Acrizanib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Acrizanib (LHA510, LHA-510) 是一种新型有效的选择性 VEGFR-2 (KDR) 抑制剂，在基于细胞的测定中 IC50 为 17.4 nM。

Acrizanib (LHA510, LHA-510) is a novel potent, selective VEGFR-2 (KDR) inhibitor with IC50 of 17.4 nM in cell-based assays; exhibits <10% remaining kinase activity against only 13 wildtype kinases, CSF1R, Kit, PDGFRα, PDGFRβ, VEGFR1, VEGFR2, VEGFR3, Fms, DDR1, DDR2, TIE1, and ABL1 in a panel of >400 kinases; demonstrates potency and efficacy in rodent CNV models, limited systemic exposure after topical ocular administration, multiple formulation options, and an acceptable rabbit ocular PK profile.Other Indication Phase 1 Clinical.

Acrizanib is a VEGFR-2 inhibitor, with an IC50 of 17.4 nM for BaF3-KDR. Acrizanib (compound 35) exhibits ≤10% remaining kinase activity against only 13 wild type kinases: CSF1R, Kit, PDGFRα, PDGFRβ, VEGFR1, VEGFR2, VEGFR3, Fms (soluble VEGFR1), DDR1, DDR2, TIE1, and ABL1 (nonphosphorylated).

Rat ocular PK studies with Acrizanib shows a distinctly different profile from that observed with compound 25. While prolonged exposure is once again evident in the PEC, the AUC ratio to the level of Acrizanib in plasma is markedly increased (>21000-fold higher exposure in the PEC than plasma on day 11). Furthermore, unlike 25, Acrizanib also afford much improved retina to plasma AUC exposure ratio after 10 days of dosing (598× for Acrizanib vs 0.8× for 25).

LHA510 | LHA 510

Angiogenesis

VEGFR

VEGFR

Other Indications

Other Disease

1229453-99-9

445.406

C20H18F3N7O2

>98% (HPLC)

10 mM in DMSO

O=C(N1C=CC2=C1C=CC(OC3=NC=NC(CNC)=C3)=C2)NC4=NN(C)C(C(F)(F)F)=C4

5-({6-[(methylamino)methyl]pyrimidin-4-yl}oxy)-N-[1-methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl]-1H-indole-1-carboxamide

(-20℃)

With Ice Pack

≥ 2 years