VEGFR. 1

Transcription

1 VEGFR VEGFRs (vascular endothelial growth factor receptors) are tyrosine kinase receptors responsible for binding with VEGF to initiate signal cascades that stimulate angiogenesis among other effects. VEGFRs convey signals to other signal transduction effectors via autophosphorylation of specific residues in its structure. VEGFR subtypes are numbered 1,2,3. The VEGFRs are a family of tyrosine kinase receptors on the surface of different cells depending on family identity. VEGFR-1 is expressed on haematopoietic stem cells, monocytes, and vascular endothelial cells. VEGFR-2 is expressed on vascular endothelial cells and lymphatic endothelial cells, while VEGFR-3 is only expressed on lymphatic endothelial cells. VEGFRs are an important target for pharmaceutical drugs treating cancer. 1

2 VEGFR Inhibitors & Modulators 2,4-Pyrimidinediamine with linker Cat. No.: HY Altiratinib (DCC-2701) Cat. No.: HY-B0791 2,4-Pyrimidinediamine with linker is a patent compound in WO A1, Page 71; multikinase inhibitor and has a -NH2 terminal linker for further synthesis. Altiratinib(DCC-2701) is a novel c-met/tie-2/vegfr inhibitor; effectively reduce tumor burden in vivo and block c-met ptyr(1349)-mediated signaling, cell growth and migration as compared with a HGF antagonist in vitro. Purity: 99.45% Purity: 98.07% Apatinib (YN 968D1; YN968D1; YN-968D1) Cat. No.: HY AST 487 (NVP-AST 487) Cat. No.: HY Apatinib is a selective VEGFR2 inhibitor with IC 50 of 1 nm. YN968D1 also potently suppresses the activities of Ret, c-kit and c-src with IC s of 13, 429 and 530 nm, respectively. YN968D1 has no significant 50 effects on EGFR, Her-2 or FGFR1 in concentrations up to 10 μm. Purity: 99.76% Phase 2, Phase 3 AST 487 is a RET kinase inhibitor with IC 50 of 880 nm, inhibits RET autophosphorylation and activation of downstream effectors, also inhibits Flt-3 with IC 50 of 520 nm. Axitinib (AG ; AG ; AG013736) Cat. No.: HY AZD2932 (AZD-2932; AZD 2932) Cat. No.: HY Axitinib is a receptor kinase inhibitor of VEGFRs and, at higher doses, PDGFRs ( IC 50 =0.1 nm for VEGFR1, 0.2 nm for VEGFR2, nm for VEGFR3, and 1.6 nm for PDGFRβ). AZD2932 is a new series of quinazoline ether inhibitor which potently inhibits VEGFR-2 and PDGFR with IC50s of 4 nm/8 nm/ 7 nm for PDGFRβ/VEGFR-2/Flt-3. Purity: 99.77% Phase 3 Size: Purity: 98.12% BFH772 (BFH-772; BFH 772) Cat. No.: HY BIBF 1120 (Nintedanib; BIBF1120; BIBF-1120) Cat. No.: HY BIBF 1120 is a potent triple angiokinase inhibitor for BFH772 is a potent oral VEGFR2 inhibitor, which is highly effective at VEGFR1/2/3, targeting VEGFR2 kinase with an IC 50 value of 3 nm. FGFR1/2/3 and PDGFRα/β with IC 50 s of 34 nm/13 nm/13 nm, 69 nm/37 nm/108 nm and 59 nm/65 nm, respectively. Purity: 98.03% Phase 2 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Purity: 99.72% Phase 3, 200 mg, 500 mg, 1 g BIBF 1120 (esylate) (Nintedanib esylate; BIBF-1120 esylate) Cat. No.: HY BIBF 1202 (BIBF1202; BIBF-1202) Cat. No.: HY Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nm/13 nm/13 nm, 69 nm/37 nm/108 nm and 59 nm/65 nm. BIBF 1202 is the carboxylate metabolite of BIBF 1120, which is an oral triple angiokinase inhibitor targeting VEGFR, PDGFR, FGFR. Purity: 99.95% Phase 3, 200 mg, 500 mg Purity: 99.37% 1 mg, 5 mg 2 Tel: Fax: sales@medchemexpress.com

