orally active, multi-targeted receptor tyrosine kinase inhibitor that inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ, exhibiting both antitumor and anti-angiogenic activity.

In Stock

Size

QTY

Cited

CP-673451

T6091343787-29-1

CP-673451 is a specific inhibitor of PDGFRα β (IC50: 10 1 nM) with antiangiogenic and antitumor activity and the selectivity is higher 450-fold than other angiogenic receptors.

In Stock

Size

QTY

Cited

Dasatinib

T1448302962-49-8

Dasatinib (BMS-354825) is an orally active, ATP-competitive tyrosine kinase inhibitor that targets Src and Bcr-Abl (Ki=16 30 pM), with antitumor activity, used in the treatment of leukemia and lymphoma.

In Stock

Size

QTY

Cited

Cabozantinib

T2586849217-68-1

Cabozantinib (XL184) is a multi-targeted tyrosine kinase receptor inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt3 (IC50=0.035 1.3 4.6 7 11.3 nM). Cabozantinib exhibits both antitumor and antiangiogenic activity.

In Stock

Size

QTY

Cited

Axitinib

T1452319460-85-0

Axitinib (AG-013736) is a multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1, VEGFR2, VEGFR3, and PDGFRβ (IC50=4 20 0.4 2 nM). Axitinib has antitumor activity and is used in the treatment of renal cell carcinoma.

In Stock

Size

QTY

Cited

Imatinib Mesylate

T1621220127-57-1

Imatinib Mesylate (STI-571) is a tyrosine kinase receptor inhibitor with antineoplastic activity (IC50s: 0.6 μM, 0.1 μM and 0.1 μM for v-Abl, c-Kit and PDGFR, respectively).

In Stock

Size

QTY

Cited

Labuxtinib

T798511426449-01-5

Labutinib is a selective inhibitor of the c-kit tyrosine kinase [1].

$142

In Stock

Size

QTY

Ponatinib

T2372943319-70-8

Ponatinib (AP24534) is an orally available, multitargeted kinase inhibitor with IC50 values of 0.37 nM (Abl), 1.1 nM (PDGFRα), 1.5 nM (VEGFR2), 2.2 nM (FGFR1), and 5.4 nM (Src).

In Stock

Size

QTY

Cited

JNK-IN-8

T26681410880-22-6

JNK-IN-8 (JNK Inhibitor XVI) is an irreversible JNK1 2 4 inhibitor (IC50: 4.7 18.7 1 nM) with over 10-fold selectivity compared to MNK2 and Fms, and no inhibition of Met, c-Kit, or PDGFRβ in the A375 cell line.

In Stock

Size

QTY

Cited

Lenvatinib mesylate

T8541857890-39-2

Lenvatinib mesylate (E7080 (mesylate)) is an oral and multi-targeted inhibitor of VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, with potent antitumor activities.

In Stock

Size

QTY

Cited

BX795

T1830702675-74-9

BX795 is an effective and selective PDK1 inhibitor (IC50: 6 nM), and its selectivity is 140- and 1600-fold for PDK1 over PKA and PKC in cell-free assays, respectively. Meanwhile, the selectivity for PDK1 is 100-fold than GSK3β.

In Stock

Size

QTY

Sunitinib

T0374L557795-19-4

Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that inhibits VEGFR2 and PDGFRβ (IC50=80 2 nM). It exhibits antitumor activity and is used for treating kidney cancer and gastrointestinal tumors.

In Stock

Size

QTY

Cited

Imatinib

T6230152459-95-5

Imatinib (STI571) is a multi-targeted receptor tyrosine kinase inhibitor that selectively inhibits the kinase activities of BCR ABL, v-Abl, PDGFR, and c-kit with oral activity. Imatinib has antitumor activity for the treatment of chronic granulocytic leukemia.

In Stock

Size

QTY

Cited

Edicotinib

T151991142363-52-7

Edicotinib (JNJ-527) is a blood-brain-penetrating, orally active, selective CSF-1R inhibitor (IC50 value is 3.2 nM), with less inhibitory effects on KIT (IC50 value is 20 nM) and FLT3 (IC50 value is 190 nM). Edicotinib (JNJ-527) can block microglial proliferation and attenuate neurodegeneration, and can be used to study Alzheimer's disease and rheumatoid arthritis.

