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FGFR-IN-1

" in MedChemExpress (MCE) Product Catalog:

By Targets:	FGFR (34) Akt (1) Apoptosis (2) Autophagy (2) c-Fms (3) c-Kit (9) c-Met/HGFR (1) Drug Metabolite (2) EGFR (1) FLT3 (4) Isotope-Labeled Compounds (3) PDGFR (15) Raf (1) RET (4) Src (2) VEGFR (18)
By Research Areas:	Cancer (38)

Inhibitors & Agonists

Isotope-Labeled Compounds

Targets Recommended: FGFR AIM2 NEKs

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-145043

FGFR-IN-1

FGFR Cancer

FGFR-IN-1 is a potent FGFR inhibitor with an IC₅₀ of <100 nM for FGFR1, FGFR2, and FGFR3, respectively (patent US20130338134A1, example 219) ^[1].
HY-12965

S49076

1 Publications Verification

FGFR c-Met/HGFR Cancer

S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3 with IC₅₀ values below 20 nM.
HY-160124

Infigratinib-Boc

FGFR Cancer

Infigratinib-Boc is a derivative of Infigratinib containing a Boc (t-Butyloxy carbonyl) group. Infigratinib is an ATP-competitive pan-FGFR inhibitor .

*FGFR-IN-1*	FGFR	Cancer
FGFR-IN-1 is a potent *FGFR* inhibitor with an IC₅₀ of <100 nM for FGFR1, FGFR2, and FGFR3, respectively (patent US20130338134A1, example 219) ^[1].

S49076 1 Publications Verification	FGFR c-Met/HGFR	Cancer
S49076 is a novel, potent inhibitor of MET, AXL/MER, and *FGFR1/2/3* with IC₅₀ values below 20 nM.

Infigratinib-Boc	FGFR	Cancer
Infigratinib-Boc is a derivative of Infigratinib containing a Boc (t-Butyloxy carbonyl) group. Infigratinib is an ATP-competitive pan-FGFR inhibitor .

HY-15813

FIIN-1 FGFR irreversible INhibitor-1	FGFR	Cancer
FIIN-1 is a potent, irreversible, selective *FGFR* inhibitor. FIIN-1 binds to *FGFR1/2/3/4* and *Flt1/4* with K_ds of 2.8/6.9/5.4/120 nM and 32/120 nM respectively. The biochemical IC₅₀s of FIIN-1 are 9.2, 6.2, 11.9, and 189 nM against FGFR1/2/3/4, respectively ^[1].

HY-160013

FGFR-IN-12

FGFR Cancer

FGFR-IN-12 (example 14), a pyrimidinyl aryl urea derivative, is a potent FGFR inhibitor .

FGFR-IN-12	FGFR	Cancer
FGFR-IN-12 (example 14), a pyrimidinyl aryl urea derivative, is a potent *FGFR* inhibitor .

HY-101544

ARQ 069	FGFR	Cancer
ARQ 069, an analog of ARQ 523, inhibits *FGFR* in an enantiospecific manner. ARQ 069 targets the unphosphorylated, inactive forms of FGFR1/FGFR2 kinases (IC₅₀s of 0.84 μM and 1.23 μM, respectively). ARQ 069 inhibits FGFR1/FGFR2 autophosphorylation (IC₅₀s of 2.8 and 1.9 μM, respectively) through a mechanism in a non-ATP competitive dependent manner ^[1].

HY-10981

Lenvatinib 35+ Cited Publications E7080	VEGFR FGFR PDGFR c-Kit RET	Cancer
Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits *VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET*, shows potent antitumor activities ^[1] .

HY-10981A

Lenvatinib mesylate 35+ Cited Publications E7080 mesylate	VEGFR FGFR PDGFR RET c-Kit	Cancer
Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits *VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET*, shows potent antitumor activities ^[1] .

HY-10337

Brivanib 3 Publications Verification BMS-540215	VEGFR Autophagy	Cancer
Brivanib (BMS-540215) is an ATP-competitive inhibitor against VEGFR2 with an IC₅₀ of 25 nM, and has moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β ^[1].

HY-18708

Erdafitinib 15+ Cited Publications JNJ-42756493	FGFR Apoptosis	Cancer
Erdafitinib (JNJ-42756493) is a potent and orally available *FGFR* family inhibitor; inhibits FGFR1/2/3/4 with IC₅₀s of 1.2, 2.5, 3.0 and 5.7 nM, respectively.

