Search Result

Results for "

PDGFR kinase

" in MedChemExpress (MCE) Product Catalog:

By Targets:	PDGFR (138) Akt (3) AMPK (1) Apoptosis (30) Aurora Kinase (3) Autophagy (35) Bcr-Abl (21) c-Fms (9) c-Kit (58) c-Met/HGFR (6) c-Myc (1) Casein Kinase (1) CDK (2) Collagen (1) DAPK (1) Discoidin Domain Receptor (2) DNA Alkylator/Crosslinker (1) DNA-PK (1) Drug Derivative (1) Drug Metabolite (3) DYRK (1) EGFR (11) Endogenous Metabolite (1) Environmental Pollutants (1) Ephrin Receptor (2) ERK (3) FGFR (45) FLT3 (23) Haspin Kinase (1) IGF-1R (1) Influenza Virus (2) IPK Superfamily (1) IRE1 (7) Isotope-Labeled Compounds (4) JAK (1) MEK (1) MELK (1) Mitophagy (7) Mitosis (2) MNK (1) mTOR (3) Necroptosis (1) Phosphodiesterase (PDE) (1) PI3K (1) RAD51 (3) Raf (7) Reference Standards (31) RET (24) RIP kinase (1) SARS-CoV (6) Src (22) TGF-beta/Smad (1) TGF-β Receptor (2) Tie (6) Tyrosinase (2) VEGFR (98)
By Research Areas:	Cancer (140) Cardiovascular Disease (11) Endocrinology (2) Infection (9) Inflammation/Immunology (12) Metabolic Disease (1) Neurological Disease (3)

By Targets:

PDGFR (138)

Akt (3)

AMPK (1)

Apoptosis (30)

Aurora Kinase (3)

Autophagy (35)

Bcr-Abl (21)

c-Fms (9)

c-Kit (58)

c-Met/HGFR (6)

c-Myc (1)

Casein Kinase (1)

CDK (2)

Collagen (1)

DAPK (1)

Discoidin Domain Receptor (2)

DNA Alkylator/Crosslinker (1)

DNA-PK (1)

Drug Derivative (1)

Drug Metabolite (3)

DYRK (1)

EGFR (11)

Endogenous Metabolite (1)

Environmental Pollutants (1)

Ephrin Receptor (2)

ERK (3)

FGFR (45)

FLT3 (23)

Haspin Kinase (1)

IGF-1R (1)

Influenza Virus (2)

IPK Superfamily (1)

IRE1 (7)

Isotope-Labeled Compounds (4)

JAK (1)

MEK (1)

MELK (1)

Mitophagy (7)

Mitosis (2)

MNK (1)

mTOR (3)

Necroptosis (1)

Phosphodiesterase (PDE) (1)

PI3K (1)

RAD51 (3)

Raf (7)

Reference Standards (31)

RET (24)

RIP kinase (1)

SARS-CoV (6)

Src (22)

TGF-beta/Smad (1)

TGF-β Receptor (2)

Tie (6)

Tyrosinase (2)

VEGFR (98)

By Research Areas:

Cancer (140)

Cardiovascular Disease (11)

Endocrinology (2)

Infection (9)

Inflammation/Immunology (12)

Metabolic Disease (1)

Neurological Disease (3)

157

Inhibitors & Agonists

Screening Libraries

Fluorescent Dyes

Biochemical Assay Reagents

Isotope-Labeled Compounds

GMP Molecules

Targets Recommended: PDGFR

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-10981

Lenvatinib 90+ 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-15463

Imatinib Maximum Cited Publications 120 Publications Verification 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-10255A

Sunitinib 90+ Cited Publications SU 11248	VEGFR PDGFR IRE1 Mitophagy Autophagy Apoptosis	Cancer
Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC₅₀s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively . Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .

HY-10065

Axitinib 35+ Cited Publications AG-013736	VEGFR PDGFR	Cancer
Axitinib is a multi-targeted tyrosine kinase inhibitor with IC₅₀s of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFRβ, respectively.

HY-12047

Ponatinib 45+ Cited Publications AP24534	Bcr-Abl PDGFR VEGFR FGFR Src Autophagy	Cancer
Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC₅₀s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively .

HY-50946

Imatinib Mesylate Maximum Cited Publications 120 Publications Verification STI571 Mesylate; CGP-57148B Mesylate	c-Kit Bcr-Abl PDGFR Autophagy	Infection Neurological Disease Inflammation/Immunology Cancer
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-10255

Sunitinib Malate 90+ Cited Publications SU 11248 Malate	PDGFR VEGFR IRE1 Mitophagy Autophagy Apoptosis	Infection Inflammation/Immunology Cancer
Sunitinib (SU 11248) Malat is a multi-targeted receptor tyrosine kinase inhibitor with IC₅₀s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively . Sunitinib Malat, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .

HY-13223

Crenolanib 15+ Cited Publications CP-868596	FLT3 PDGFR Autophagy	Cancer
Crenolanib is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with K_ds of 0.74 nM and 2.1 nM/3.2 nM, respectively.

HY-10407

SU 5402 10+ Cited Publications	VEGFR FGFR PDGFR	Cancer
SU 5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC₅₀ of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGFRβ, respectively.

HY-50751

Linifanib 5 Publications Verification ABT-869; AL-39324	PDGFR VEGFR FLT3 c-Fms c-Kit Autophagy Apoptosis	Cancer
Linifanib (ABT-869) is a potent and orally active multi-target inhibitor of VEGFR and *PDGFR* family with IC₅₀s of 4, 3, 66, and 4 nM for KDR, FLT1, PDGFRβ, and FLT3, respectively. Linifanib shows prominent antitumor activity. Linifanib has much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. Linifanib is a specific miR-10b inhibitor that blocks miR-10b biogenesis .

HY-50905

Dovitinib 10+ Cited Publications 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-10205

Cediranib 10+ Cited Publications 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-10981A

Lenvatinib mesylate 90+ 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-108766

Ponatinib hydrochloride 45+ Cited Publications AP24534 hydrochloride	Bcr-Abl FGFR PDGFR VEGFR Src Autophagy	Infection Cancer
Ponatinib hydrochloride (AP24534 hydrochloride) is a hydrochloride of ponatinib. Ponatinib is an orally active multi-targeted kinase inhibitor with IC₅₀s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively .

HY-13302

CP-547632 1 Publications Verification	VEGFR FGFR	Cancer
CP-547632 is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC₅₀s of 11 nM and 9 nM, respectively. CP-547632 is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 has antitumor efficacy .

HY-101957

AG 1295 4 Publications Verification	PDGFR	Cardiovascular Disease
AG 1295 is a selective platelet-derived growth factor receptor (PDGFR) tyrosine-kinase inhibitor. AG1295 abolishes autophosphorylation of the PDGFR whereas not affects the autophosphorylation of the EGF receptor .

HY-16265

JI-101	Ephrin Receptor PDGFR VEGFR	Cardiovascular Disease Cancer
JI-101 is an orally available multi-kinase inhibitor of VEGFR2, PDGFRβ and EphB4 with potent anti-cancer activity.

HY-10330A

Toceranib phosphate SU11654 phosphate; PHA 291639E phosphate	PDGFR VEGFR c-Kit	Cancer
Toceranib phosphate (SU11654 phosphate) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits *PDGFR, VEGFR, and Kit* with K_is of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. Toceranib phosphate (SU11654 phosphate) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors .

HY-10372

PP121 4 Publications Verification	mTOR PDGFR VEGFR Src Apoptosis	Cancer
PP121 is a multi-targeted kinase inhibitor with IC₅₀s of 10, 60, 12, 14, 2 nM for mTOR, DNK-PK, VEGFR2, Src, *PDGFR*, respectively.

HY-10517

Orantinib 5+ Cited Publications SU6668; TSU-68	PDGFR FGFR VEGFR Apoptosis	Cancer
Orantinib (SU6668; TSU-68) is a multi-targeted receptor tyrosine kinase inhibitor with K_is of 2.1 μM, 8 nM and 1.2 μM for Flt-1, PDGFRβ and FGFR1, respectively.

HY-10330

Toceranib SU11654; PHA 291639E	PDGFR VEGFR c-Kit	Cancer
Toceranib phosphate (SU11654 phosphate) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits *PDGFR, VEGFR, and Kit* with K_is of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. Toceranib phosphate (SU11654 phosphate) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors .

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-124526

Chiauranib 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-15511

Tyrphostin A9 5+ Cited Publications Tyrphostin 9; Malonoben	Environmental Pollutants VEGFR PDGFR Influenza Virus	Infection Cancer
Tyrphostin A9, a *PDGFR* inhibitor, is a potent inducer of mitochondrial fission. Tyrphostin A9 emerged as the most potent and selective of 51 tyrosine kinase inhibitors tested against the TNF-induced respiratory burst. Tyrphostin A9 has anti-influenza virus activities.

HY-10207

Dovitinib lactate 10+ Cited Publications 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-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-13896

PD168393 3 Publications Verification	EGFR Autophagy Apoptosis	Cancer
PD168393 is a potent, selective and cell-permeable inhibitor of EGFR tyrosine kinase and ErbB2. PD168393 irreversiblely inactivates EGF receptor ( IC₅₀=0.7 nM) and is inactive against insulin receptor, PDGFR, FGFR and PKC .