3 BMS (BMS690514; BMS ) Cat. No.: HY BMS Cat. No.: HY BMS is a potent and selective inhibitor of epidermal growth factor receptor (EGFR), HER2, and HER4, as well as the VEGF receptor kinases. BMS is a potent ATP competitive inhibitor of Met/VEGFR2 with IC50 of 1.7/15 nm; also inhibits Ron, Axl and Flt3 with IC50 of <3 nm; a prodrug of BMS mg, Purity: 99.87% Phase 1 Brivanib (BMS ; BMS540215; BMS ) Cat. No.: HY Brivanib (alaninate) (BMS ; BMS ; BMS582664) Cat. No.: HY Brivanib is an ATP-competitive inhibitor against VEGFR2 with IC 50 of 25 nm, abd has moderate potency against VEGFR-1 and FGFR-1, but > 240-fold against PDGFR-β. Brivanib alaninate(bms582664) is an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nm, moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β Purity: 98.34% Purity: >98.0% Phase 3 c-met inhibitor 2 (3(4H)-Pyridinecarboxamide, N-[4-[(2-am ino-3-chloro-4-pyridinyl)oxy]-3-fluorophenyl]-5- ) Cat. No.: HY-18711A Cabozantinib (XL184; BMS ; XL-184; XL184) Cat. No.: HY c-met inhibitor 2 is a potent compound that has activity against cancers dependent upon Met activation and also has activity against cancers as a VEGFR inhibitor. Cabozantinib is a potent multiple RTKs inhibitor that inhibits VEGFR2,,, and with of 0.035, 1.3, 4.6, 7 and 11.3 nm, c-met Kit Axl Flt3 IC 50 respectively. Purity: 99.95% Purity: 99.89% Phase 3, Phase 4, 200 mg Cabozantinib (S-malate) (XL184; XL-184; Cabozantinib; XL 184) Cat. No.: HY Cediranib (AZD2171; AZD 2171; AZD-2171) Cat. No.: HY Cabozantinib (S-malate) is a potent VEGFR2 inhibitor with IC 50 of nm, and also inhibits c-met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC 50 s of 1.3 nm, 4 nm, 4.6 nm, 12 nm/11.3 nm/6 nm, 14.3 nm and 7 nm, respectively. Purity: 99.83% Phase 2, 200 mg Cediranib is a highly potent VEGFR(KDR) inhibitor with IC 50 of <1 nm, and also inhibits Flt1/4 with IC 50 of 5 nm/ 3 nm, with similar activity against c-kit and PDGFRβ, 36-, 110-fold and is >1000-fold selective more for VEGFR than PDGFR-α, CSF-1R and Flt3. Purity: 99.48% Phase 3, 200 mg Cediranib (maleate) (AZD-2171 maleate) Cat. No.: HY E-3810 (E 3810; E3810; Lucitanib) Cat. No.: HY Cediranib (AZD2171) maleate is a highly potent VEGFR(KDR) inhibitor with IC50 of <1 nm, also inhibits Flt1/4 with IC50 of 5 nm/ 3 nm, similar activity against c-kit and PDGFRβ, 36-, 110-fold and >1000-fold selective more for VEGFR than PDGFR-α, CSF-1R and Flt3 E-3810 is a novel dual inhibitor of the VEGF and FGF receptors, potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC 50 of 7 nm, 25 nm, 10 nm, 17.5 nm, and 82.5 nm, respectively. Purity: 99.31% Phase 2, Phase 3 Purity: 98.24% Phase 1, Phase 2 2 mg, 3