HY-147621

FGFR-IN-6	FGFR	Cancer
FGFR-IN-6 (Compound 5) is a *FGFR* inhibitor . FGFR-IN-6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-148778

FGFR3-IN-4

FGFR Cancer

FGFR3-IN-4 is a selective FGFR3 inhibitor, with an IC₅₀ value of less than 50 nM. FGFR3-IN-4 is at least 10 fold more selective for FGFR3 than for FGFR1 ^[1].

FGFR3-IN-4	FGFR	Cancer
FGFR3-IN-4 is a selective *FGFR3* inhibitor, with an IC₅₀ value of less than 50 nM. FGFR3-IN-4 is at least 10 fold more selective for FGFR3 than for FGFR1 ^[1].

HY-10336

Brivanib (alaninate) 3 Publications Verification BMS-582664	VEGFR Autophagy	Cancer
Brivanib alaninate (BMS-582664) is an ATP-competitive inhibitor against VEGFR2 with an IC₅₀ of 25 nM; has moderate potency against VEGFR-1 and FGFR-1, but more than 240-fold against PDGFRβ ^[1].

HY-19981A

Derazantinib Racemate ARQ-087 Racemate	FGFR	Cancer
Derazantinib Racemate (ARQ-087 Racemate) is the racemate of Derazantinib. Derazantinib is an orally bioavailable, ATP competitive tyrosine kinase inhibitor; exhibits potent activity against *FGFR1-3* chondrocytes with IC₅₀s of 4.5, 1.8, and 4.5 nM, respectively.

HY-101466A

E7090 succinate	FGFR	Cancer
E7090 succinate is an orally available, selective and potent inhibitor of **FGFR1, FGFR2 and FGFR3 tyrosine kinase activities, with IC₅₀** values of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/2/3/4, respectively ^[1].

HY-10981S1

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

HY-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[1][2].

HY-101466

E7090	FGFR	Cancer
E7090 is an orally available, potent, and selective *FGFR* inhibitor with IC₅₀s of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for *FGFR1/FGFR2/FGFR3/FGFR4*, respectively ^[1].

HY-133980

O-Demethyl Lenvatinib	Drug Metabolite	Cancer
O-Demethyl Lenvatinib 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, shows potent antitumor activities ^[1] .

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 ^[1] .

HY-101768

PRN1371 1 Publications Verification	FGFR c-Fms	Cancer
PRN1371 is a highly selective and potent *FGFR1-4* and *CSF1R* inhibitor with IC₅₀s of 0.6, 1.3, 4.1, 19.3 and 8.1 nM for FGFR1, FGFR2, FGFR3, FGFR4 and CSF1R, respectively ^[1].

HY-146541

FGFR4-IN-10	FGFR	Cancer
FGFR4-IN-10 (compound 5a) is a potent and selective *FGFR4* inhibitor with an IC₅₀ value of 70.7 nM. FGFR4-IN-10 shows no inhibition against other FGFR family members, i.e. FGFR1, FGFR2 and FGFR3 .

HY-10207

Dovitinib lactate 5+ 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 ^[1].

HY-B0062

Dovitinib lactate hydrate 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 ^[1].

HY-50904

Nintedanib Maximum Cited Publications 43 Publications Verification BIBF 1120	PDGFR VEGFR FGFR	Cancer
Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for *VEGFR1/2/3, FGFR1/2/3* and PDGFRα/β with IC₅₀s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.

HY-100019

Rogaratinib 5 Publications Verification BAY1163877	FGFR	Cancer
Rogaratinib (BAY1163877) is a potent and selective fibroblast growth factor receptor (FGFR) inhibitor. Rogaratinib inhibits FGFRs with IC50s of 11.2 nM (FGFR1), <1 nM (FGFR2), 18.5 nM (FGFR3), 127 nM (VEGFR3/FLT4), 201 nM (FGFR4), respectively ^[1] .

HY-11106

Nintedanib esylate Maximum Cited Publications 43 Publications Verification BIBF 1120 esylate	PDGFR VEGFR FGFR	Cancer
Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor for *VEGFR1/2/3, FGFR1/2/3* and PDGFRα/β with IC₅₀s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.

HY-119367

ODM-203	FGFR VEGFR	Cancer
ODM-203 is an orally active and selective *FGFR/VEGFR* inhibitor with IC₅₀ values of 6, 11, 16, 5, 9, 26 and 35 nM for *FGFR3/1/2* and *VEGFR3/2/1/4*, respectively. ODM-203 has strong anti-tumour activity and activates immune responses in the tumour microenvironment ^[1].

