WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H206780
CAS#: 1229453-99-9 (free base)
Description: Acrizanib, also known as LHA510, is a potent and selective angiogenesis inhibitor and VEGFR‑2 Inhibitor Specifically Designed for Topical Ocular Delivery, as a Therapy for Neovascular Age-Related Macular Degeneration.
Hodoodo Cat#: H206780
Name: Acrizanib
CAS#: 1229453-99-9 (free base)
Chemical Formula: C20H18F3N7O2
Exact Mass: 445.15
Molecular Weight: 445.406
Elemental Analysis: C, 53.93; H, 4.07; F, 12.80; N, 22.01; O, 7.18
Related CAS #: 1229453-99-9 (free base) 1637434-72-0 (HCl)
Synonym: Acrizanib; LHA510; LHA 510; LHA-510
IUPAC/Chemical Name: 5-({6-[(methylamino)methyl]pyrimidin-4-yl}oxy)-N-[1-methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl]-1H-indole-1-carboxamide
InChi Key: XPIHPLVWOUDMPF-UHFFFAOYSA-N
InChi Code: InChI=1S/C20H18F3N7O2/c1-24-10-13-8-18(26-11-25-13)32-14-3-4-15-12(7-14)5-6-30(15)19(31)27-17-9-16(20(21,22)23)29(2)28-17/h3-9,11,24H,10H2,1-2H3,(H,27,28,31)
SMILES Code: O=C(N1C=CC2=C1C=CC(OC3=NC=NC(CNC)=C3)=C2)NC4=NN(C)C(C(F)(F)F)=C4
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
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
More Info:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 445.41 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 |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Poor SH, Weissgerber G, Adams CM, Bhatt H, Browning DJ, Chastain J, Ciulla TA, Ferriere M, Gedif K, Glazer LC, Joondeph BC, Normand G, Sheth V, Watters C, Grosskreutz CL. A Randomized, Double-Masked, Multicenter Trial of Topical Acrizanib (LHA510), a Tyrosine Kinase VEGF-Receptor Inhibitor, in Treatment- Experienced Subjects With Neovascular Age-Related Macular Degeneration. Am J Ophthalmol. 2022 Jul;239:180-189. doi: 10.1016/j.ajo.2022.02.019. Epub 2022 Mar 2. PMID: 35247334.
2: Adams CM, Anderson K, Artman G 3rd, Bizec JC, Cepeda R, Elliott J, Fassbender E, Ghosh M, Hanks S, Hardegger LA, Hosagrahara VP, Jaffee B, Jendza K, Ji N, Johnson L, Lee W, Liu D, Liu F, Long D, Ma F, Mainolfi N, Meredith EL, Miranda K, Peng Y, Poor S, Powers J, Qiu Y, Rao C, Shen S, Sivak JM, Solovay C, Tarsa P, Woolfenden A, Zhang C, Zhang Y. The Discovery of N-(1-Methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6- ((methylamino)methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide (Acrizanib), a VEGFR-2 Inhibitor Specifically Designed for Topical Ocular Delivery, as a Therapy for Neovascular Age-Related Macular Degeneration. J Med Chem. 2018 Feb 22;61(4):1622-1635. doi: 10.1021/acs.jmedchem.7b01731. Epub 2018 Feb 5. PMID: 29400470.
3: Zeitz O, Joussen AM. Tropfen statt spritzen? Der Traum von einer Therapie von Makulaerkrankungen mit Augentropfen [Eye Drops Instead of Intravitreal Injections? The Dream of Treating Macular Diseases by Topically Administered Drugs]. Klin Monbl Augenheilkd. 2017 Sep;234(9):1088-1093. German. doi: 10.1055/s-0043-113253. Epub 2017 Aug 11. PMID: 28800660.