4 E-7050 (E 7050; E7050) Cat. No.: HY EG00229 (EG 00229; EG-00229) Cat. No.: HY E7050(Golvatinib) is a dual c-met and VEGFR-2 inhibitor with IC50 of 14 nm and 16 nm. EG00229 is the first small molecule inhibitors of the neuropilin-1 and VEGF-A interaction with an IC50 of inhibition of 8 um(125i-vegf binding to PAE/NRP1 cells). Phase 1, Phase 2 Purity: 98.08% ENMD-2076 (ENMD 2076; ENMD2076) Cat. No.: HY-10987A ENMD-2076 (Tartrate) (ENMD 2076; ENMD2076) Cat. No.: HY ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nm and 1.86 nm, 25-fold selective for Aurora A than over Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα. ENMD-2076 tartrate has selective activity against Aurora A and Flt3 with IC50 of 14 nm and 1.86 nm, 25-fold selective for Aurora A than over Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα. Purity: 98.77% Phase 1, Phase 2 Foretinib (XL880; GSK ; GSK089; EXEL-2880) Cat. No.: HY Fruquintinib (HMPL-013; HMPL013; HMPL 013) Cat. No.: HY Foretinib is an ATP-competitive inhibitor of HGFR and VEGFR, with IC 50 of 0.4 nm and 0.9 nm for Met and KDR, less potent against Ron, Flt-1/3/4, Kit, PDGFRα/β and Tie-2, and has little activity to FGFR1 and EGFR. Purity: 99.81% Phase 2 Fruquintinib (HMPL-013) inhibits VEGFR family member (VEGFR1, 2, 3) with IC50s of 33 nm, 35 nm and 0.5 nm, respectively with weak inhibition of RET, FGFR-1 and c-kit kinases. Purity: 99.93% Phase 2 JI-101 (JI 101; JI101) Cat. No.: HY Ki8751 (Ki 8751; Ki-8751) Cat. No.: HY JI-101 is an oral multi-kinase inhibitor that targets vascular endothelial growth factor receptor type 2 (VEGFR-2), platelet derived growth factor receptor β (PDGFR-β), and ephrin type-b receptor 4 (EphB4). JI-101 inhibits angiogenesis, and subsequently tumor growth. [1] Purity: 99.78% Ki8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nm, >40-fold selective for VEGFR2 than c-kit, PDGFRα and FGFR-2, little activity to EGFR, HGFR and InsR. Purity: 99.62% KRN-633 (KRN 633; KRN633) Cat. No.: HY Lenvatinib (E7080; E-7080; E 7080) Cat. No.: HY KRN-633 is a cell-permeable, reversible, ATP-competitive VEGFR kinase inhibitor with IC50 of 170 nm, 160 nm, and 125 nm for VEGFR-1, VEGFR-2, VEGFR-3, respectively Lenvatinib is an orally active, multi-target inhibitor, mostly for VEGFR2(KDR) / VEGFR3(Flt-4) with IC 50 of 4 nm/5.2 nm, and less potent against VEGFR1/Flt-1, and appr 10-fold more selective for VEGFR2/3 against FGFR1, PDGFRα/β. Purity: 98.2% Purity: 99.69% Phase 2, Phase 3, 200 mg, 500 mg 4 Tel: Fax: sales@medchemexpress.com

5 Linifanib (ABT-869; AL-39324; ABT 86 9; ABT869; AL 39324; AL39324) Cat. No.: HY MGCD-265 analog (MGCD 265 analog; MGCD265 analog) Cat. No.: HY Linifanib (ABT-869; AL-39324) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR, CSF-1R, Flt-1/3 and PDGFRβ with IC50 of 4 nm, 3 nm, 3 nm/4 nm and 66 nm respectively MGCD-265-analog (structurally related to MGCD-265) is an orally bioavailable multitargeted tyrosine kinase inhibitor with potential antineoplastic activity with