HY-100315

XL 999 Tyrosine kinase-IN-1	VEGFR PDGFR FGFR	Cardiovascular Disease Cancer
XL999 is a multi-target tyrosine kinase inhibitor. XL999 has IC₅₀ values for KDR, Flt-1, FGFR1 and PDGFRα of 4 nM, 20 nM, 4 nM and 2 nM, respectively. XL999 can be used in the research of cancer .

HY-10065S

Axitinib-13C,d3 AG-013736-¹³C，d₃	VEGFR PDGFR	Cancer
Axitinib- ¹³C,d₃ is a ¹³C-labeled and deuterium labeled Axitinib. Axitinib is a multi-targeted tyrosine kinase inhibitor with IC₅₀ values of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFRβ, respectively .

HY-111507

PDGFRα kinase inhibitor 1 1 Publications Verification	PDGFR	Cancer
PDGFRα kinase inhibitor 1 is a highly selective type II PDGFRα kinase inhibitor with IC₅₀s of 132 nM and 6115 nM for PDGFRα and PDGFRβ, respectively .

HY-W011266

JNJ-10198409 1 Publications Verification	PDGFR	Cancer
JNJ-10198409 is a relatively selective, orally active, and ATP competitive *PDGF-RTK* (platelet-derived growth factor receptor tyrosine kinase) inhibitor (IC₅₀=2 nM). It is a dual-mechanism, antiangiogenic, and tumor cell antiproliferative agent. JNJ-10198409 has good activity against *PDGFR-β* kinase (IC₅₀=4.2 nM) and *PDGFR-α* kinase (IC₅₀=45 nM) .

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-15463S1

Imatinib-d4 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-112412

PDGFR Tyrosine kinase-IN-1	PDGFR	Neurological Disease
PDGFR Tyrosine kinase-IN-1, a multikinase inhibitor, inhibits PDGFR, EGFR, FGFR, PKA, and PKC, respectively. PDGFR Tyrosine kinase-IN-1 can be used for the research of amyotrophic lateral sclerosis .

HY-10185

TG 100572 Hydrochloride 3 Publications Verification	Src VEGFR FGFR PDGFR	Inflammation/Immunology
TG 100572 Hydrochloride is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC₅₀s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.

HY-10981S

Lenvatinib-d4 E7080-d₄	VEGFR FGFR PDGFR c-Kit RET	Cancer
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 .

HY-147243

Ansornitinib ANG-3070	VEGFR PDGFR	Cardiovascular Disease Inflammation/Immunology
Ansornitinib is an orally active dual kinase inhibitor that inhibits platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR2). Ansornitinib can be used as an antifibrotic agent in lung, liver, kidney, and gastrointestinal fibrotic diseases .

HY-21291

SU-4313	PDGFR EGFR IGF-1R	Cancer
SU-4313 is a potent *protein tyrosine kinases* (PTKs) modulator with IC₅₀*s of 14.5 μM, 18.8 μM, 11 μM, 16.9 μM, 8.0 μM for PDGFR, FLK-1, EGFR, HER2 Kinase* and IGF-1R, respectively. SU-4313 has the potential for modulating tyrosine kinase signal transduction in order to regulate abnormal cell proliferation .

HY-42933

PDGFR-IN-2	PDGFR	Cardiovascular Disease
PDGFR-IN-2 (Compound 16C) is a 4-phenoxyquinoline derivative. PDGFR-IN-2 is a platelet-derived growth factor receptor (PDGFr) inhibitor (IC₅₀: 0.20 μM). PDGFR-IN-2 inhibits the activity of PDGFr tyrosine kinase .

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 .

HY-W143698

PDGFRα kinase inhibitor 2	Bcr-Abl c-Kit PDGFR	Cancer
PDGFRα kinase inhibitor 2 (compound 1), an Imatinib (HY-15463) analogue, is a covalent and irreversible kinase inhibitor with IC₅₀s of 6.95 μM, 2.45 μM, 1.39 μM for ABL1 wt, KIT wt, PDGFRR wt .

HY-10186

TG 100801 1 Publications Verification	VEGFR FGFR PDGFR Src	Cancer
TG 100801 is a proagent that generates TG 100572 by de-esterification in development to treat age-related macular degeneration. TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC₅₀s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.

HY-15814

HG-7-85-01	Bcr-Abl PDGFR c-Kit Src JAK Apoptosis	Cancer
HG-7-85-01 is a type II ATP competitive inhibitor of wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibits T315I mutant Bcr-Abl kinase, KDR and RET with IC₅₀s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC₅₀>2 μM). HG-7-85-01 inhibits the cell proliferation, which is mediated by the induction of apoptosis, and inhibition of cell-cycle progression .