In Stock

Size

QTY

Dovitinib

T6289405169-16-6

Dovitinib is an orally active, multi-targeted tyrosine kinase (RTK) inhibitor with anti-tumor effects.

In Stock

Size

QTY

Chiauranib

T355701256349-48-0

Chiauranib is a multi-target inhibitor against tumor angiogenesis and exhibits potent anticancer effects. Chiauranib potently inhibits the angiogenesis-related kinases (VEGFR1, VEGFR2, VEGFR3, PDGFRα and c-Kit), mitosis-related kinase Aurora B, and chronic inflammation-related kinase CSF1R, with IC50 values ranging from 1-9 nM.

In Stock

Size

QTY

Cediranib

T2500288383-20-0

Cediranib (AZD2171) (AZD2171) is a highly potent (IC50 < 1 nmol L) ATP-competitive inhibitor of recombinant KDR tyrosine kinase in vitro, also inhibits Flt1 4 (IC50: 5 nM ≤3 nM), similar activity against PDGFRβ and c-Kit, selective more for VEGFR than PDGFR-α (36-fold), CSF-1R (110-fold), and Flt3 (1000-fold) in HUVEC cells.

In Stock

Size

QTY

Cited

Dasatinib monohydrate

T1448L863127-77-9

Dasatinib monohydrate (BMS-354825 Monohydrate) is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. Dasatinib monohydrate binds to and inhibits the growth-promoting activities of these kinases. Apparently, because of its less stringent binding affinity for the BCR-ABL kinase, Dasatinib monohydrate has been shown to overcome the resistance to imatinib of chronic myeloid leukemia (CML) cells harboring BCR-ABL kinase domain point mutations.

In Stock

Size

QTY

Cited

Bezuclastinib

T609761616385-51-3

Bezuclastinib (CGT9486) is a novel, potent and highly selective tyrosine kinase and c-kit D816V inhibitor for the study of advanced mastocytosis.

$179

In Stock

Size

QTY

Dovitinib lactate hydrate

T6479915769-50-5

Dovitinib lactate hydrate (TKI258) is the Lactate of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3 c-Kit) with IC50 of 1 nM 2 nM, also potent to class IV (FGFR1 3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Phase 4.

In Stock

Size

QTY

Sorafenib tosylate

T0093475207-59-1

Sorafenib tosylate (Bay 43-9006) is a potent multikinase inhibitor (IC50s: 6 20 22 nM for Raf-1 VEGFR-3 B-Raf).

In Stock

Size

QTY

Cited

Pazopanib

T0097L444731-52-6

Pazopanib (GW786034) is an inhibitor of protein tyrosine kinases that inhibits VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms (IC50=10 30 47 84 74 140 146 nM). Pazopanib has antitumor activity.

In Stock

Size

QTY

Cited

BLU-263

T92952505078-08-8

BLU-263 is an investigational, potent, and selective oral small molecule inhibitor of KIT with sub-nanomolar potency against D816V-mutant KIT.

In Stock

Size

QTY

Vimseltinib

T106521628606-05-2

Vimseltinib (DCC-3014) is a dual inhibitor targeting c-FMS (CSF-IR) and c-Kit with IC50 values of less than 0.01 μM and 0.1-1 μM, respectively.

In Stock

Size

QTY

Sitravatinib

T43491123837-84-2

Sitravatinib (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα β, PDGFR, and Axl.

In Stock

Size

QTY

Cited

GW786034B

T6930635702-64-6

Pazopanib Hydrochloride (Votrient HCl) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively.