IC50 of 29 nm and 10 nm for c-met and VEGFR2, respectively Purity: 99.8%, 200 mg, 500 mg Motesanib (AMG 706; AMG-706) Cat. No.: HY Motesanib (Diphosphate) (AMG-706; Motesanib; AMG706; AMG 706) Cat. No.: HY Motesanib is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC 50 s of 2 nm/3 nm/6 nm, respectively, and has similar activity against Kit, and is appr 10-fold more selective for VEGFR than PDGFR and Ret. Motesanib diphosphate (AMG-706) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 2 nm/3 nm/6 nm, respectively; similar activity against Kit, ~10-fold more selective for VEGFR than PDGFR and Ret. Purity: 99.93% Phase 2, Phase 3 Purity: 99.54% Phase 2, Phase 3 N-Desethyl Sunitinib (SU11662; SU 11662; SU-11662) Cat. No.: HY NVP-BAW2881 (BAW2881; BAW 2881; BAW-2881) Cat. No.: HY N-Desethyl Sunitinib is a major and pharmacologically active metabolite of sunitinib, which is potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with K i values of 2, 9, 17, 8 and 4 nm for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively. BAW2881 is a potent and selective VEGFR inhibitor (vascular endothelial growth factor receptor tyrosine kinase inhibitor) with activity to inhibit chronic and acute skin inflammation. Purity: 98.32% Purity: 98.05% 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Oglufanide (H-Glu-Trp-OH; L-Glutamyl-L-tryptophan) Cat. No.: HY OSI-930 (OSI 930; OSI930) Cat. No.: HY Oglufanide inhibits vascular endothelial growth factor (VEGF), which may inhibit angiogenesis. OSI-930 is a potent inhibitor of Kit, KDR and CSF-1R with IC50 of 80 nm, 9 nm and 15 nm, respectively; also potent to Flt-1, c-raf and Lck and low activity against PDGFRα/β, Flt-3 and Abl Purity: 98.71% Phase 1 Pazopanib (GW ; GW ; GW786034) Cat. No.: HY Pazopanib (Hydrochloride) (GW786034; GW ; GW ) Cat. No.: HY Pazopanib is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-kit, FGFR1, and c-fms with IC 50 of 10, 30, 47, 84, 74, 140 and 146 nm, respectively. Pazopanib Hcl (GW ) 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, respectively Purity: >98.0% Phase 4, 200 mg, 500 mg Purity: 99.92% Phase 3, Phase 4, 200 mg, 500 mg 5

6 Ponatinib (AP 24534; AP24534; AP-24534) Cat. No.: HY PP121 (PP 121; PP-121) Cat. No.: HY Ponatinib is a potent, orally available multi-targeted kinase inhibitor with IC 50 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. PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mtor, VEGFR2, Src and Abl with IC50 of 2 nm, 8 nm, 10 nm, 12 nm, 14 nm and 18 nm, also inhibits DNA-PK with IC50 of 60 nm. Purity: 99.53% Phase 2, Phase 3 Purity: 99.11% R1530 (R 1530; R-1530) Cat. No.: HY RAF265 (CHIR-265; RAF 265; RAF-265; CHIR265) Cat. No.: HY R1530 is the multikinase inhibitor with potential antiangiogenesis and antineoplastic activities. RAF265 (CHIR-265) is a potent selective inhibitor of C-Raf/B-Raf/B-Raf V600E with IC50 of 3-60 nm, and exhibits potent inhibition on VEGFR2 phosphorylation with EC50 of 30 nm Purity: 98.73% Purity: 