Comparison between the in vivo and in vitro activities of small-molecule compounds
| Phenotype class in vivo/compound name . | HUVEC proliferation . | HUVEC tube formation . | LEC proliferation . | LEC tube formation . |
|---|---|---|---|---|
| Compounds affecting in vivo blood vessel development only | ||||
| Defective vasculogenesis | ||||
| Nocodazole | − | −− | − | −− |
| Podophyllotoxin | − | −− | − | −− |
| 2-Methoxyestradiol | O | −− | − | − |
| IC 261 | O | − | − | − |
| Tyrphostin AG 494 | O | O | O | − |
| Defective angiogenesis | ||||
| Retinoic acid | + | − | + | − |
| L-162,313 | + | − | O | − |
| Indirubin-3′-oxime | − | − | O | O |
| SU 5416 | O | O | O | − |
| Ectopic angiogenic sprouting | ||||
| GW5074 | O | O | + | − |
| VVN hypoplasia | ||||
| MK-886 | + | − | O | − |
| Compounds affecting in vivo blood and lymph vessel formation | ||||
| Defective blood and lymphangiogenesis | ||||
| Naphthyridine | −− | − | −− | − |
| 7-Cyclo | O | −− | O | −− |
| SP600125 | O | O | O | − |
| VVN hyperplasia and defective lymphangiogenesis | ||||
| 1,3-Diethyl-8-phenylxanthine | O | + | O | O |
| 4-Amino-1,8-naphthalimide | + | O | O | − |
| Genistein | O | − | O | − |
| Compounds affecting in vivo lymph vessel formation only | ||||
| Defective lymphangiogenesis | ||||
| Felodipine | O | − | O | O |
| Sobuzoxane | + | O | + | O |
| Nicardipine hydrochloride | O | O | O | O |
| GW2974 | + | − | + | − |
| SU 4312 | + | O | O | O |
| Compounds with no effect on vascular development in vivo | ||||
| Cyclosporin A | O | O | O | O |
| MRS 1845 | + | O | O | − |
| L-687,384 hydrochloride | + | − | O | − |
| Phenotype class in vivo/compound name . | HUVEC proliferation . | HUVEC tube formation . | LEC proliferation . | LEC tube formation . |
|---|---|---|---|---|
| Compounds affecting in vivo blood vessel development only | ||||
| Defective vasculogenesis | ||||
| Nocodazole | − | −− | − | −− |
| Podophyllotoxin | − | −− | − | −− |
| 2-Methoxyestradiol | O | −− | − | − |
| IC 261 | O | − | − | − |
| Tyrphostin AG 494 | O | O | O | − |
| Defective angiogenesis | ||||
| Retinoic acid | + | − | + | − |
| L-162,313 | + | − | O | − |
| Indirubin-3′-oxime | − | − | O | O |
| SU 5416 | O | O | O | − |
| Ectopic angiogenic sprouting | ||||
| GW5074 | O | O | + | − |
| VVN hypoplasia | ||||
| MK-886 | + | − | O | − |
| Compounds affecting in vivo blood and lymph vessel formation | ||||
| Defective blood and lymphangiogenesis | ||||
| Naphthyridine | −− | − | −− | − |
| 7-Cyclo | O | −− | O | −− |
| SP600125 | O | O | O | − |
| VVN hyperplasia and defective lymphangiogenesis | ||||
| 1,3-Diethyl-8-phenylxanthine | O | + | O | O |
| 4-Amino-1,8-naphthalimide | + | O | O | − |
| Genistein | O | − | O | − |
| Compounds affecting in vivo lymph vessel formation only | ||||
| Defective lymphangiogenesis | ||||
| Felodipine | O | − | O | O |
| Sobuzoxane | + | O | + | O |
| Nicardipine hydrochloride | O | O | O | O |
| GW2974 | + | − | + | − |
| SU 4312 | + | O | O | O |
| Compounds with no effect on vascular development in vivo | ||||
| Cyclosporin A | O | O | O | O |
| MRS 1845 | + | O | O | − |
| L-687,384 hydrochloride | + | − | O | − |
Scoring system for in vitro assays: O indicates inactive or marginal effects (85%-115% of control); −, moderate inhibition (50%-85% of control); −−, strong inhibition (< 50% of control); and +, moderate promotion (> 115%-150% of control).
HUVEC indicates human umbilical vein endothelial cell; LEC, lymphatic endothelial cell; VVN, vitelline vein network; Naphthyridine, 7-chloro-4-hydroxy-2-phenyl-1,8-naphthyridine; and 7-Cyclo, 7-cyclopentyl-5-(4-phenoxy)phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamine.