Acrizanib

Product Name: Acrizanib
CAS No.: 1229453-99-9
Chemical Name: Acrizanib
Synonyms: LHA510;LHA 510;Acrizanib;LHA510;LHA 510;Acrizanib (LHA-510);Acrizanib, 10 mM in DMSO;5-[6-(methylaminomethyl)pyrimidin-4-yl]oxy-N-[1-methyl-5-(trifluoromethyl)pyrazol-3-yl]indole-1-carboxamide;N-(1-methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6-((methylamino)methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide;1H-Indole-1-carboxamide, 5-[[6-[(methylamino)methyl]-4-pyrimidinyl]oxy]-N-[1-methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl]-
CBNumber: CB04667490
Molecular Formula: C20H18F3N7O2
Formula Weight: 445.4
MOL File: 1229453-99-9.mol

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Acrizanib Property

Density: 1.47±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMSO : 41.67 mg/mL (93.56 mM)
form: Solid
pka: 10.53±0.46(Predicted)
color: Light yellow to yellow

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Safety

HS Code: 2933998090

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

ChemScene

Product number: CS-0030518
Product name: Acrizanib
Purity: 99.84%
Packaging: 5mg
Price: $550
Updated: 2021/12/16

ChemScene

Product number: CS-0030518
Product name: Acrizanib
Purity: 99.84%
Packaging: 10mg
Price: $850
Updated: 2021/12/16

Biorbyt Ltd

Product number: orb573147
Product name: Acrizanib
Purity: >98%
Packaging: 100mg
Price: $1431.4
Updated: 2021/12/16

Biorbyt Ltd

Product number: orb573147
Product name: Acrizanib
Purity: >98%
Packaging: 250mg
Price: $2541.5
Updated: 2021/12/16

ChemScene

Product number: CS-0030518
Product name: Acrizanib
Purity: 99.84%
Packaging: 50mg
Price: $2650
Updated: 2021/12/16

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Acrizanib Chemical Properties,Usage,Production

Uses

Acrizanib (LHA510) is a VEGFR-2 inhibitor, with an IC50 of 17.4 nM for BaF3-VEGFR-2[1].

in vivo

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)^[1].

IC 50

VEGFR-2: 17.4 nM (IC₅₀)

References

[1] Adams CM, et al. 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

Acrizanib Preparation Products And Raw materials

Raw materials

Preparation Products

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Acrizanib Suppliers

China 24 United States 3 Global 27

Hangzhou J&H Chemical Co., Ltd.

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1229453-99-9, AcrizanibRelated Search:

LHA 510

LHA510

LHA510;LHA 510

Acrizanib

1H-Indole-1-carboxamide, 5-[[6-[(methylamino)methyl]-4-pyrimidinyl]oxy]-N-[1-methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl]-

Acrizanib (LHA-510)

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

Acrizanib, 10 mM in DMSO

5-[6-(methylaminomethyl)pyrimidin-4-yl]oxy-N-[1-methyl-5-(trifluoromethyl)pyrazol-3-yl]indole-1-carboxamide

1229453-99-9

C20H18F3N7O2