99.72% Phase 1, Phase 2 Regorafenib (BAY ; BAY ) Cat. No.: HY Regorafenib (Hydrochloride) (BAY hydrochloride) Cat. No.: HY Regorafenib is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC 50 of 13 nm, 4.2 nm, 46 nm, 22 nm, 7 nm, 1.5 nm and 2.5 nm, respectively. Regorafenib (BAY ) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nm/4 Purity: 99.63% Phase 3, Phase 4, 200 mg Purity: 99.58% Phase 1, Phase 2 Regorafenib (monohydrate) (BAY monohydrate) Cat. No.: HY-10331A SAR (SAR ; SAR ) Cat. No.: HY Regorafenib (BAY ) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nm/4 SAR is a VEGFR3 inhibitor with IC50/Ki of 23 nm/12 nm, about 50- and 10-fold more selective for VEGFR3 than VEGFR1/2, little activity against Akt1, CDKs, PLK1, EGFR, IGF-1R, c-met, Flt2 etc. Purity: 99.96% Phase 3, Phase 4, 200 mg Purity: 99.8% SKLB1002 (SKLB 1002; SKLB-1002) Cat. No.: HY SKLB610 (SKLB 610; SKLB-610) Cat. No.: HY SKLB1002 is a novel and potent VEGFR-2 inhibitor with an IC50 value of 32 nm. SKLB610, a novel multi-targeted inhibitor, inhibits angiogenesis-related tyrosine kinase VEGFR2, FGFR2 and PDGFR at rate of 97%, 65% and 55%, respectively, at concentration of 10 μm in biochemical kinase assays. Purity: 97.94% Purity: 99.47% 6 Tel: Fax: sales@medchemexpress.com

7 Sorafenib (Bay ) Cat. No.: HY Sorafenib (Tosylate) (Bay ) Cat. No.: HY-10201A Sorafenib is a potent multikinase inhibitor with IC 50 s of 6 nm, 20 nm, and 22 nm for Raf-1, B-Raf, and VEGFR-3, respectively. Sorafenib tosylate is a potent multikinase inhibitor, with IC 50 s of 6 nm, 20 nm, and 22 nm for Raf-1, B-Raf, and VEGFR-3, respectively. Purity: 99.84% Phase mg, 500 mg Purity: >98.0% Phase mg, 500 mg SU 5402 (SU-5402; SU5402) Cat. No.: HY SU14813 (SU-14813; SU 14813) Cat. No.: HY SU 5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC 50 of 20 nm, 30 nm, and 510 nm for VEGFR2, FGFR1, and PDGFRβ, respectively. SU14813 is an oral, multitargeted tyrosine kinase inhibitor (TKI) targeting vascular endothelial growth factor receptors (VEGFR), platelet-derived growth factor receptors (PDGFR), Kit, and fms-like tyrosine kinase 3 (FLT-3). Purity: 99.23% Purity: 95.74% SU14813 (maleate) (SU maleate; SU maleate) Cat. No.: HY-10501A SU5416 (Semaxinib; SU-5416; SU 5416) Cat. No.: HY SU14813 maleate is an oral, multitargeted tyrosine kinase inhibitor (TKI) targeting vascular endothelial growth factor receptors (VEGFR), platelet-derived growth factor receptors (PDGFR), Kit, and fms-like tyrosine kinase 3 (FLT-3). SU5416 is a potent and selective inhibitor of the VEGFR ( Flk-1/ KDR) that inhibits tyrosine kinase catalysis, and inhibits autophosphorylation of the Flk-1 receptor with an IC 50 of 1.23±0.2 μm (n=4) using an ELISA-based biochemical kinase assay. Phase 1, Phase 2 Purity: 99.93% Phase 2, Phase 3 Sulfatinib (HMPL-012; HMPL 012; HMPL012) Cat. No.: HY Sunitinib (SU 11248; SU-11248) Cat. No.: HY-10255A Sulfatinib (HMPL-012) may be a potent drug for cancer. It inhibits KDR and FGFR1 enzymatic