HY-10501A

SU14813 maleate	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-13223A

Crenolanib benzenesulfonate 15+ Cited Publications CP 868596-26	Autophagy PDGFR FLT3	Cancer
Crenolanib benzenesulfonate is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with K_ds of 0.74 nM and 2.1 nM/3.2 nM, respectively.

HY-10184

TG 100572	Src VEGFR PDGFR FGFR	Cancer
TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC₅₀s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.

HY-13302B

CP-547632 hydrochloride 1 Publications Verification	VEGFR FGFR	Cancer
CP-547632 hydrochloride is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC₅₀s of 11 nM and 9 nM, respectively. CP-547632 hydrochloride is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 hydrochloride has antitumor efficacy .

HY-10981R

Lenvatinib (Standard) E7080 (Standard)	Reference Standards VEGFR FGFR PDGFR c-Kit RET	Cancer
Lenvatinib (Standard) is the analytical standard of Lenvatinib. This product is intended for research and analytical applications. 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-171878

BI-4659	TGF-β Receptor PDGFR TGF-beta/Smad	Inflammation/Immunology Cancer
BI-4659 is a TGFβRI and PDGFRα inhibitor with IC₅₀ values of 19 nM and 99 nM, respectively. BI-4659 inhibits the kinase activities of TGFβRI and PDGFRα, blocks the downstream TGFβRI signaling pathway, and reduces the phosphorylation level of Smad2/3 without altering the expression of TGF-β1. BI-4659 is applicable to research related to pulmonary fibrosis, cancer, and renal ischemia-reperfusion injury .

HY-133980A

O-Demethyl Lenvatinib hydrochloride	Drug Metabolite	Cancer
O-Demethyl Lenvatinib hydrochloride is a metabolite of Lenvatinib (HY-10981). Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET. Lenvatinib shows potent antitumor activities .

Cat. No.	Product Name

HY-L016

Protein Tyrosine Kinase Compound Library

1,578 compounds

Protein tyrosine kinases (PTKs) are key signaling molecules and important drug targets. Two classes of PTKs are present in cells: the transmembrane receptor PTKs (RTKs) and the nonreceptor PTKs. The RTK family includes the receptors for insulin and for many growth factors, such as EGFR, FGFR, PDGFR, VEGFR, and NGFR. RTKs are transmembrane glycoproteins that are activated by the binding of their ligands, and they transduce the extracellular signal to the cytoplasm by phosphorylating tyrosine residues on the receptors themselves (autophosphorylation) and on downstream signaling proteins. Their principal functions of PTKs involve the regulation of multicellular aspects of the organism. Cell to cell signals concerning growth, differentiation, adhesion, motility, and death are frequently transmitted through tyrosine kinases. In humans, tyrosine kinases have been demonstrated to play significant roles in the development of many disease states, including diabetes and cancers.

MCE designs a unique collection of 1,578 compounds that act as a useful tool for PTKs-related drug screening and disease research.

Cat. No.	Product Name	Chemical Structure

HY-10065S

Axitinib-13C,d3
Axitinib- ¹³C,d₃ is a ¹³C-labeled and deuterium labeled Axitinib. Axitinib is a multi-targeted tyrosine kinase inhibitor with IC₅₀ values of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFRβ, respectively .

HY-15463S1

Imatinib-d4
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-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 .

HY-10065S1

Axitinib-d3
Axitinib-d₃ (AG-013736-d₃) is deuterium labeled Axitinib. Axitinib is a multi-targeted tyrosine kinase inhibitor with IC₅₀s of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFRβ, respectively .

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 .

HY-12047S

Ponatinib-d8
Ponatinib-d₈ (AP24534-d₈) is a deuterium labeled Ponatinib. Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.

HY-13342AS

Apatinib-d8 free base

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-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 .

HY-10255AS1

Sunitinib-d4
Sunitinib-d₄ is the deuterium labeled Sunitinib. Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC₅₀s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively . Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .

HY-10255AS

Sunitinib-d10
Sunitinib-d₁₀ (SU 11248-d₁₀) is a deuterium labeled Sunitinib. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor with IC₅₀s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively . Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .

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 .

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 .

HY-10981S2

Lenvatinib-15N,d4
Lenvatinib- ¹⁵N,d₄ is ¹⁵N and deuterated labeled Lenvatinib (HY-10981). 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-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-15463S3

Imatinib-13C,d3

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-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.

Targets Recommended: PDGFR

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-10407G

SU 5402	VEGFR EGFR PDGFR	Cancer
SU 5402 (GMP) is SU 5402 (HY-10407) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. SU 5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC₅₀ of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGFRβ, respectively .

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