WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406288
Description: KRN633 is a potent and selective VEGFR inhibitor. which inhibits tyrosine phosphorylation of VEGFR-2 (IC50 = 1.16 nmol/L) in human umbilical vein endothelial cells. Selectivity profiling with recombinant tyrosine kinases showed that KRN633 is highly selective for VEGFR-1, -2, and -3. KRN633 inhibits tumor growth in several in vivo tumor xenograft models with diverse tissue origins, including lung, colon, and prostate, in athymic mice and rats. KRN633 also causes the regression of some well-established tumors and those that had regrown after the cessation of treatment. KRN633 was well tolerated and had no significant effects on body weight or the general health of the animals. KRN633 might be useful in the treatment of solid tumors and other diseases that depend on pathologic angiogenesis. ( Mol Cancer Ther. 2004 Dec;3(12):1639-49 )
MedKoo Cat#: 406288
Chemical Formula: C20H21ClN4O4
Exact Mass: 416.12513
Molecular Weight: 416.86
Elemental Analysis: C, 57.62; H, 5.08; Cl, 8.50; N, 13.44; O, 15.35
Synonym: KRN633; KRN-633; KRN 633.
IUPAC/Chemical Name: 1-(2-chloro-4-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-propylurea
InChi Key: VPBYZLCHOKSGRX-UHFFFAOYSA-N
InChi Code: InChI=1S/C20H21ClN4O4/c1-4-7-22-20(26)25-15-6-5-12(8-14(15)21)29-19-13-9-17(27-2)18(28-3)10-16(13)23-11-24-19/h5-6,8-11H,4,7H2,1-3H3,(H2,22,25,26)
SMILES Code: O=C(NCCC)NC1=CC=C(OC2=C3C=C(OC)C(OC)=CC3=NC=N2)C=C1Cl
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 416.86 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Asano D, Nakahara T, Mori A, Sakamoto K, Ishii K. Regression of retinal capillaries following N-methyl-D-aspartate-induced neurotoxicity in the neonatal rat retina. J Neurosci Res. 2014 Oct 3. doi: 10.1002/jnr.23492. [Epub ahead of print] PubMed PMID: 25284371.
2: Morita A, Nakahara T, Abe N, Kurauchi Y, Mori A, Sakamoto K, Nagamitsu T, Ishii K. Treatment of mid-pregnant mice with KRN633, an inhibitor of vascular endothelial growth factor receptor tyrosine kinase, induces abnormal retinal vascular patterning in their newborn pups. Birth Defects Res B Dev Reprod Toxicol. 2014 Aug;101(4):293-9. doi: 10.1002/bdrb.21112. Epub 2014 May 15. PubMed PMID: 24831925.
3: Morita A, Nakahara T, Abe N, Kurauchi Y, Mori A, Sakamoto K, Nagamitsu T, Ishii K. Effects of pre- and post-natal treatment with KRN633, an inhibitor of vascular endothelial growth factor receptor tyrosine kinase, on retinal vascular development and patterning in mice. Exp Eye Res. 2014 Mar;120:127-37. doi: 10.1016/j.exer.2014.01.009. Epub 2014 Jan 23. PubMed PMID: 24462631.
4: Abe N, Nakahara T, Morita A, Wada Y, Mori A, Sakamoto K, Nagamitsu T, Ishii K. KRN633, an inhibitor of vascular endothelial growth factor receptor tyrosine kinase, induces intrauterine growth restriction in mice. Birth Defects Res B Dev Reprod Toxicol. 2013 Aug;98(4):297-303. doi: 10.1002/bdrb.21064. Epub 2013 Jun 18. PubMed PMID: 23780833.
5: Wada Y, Ozaki H, Abe N, Mori A, Sakamoto K, Nagamitsu T, Nakahara T, Ishii K. Role of vascular endothelial growth factor in maintenance of pregnancy in mice. Endocrinology. 2013 Feb;154(2):900-10. doi: 10.1210/en.2012-1967. Epub 2013 Jan 10. PubMed PMID: 23307787.
6: Sassoli C, Pini A, Chellini F, Mazzanti B, Nistri S, Nosi D, Saccardi R, Quercioli F, Zecchi-Orlandini S, Formigli L. Bone marrow mesenchymal stromal cells stimulate skeletal myoblast proliferation through the paracrine release of VEGF. PLoS One. 2012;7(7):e37512. doi: 10.1371/journal.pone.0037512. Epub 2012 Jul 16. PubMed PMID: 22815682; PubMed Central PMCID: PMC3398011.
7: Loganathan S, Kanteti R, Siddiqui SS, El-Hashani E, Tretiakova M, Vigneswaran H, Cervantes G, Natarajan V, Husain AN, Vokes EE, Kindler HL, Salgia R. Role of protein kinase C β and vascular endothelial growth factor receptor in malignant pleural mesothelioma: Therapeutic implications and the usefulness of Caenorhabditis elegans model organism. J Carcinog. 2011 Mar 3;10:4. doi: 10.4103/1477-3163.77274. PubMed PMID: 21383961; PubMed Central PMCID: PMC3049271.
8: Hah YS, Jun JS, Lee SG, Park BW, Kim DR, Kim UK, Kim JR, Byun JH. Vascular endothelial growth factor stimulates osteoblastic differentiation of cultured human periosteal-derived cells expressing vascular endothelial growth factor receptors. Mol Biol Rep. 2011 Feb;38(2):1443-50. doi: 10.1007/s11033-010-0249-1. Epub 2010 Sep 15. PubMed PMID: 20842453.
9: Ban HS, Uno M, Nakamura H. Suppression of hypoxia-induced HIF-1alpha accumulation by VEGFR inhibitors: Different profiles of AAL993 versus SU5416 and KRN633. Cancer Lett. 2010 Oct 1;296(1):17-26. doi: 10.1016/j.canlet.2010.03.010. Epub 2010 Apr 7. PubMed PMID: 20378243.
10: Wada Y, Ozaki H, Abe N, Nagamitsu T, Ohta H, Nakahara T, Ishii K. Effects of KRN633, an inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase, on vascular development of placenta and fetus of mid-pregnancy in mice. J Pharmacol Sci. 2010;112(3):290-8. Epub 2010 Mar 2. PubMed PMID: 20197639.
11: Lee MJ, Song HY, Kim MR, Sung SM, Jung JS, Kim JH. Oncostatin M stimulates expression of stromal-derived factor-1 in human mesenchymal stem cells. Int J Biochem Cell Biol. 2007;39(3):650-9. Epub 2006 Nov 23. PubMed PMID: 17169599.
12: Matsunaga N, Nakamura K, Yamamoto A, Taguchi E, Tsunoda H, Takahashi K. Improvement by solid dispersion of the bioavailability of KRN633, a selective inhibitor of VEGF receptor-2 tyrosine kinase, and identification of its potential therapeutic window. Mol Cancer Ther. 2006 Jan;5(1):80-8. PubMed PMID: 16432165.
13: Nakamura K, Yamamoto A, Kamishohara M, Takahashi K, Taguchi E, Miura T, Kubo K, Shibuya M, Isoe T. KRN633: A selective inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase that suppresses tumor angiogenesis and growth. Mol Cancer Ther. 2004 Dec;3(12):1639-49. PubMed PMID: 15634658.