activity, with IC50 values of and μm, respectively. Also, it is a herg inhibitor with IC 50 of 6.8 μm in CHO cell. Sunitinib is a potent tyrosine kinase inhibitor targeting VEGFR2 and PDGFRβ with IC 50 of 80 nm and 2 nm, respectively. Purity: 98.34% 1 mg, Purity: 99.49% Phase mg, 200 mg, 500 mg Sunitinib (Malate) (SU 11248; Sutent; SU-11248; Sunitinib) Cat. No.: HY TAK-593 (TAK593; TAK 593) Cat. No.: HY Sunitinib Malate is a potent tyrosine kinase inhibitor targeting VEGFR2 and PDGFRβ with IC 50 of 80 nm and 2 nm, respectively. TAK-593 is a potent and selective dual VEGFR/PDGFR inhibitor with IC50s of 3.2/0.95/1.1 nm(vegfr1/2/3) and 4.3/1/13 nm(pdgfrα/pdgfrα V561D/PDGFRβ); with an IC50 >1 μm when tested against more than 200 protein and lipid kinases. Purity: 99.47% Phase 4 Size: Purity: 96.86% 7

8 Tanshinone IIA (Dan Shen ketone) Cat. No.: HY-N0135 Tanshinone IIA sulfonate (sodium) (Sodium Tanshinone IIA sulf onate; Tanshinone IIA sodium sulfonate) Cat. No.: HY-N1370 Tanshinone IIA (Tan IIA) is one of the main fat-soluble compositions in the root of red-rooted salvia. Tanshinone IIA may suppress angiogenesis by targeting the protein kinase domains of VEGF/ VEGFR2. Tanshinone IIA sulfonate (sodium) is a water-soluble derivative of tanshinone IIA, which acts as an inhibitor of store-operated Ca 2+ entry (SOCE), and is used to treat cardiovascular disorders. Phase 3 Size: 10 mg, 25 mg, 50 mg Size: 10 mg, 25 mg Telatinib (Bay ) Cat. No.: HY TG (TG100572; TG ) Cat. No.: HY Telatinib(Bay ) is a potent inhibitor of VEGFR2/3, c-kit and PDGFRα with IC50 of 6 nm/4 nm, 1 nm and 15 nm, respectively. TG is a multi-targeted kinase inhibitor that inhibit select growth factor receptor tyrosine kinases and Src familt kinases with IC50 values of 2/7/2/1/0.5 nm for VEGFR1/VEGFR2/FGFR1/Src/Fyn kianse respectively. Purity: 98.54% Phase 2 Size: TG (Hydrochloride) (TG Hydrochloride; TG Hydrochloride) Cat. No.: HY TG (TG100801; TG ) Cat. No.: HY TG is a multi-targeted kinase inhibitor that inhibit select growth factor receptor tyrosine kinases and Src familt kinases with IC50 values of 2/7/2/1/0.5 nm for VEGFR1/VEGFR2/FGFR1/Src/Fyn kianse respectively. TG is the prodrug of TG , which is a multi-targeted kinase inhibitor, and inhibits select growth factor receptor tyrosine kinases and Src familt kinases with IC values of 2/7/2/1/0.5 nm for 50 VEGFR1/VEGFR2/FGFR1/Src/Fyn kianse, respectively. Purity: 98.07% 1 mg, TG (Hydrochloride) (TG Hydrochloride; TG Hydrochloride) Cat. No.: HY Tivozanib (AV-951; AV951; AV 951) Cat. No.: HY TG is the prodrug of TG (HY-10184), TG is a multi-targeted kinase inhibitor that inhibit select growth factor receptor tyrosine kinases and Src familt kinases with IC50 values of 2/7/2/1/0.5 nm or VEGFR1/VEGFR2/FGFR1/Src/Fyn kianse respectively. Size: Tivozanib (AV-951) is a potent and selective VEGFR inhibitor for VEGFR1/2/3 with IC50 of 30 nm/6 Purity: 99.46% Phase 2, Phase 3 Toceranib (SU 11654; PHA ; SU11654; SU-11654; PHA ; PHA291639) Cat. No.: HY