Research Area
Product Type
United States ( Change Country )
Apatinib (YN968D1) Chemical Structure
Linifanib (ABT-869)
Linifanib (ABT869) is a structurally novel, potent RTK and VEGF and PDGF receptor families inhibitor for, PDGFR-β, KDR, and CSF-1R, with IC50 of 0.2 nM, 2 nM, 4 nM, and 7 nM, respectively.
Axitinib
Axitinib (AG-013736) is a multiple receptor kinase inhibitor of VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-β and c-KIT with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM, respectively.
BIBF1120 (Vargatef)
BIBF1120 (Vargatef) is a potent VEGF receptor (VEGFR), PDGFR and FGFR kinase inhibitor for VEGFR1, VEGFR2, VEGFR3 with IC50 of 34 nM, 5 nM and 5 nM, respectively.
BIBW2992 (Afatinib)
BIBW2992 (Afatinib, Tomtovok, Tovok) irreversibly inhibits EGFR/HER2 including EGFRwt, EGFR L858R , EGFR L858R/T790M and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM, 14 nM, respectively.
Cediranib (AZD2171)
Cediranib (AZD2171) is a highly potent VEGFR2 inhibitor for VEGF-stimulated proliferation and KDR phosphorylation with IC50 of 0.4 nM and 0.5 nM, respectively.
CI-1033 (Canertinib)
CI-1033 is a potent tyrosine kinase inhibitor of EGFR and erbB2 with IC50 of 1.5 nM and 9.0 nM, respectively.
Erlotinib HCl
Erlotinib HCl also known as Tarceva, CP-358774, OSI-774, NSC-718781 is a HCL salt with IC50 of 2 nM for HER1/EGFR TK.
Gefitinib (Iressa)
Gefitinib (Iressa) also known as ZD-1839 & Iressa is a novel potent EGFR tyrosine kinase & Akt phosphorylations inhibitor with IC50 of 37, 26 and 57 nM.
Lapatinib Ditosylate (Tykerb)
Lapatinib (Tyverb, GW-572016, GW-2016) is a potent purified EGFR and ErbB-2 inhibitor with IC50 of 10.2 and 9.8 nM, respectively.
Motesanib Diphosphate (AMG-706)
Motesanib (AMG-706) is a multiple inhibitor of VEGFR1/2/3(IC50: 2 ηM /3 ηM /6 ηM),PDGFR (84ηM), kit (8ηM), and Ret (59ηM)receptors
Biological Activity
Apatinib (YN968D1) is a small-molecule selective multitargeted tyrosine kinase inhibitor with an IC50 of 2.43 nM for the inhibition of VEGFR2. Apatinib (YN968D1) has potential antiangiogenic and antineoplastic activities. It is an orally bioavailable, small molecule agent which is thought to inhibit angiogenesis in cancer cells; specifically apatinib inhibits VEGF-mediated endothelial cell migration and proliferation thus blocking new blood vessel formation in tumor tissue. Apatinib (YN968D1) once daily is orally bioavailable in patients with solid tumors refractory to standard therapy. Apatinib exhibited quick absorption, with Cmax reached in 3 to 4 hours. The mean half-life, estimated to be approximately 9 hours, was constant over all dose groups. Steady-state conditions were achieved within 6 days of dosing, with no accumulation during 56 days of once daily dosing of apatinib. Compared with sorafenib and sunitinib, apatinib (YN968D1) shows good anti-cancer effects for gastric and colorectal cancer. Apatinib (YN968D1) also mildly inhibits c-Kit and c-SRC tyrosine kinases. [1][2][3]
References on Apatinib (YN968D1)
- [2] BMC Cancer 2010;10:529
- [3] Cancer Res 2010;70:7981-7991
Product Information
| Molecular Weight (WM): | 493.58 |
|---|---|
| Formula: | C25H27N5O4S |
| CAS No.: | 811803-05-1 |
| Synonyms: |
N/A
|
| Dissolve in (25°C): | DMSO ≥99mg/mL |
| Water ≥8mg/mL | |
| Ethanol <1mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
Research Area
Notes:
Related Inhibitors
Recommended Screening Libraries
Chemical Library
A collection of 864 bioactive compounds
Inhibitor Library
A collection of 481 inhibitors
Kinase Inhibitor Library
A collection of 194 kinase inhibitors
Tyrosine Kinase Inhibitor Library
A collection of 85 tyrosine kinase inhibitors.
FDA Approved Drug Library
A collection of 426 FDA approved drugs
Natural Product Library
A collection of 139 natural products
Chemotherapeutic Agent Library
A collection of 40 chemotherapeutic agents
Epigenetics Compound library
A unique collection of 17 small molecule modulators
Stem Cell Compound library
A unique collection of 47 small molecule inhibitors
GPCR Compound library
A unique collection of 63 GPCR small molecules
Recently Viewed Items
Keywords:buy Apatinib (YN968D1) | Apatinib (YN968D1) supplier | purchase Apatinib (YN968D1) | Apatinib (YN968D1) cost | Apatinib (YN968D1) manufacturer | order Apatinib (YN968D1) | Apatinib (YN968D1) distributor