In Stock

Size

QTY

Linifanib

T2514796967-16-3

Linifanib (AL-39324) (ABT-869) is a novel, potent ATP-competitive VEGFR PDGFR inhibitor for KDR (IC50: 4 nM), CSF-1R (IC50: 3 nM), Flt-1 3 (IC50: 3 4 nM) and PDGFRβ (IC50: 66 nM). Linifanib may exhibit potent antiproliferative and apoptotic effects on tumor cells whose proliferation is dependent on mutant kinases, such as FMS-related tyrosine kinase receptor-3 (FLT3).

In Stock

Size

QTY

Cabozantinib hydrochloride

T51641817759-42-4

Cabozantinib hydrochloride (XL184) is a potent pan-tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt4 (IC50s: 0.035, 1.3, 4.6, 7 and 6 nM).

In Stock

Size

QTY

Flumatinib

T4320895519-90-1

Flumatinib (HHGV678) is an orally bioavailable tyrosine kinase inhibitor with potential antineoplastic activity.

In Stock

Size

QTY

Masitinib mesylate

T85441048007-93-7

Masitinib mesylate (AB-1010 mesylate) is a selective, orally bioavailable c-Kit inhibitor with an IC50 of 200 nM for human recombinant c-Kit, and IC50 values of 540 800 nM and 510 nM for PDGFRα β and LynB, respectively.

In Stock

Size

QTY

Agerafenib

T20701188910-76-0

Agerafenib (CEP32496) is a highly potent inhibitor of BRAF.

In Stock

Size

QTY

Dovitinib lactate

T7104692737-80-7

Dovitinib lactate (TKI-258 lactate)(TKI258) lactate is a potent inhibitor of fibroblast growth factor receptor 3 (FGFR3) (IC50 :5 nM).

In Stock

Size

QTY

Sunitinib Malate

T0374341031-54-7

Sunitinib Malate (Sunitinib) is an indolinone-based tyrosine kinase inhibitor. It blocks the tyrosine kinase activities of VEGFR2, PDGFRβ (IC50: 80 2 nM), and c-kit.

In Stock

Size

QTY

AZD3229

T54092248003-60-1

AZD3229 is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors. It demonstrates potent single-digit nM growth inhibition across a broad cell panel.

In Stock

Size

QTY

N-Desmethyl imatinib

T11641404844-02-6

N-Desmethyl imatinib (Imatinib metabolite N-Desmethyl imatinib) is a metabolite of Imatinib, which is a multi-target inhibitor of c-Kit, v-Abl, and PDGFR.

In Stock

Size

QTY

PP1

T6196172889-26-8

PP1 (AGL 1872), a specific and effective Src inhibitor, is with IC50 for Lck Fyn is 5 nM 6 nM, respectively.

In Stock

Size

QTY

Cited

KI8751

T2446228559-41-9

KI8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM.

In Stock

Size

QTY

AMG-25

T222561003311-62-3

AMG-25 (c-Kit-IN-5-1) is a selective and potent c-Kit inhibitor that inhibits c-Kit, KDR, p38, Lck, and Src, and can be used in the study of mast cell-associated fibrosis.

$499

In Stock

Size

QTY

Regorafénib N-oxyde (M2)

T10157835621-11-9

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

In Stock

Size

QTY

Dasatinib hydrochloride

T22303854001-07-3

Dasatinib hydrochloride (BMS-354825 HCl) (BMS-354825) hydrochloride is a highly potent, ATP competitive, orally active dual Src Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib hydrochloride hydrochloride inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib hydrochloride hydrochloride also induces Apoptosis and Autophagy.

In Stock

Size

QTY

Masitinib

T2609790299-79-5

Masitinib (AB1010) is a tyrosine-kinase inhibitor used in the treatment of mast cell tumors in animals, specifically dogs. Since its introduction in November 2008 it has been distributed under the commercial name Masivet. It has been available in Europe since the second part of 2009. In the USA it is distributed under the name Kinavet and has been available for veterinaries since 2011.

In Stock

Size

QTY

Motesanib Diphosphate

T2288L857876-30-3

Motesanib Diphosphate (AMG 706) is the orally bioavailable diphosphate salt of a multiple-receptor tyrosine kinase inhibitor with potential antineoplastic activity.

In Stock

Size

QTY

Go to page 1

Page of 2