HY-W758126

(R)-Brivanib alaninate-d4	Isotope-Labeled Compounds	Others
(R)-Brivanib alaninate-d₄ is the deuterium-labeled Brivanib (alaninate) (HY-10336). Brivanib alaninate (BMS-582664) is an ATP-competitive inhibitor against VEGFR2 with an IC₅₀ of 25 nM; has moderate potency against VEGFR-1 and FGFR-1, but more than 240-fold against PDGFRβ ^[1].

HY-50904S

Nintedanib-d3 BIBF 1120-d₃	PDGFR VEGFR FGFR	Cancer
Nintedanib-d₃ is the deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.

HY-50904S2

Nintedanib-d8 BIBF 1120-d₈	Isotope-Labeled Compounds PDGFR VEGFR FGFR	Cancer
Nintedanib-d₈ is deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.

HY-158027

B-Raf IN 17	Raf VEGFR FGFR	Cancer
B-Raf IN 17 (Compound 8e) is a potent and orally active type II multi-kinase inhibitor. B-Raf IN 17 exhibits potent cellular-level suppression of BRAF_WT, VEGFR-2, and FGFR-1 in A375 cell line, with IC₅₀ values of 0.02, 0.18 and 1.65 μM, respectively. B-Raf IN 17 can be used for the research of cancer ^[1].

HY-50904S1

Nintedanib-13C,d3 BIBF 1120-¹³C,d₃	Isotope-Labeled Compounds PDGFR VEGFR FGFR	Cancer
Nintedanib- ¹³C,d₃ is the ¹³C- and deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.

HY-50905S

Dovitinib-d8	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[1][2].

HY-100491

H3B-6527	FGFR	Cancer
H3B-6527 is an orally active, highly selective and covalent *FGFR4* inhibitor with an IC₅₀ of <1.2 nM. H3B-6527 has at least 250-fold selectivity over FGFR1-3 with IC₅₀s of 320 nM, 1290 nM and 1060 nM respectively. H3B-6527 has potent anti-cancer activity ^[1].

HY-50905

Dovitinib 5+ 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 ^[1] .

HY-150026

Multi-kinase-IN-2	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 ^[1].

HY-112345

PD-089828	FGFR PDGFR EGFR Src	Cancer
PD-089828 is an ATP competitive inhibitor of *FGFR-1, PDGFR-β* and EGFR (IC₅₀s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC₅₀=0.18 µM). PD-089828 also inhibits MAPK with an IC₅₀ of 7.1 µM. PD-089828 inhibits PDGF-, EGF- and bFGF-mediated tyrosine kinase receptor autophosphorylation in vitro. PD-089828 has a long-lasting cellular activity ^[1].

HY-151903S

FGFR2/3-IN-1	FGFR	Cancer
FGFR2/3-IN-1 is a potent and selective FGFR2 and FGFR3 (FGFR) inhibitor with IC50s of 1 nM and 0.5 nM, respectively. FGFR2/3-IN-1 displays >40-fold selectivity over FGFR1/FGFR4 and other kinome. FGFR2/3-IN-1 also inhibits FGFR3 V555L and V555M mutants with IC50s of 2.7 nM and 6.1 nM, respectively[1].

Cat. No.	Product Name	Chemical Structure

HY-10981S

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

HY-50904S2

Nintedanib-d8
Nintedanib-d₈ is deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, 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[1][2].

HY-W758126

(R)-Brivanib alaninate-d4
(R)-Brivanib alaninate-d₄ is the deuterium-labeled Brivanib (alaninate) (HY-10336). Brivanib alaninate (BMS-582664) is an ATP-competitive inhibitor against VEGFR2 with an IC₅₀ of 25 nM; has moderate potency against VEGFR-1 and FGFR-1, but more than 240-fold against PDGFRβ ^[1].

HY-50904S

Nintedanib-d3
Nintedanib-d₃ is the deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.

HY-50904S1

Nintedanib-13C,d3
Nintedanib- ¹³C,d₃ is the ¹³C- and deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.

HY-50905S

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

HY-151903S

FGFR2/3-IN-1
FGFR2/3-IN-1 is a potent and selective FGFR2 and FGFR3 (FGFR) inhibitor with IC50s of 1 nM and 0.5 nM, respectively. FGFR2/3-IN-1 displays >40-fold selectivity over FGFR1/FGFR4 and other kinome. FGFR2/3-IN-1 also inhibits FGFR3 V555L and V555M mutants with IC50s of 2.7 nM and 6.1 nM, respectively[1].

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