Toceranib (phosphate) (SU 11654; PHA ; SU11654; SU ; PHA ; PHA291639) Cat. No.: HY-10330A Toceranib(SU 11654; PHA ) is a kinase inhibitor with both antitumor and antiangiogenic activity through inhibition of KIT, vascular endothelial growth factor receptor 2, and PDGFRβ. Toceranib phosphate (SU 11654; PHA ) is a kinase inhibitor with both antitumor and antiangiogenic activity through inhibition of KIT, vascular endothelial growth factor receptor 2, and PDGFRβ. Purity: 99.34% 8 Tel: Fax: sales@medchemexpress.com

9 Tyrphostin A9 (AG 17; Tyrphostin 9; Malonoben) Cat. No.: HY Vandetanib (ZD6474; ZD-6474; ZD 6474) Cat. No.: HY Tyrphostin A9(AG 17), a tyrosine kinase 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. Vandetanib is a potent inhibitor of VEGFR2 with IC 50 of 40 nm. Purity: >98.0% 50 mg Purity: 99.89% Phase 3, Phase 4 25 mg, 50 mg, 100 mg, 500 mg Vandetanib (hydrochloride) (ZD6474 hydrochloride; ZD hydrochloride; ZD 6474 hydrochloride) Cat. No.: HY-10260B Vandetanib (ZD6474) is a potent inhibitor of VEGFR2 with IC50 of 40 nm Vandetanib (trifluoroacetate) (ZD6474 trifluoroacetate; Z D-6474 trifluoroacetate; ZD 6474 trifluoroacetate) Cat. No.: HY-10260A Vandetanib (ZD6474) is a potent inhibitor of VEGFR2 with IC50 of 40 nm Phase 2, Phase 3 Size: 25 mg, 100 mg, 200 mg Phase 2, Phase 3 Size: 25 mg, 100 mg, 200 mg Vatalanib (PTK787; PTK/ZK; CGP-79787D; CGP-79787; ZK ) Cat. No.: HY Vatalanib (free base) (PTK787 free base; PTK/ZK free base; CG P free base; ZK free base) Cat. No.: HY Vatalanib (PTK787; ZK ; CGP-79787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nm, less potent against VEGFR1/Flt-1, 18-fold against VEGFR3/Flt-4. Vatalanib free base (PTK787 free base) is an inhibitor of VEGFR2/KDR with IC50 of 37 nm, less potent against VEGFR1/Flt-1, 18-fold against VEGFR3/Flt-4. Purity: 99.86% Phase 2, Phase 3 Size: WHI-P154 (WHI-P 154) Cat. No.: HY XL-647 (Tesevatinib; EXEL-7647; KD-019) Cat. No.: HY WHI-P154 is a potent JAK3 inhibitor with IC50 of 1.8 μm, no activity against JAK1 or JAK2, also inhibits EGFR, Src, Abl, VEGFR and MAPK, prevents Stat3, but not Stat5 phosphorylation. XL647 is an orally bioavailable small-molecule receptor tyrosine kinase inhibitor with potential antineoplastic activity; inhibits EGFR, HER2, VEGFR and EphB4 kinase. Purity: 98.6% Purity: 99.21% Phase 1, Phase 2 ZM (CB ; ZM ; ZM ; CB ; CB676475) Cat. No.: HY ZM (ZM ; ZM ) Cat. No.: HY ZM (CB ) is a VEGFR inhibitor that inhibits Flk-1 (KDR) (IC50=100 nm) and Flt (IC50 =2 μm); displays 4-fold selectivity over FGFR-1; inhibitor of c-abl, Flt-1 and Src. ZZM is a potent and selective VEGFR2 inhibitor with IC50 of <2 nm, almost no activity on VEGFR1, PDGFRβ, FGFR1, EGFR and ErbB2. Purity: 99.8% Size: 9

10 ZM (hydrochloride) (ZM hydrochloride; ZM hydrochloride) Cat. No.: HY-15467A ZZZM Hcl is a potent and selective VEGFR2 inhibitor with IC50 of <2 nm, almost no activity on VEGFR1, PDGFRβ, FGFR1, EGFR and ErbB2. Purity: 99.53% 10 Tel: Fax: sales@medchemexpress.com