BFH772
- CAS No.
- 890128-81-1
- Chemical Name:
- BFH772
- Synonyms
- BFH772;CS-2412;Bfh-722;BFH-772; BFH 772;6-((6-(Hydroxymethyl)pyrimidin-4-yl)oxy)-N-(3-(trifluoromethyl)phenyl)-1-naphthamide;inhibit,BFH 772,VEGFR,BFH-772,BFH772,Vascular endothelial growth factor receptor,Inhibitor;1-Naphthalenecarboxamide, 6-[[6-(hydroxymethyl)-4-pyrimidinyl]oxy]-N-[3-(trifluoromethyl)phenyl]-
- CBNumber:
- CB03147777
- Molecular Formula:
- C23H16F3N3O3
- Molecular Weight:
- 439.39
- MDL Number:
- MFCD30534392
- MOL File:
- 890128-81-1.mol
Boiling point | 541.2±50.0 °C(Predicted) |
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Density | 1.432±0.06 g/cm3(Predicted) |
storage temp. | Store at -20°C |
solubility | Soluble in DMSO |
form | A crystalline solid |
pka | 12.65±0.70(Predicted) |
color | White to off-white |
FDA UNII | T1IV236CVP |
SAFETY
Risk and Safety Statements
Symbol(GHS) | GHS07 |
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Signal word | Warning | |||||||||
Hazard statements | H302-H315-H319-H335 | |||||||||
Precautionary statements | P261-P305+P351+P338 | |||||||||
NFPA 704 |
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BFH772 price More Price(30)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Cayman Chemical | 21386 | BFH-772 | 890128-81-1 | 1mg | $38 | 2024-03-01 | Buy |
Cayman Chemical | 21386 | BFH-772 | 890128-81-1 | 5mg | $166 | 2024-03-01 | Buy |
Cayman Chemical | 21386 | BFH-772 | 890128-81-1 | 10mg | $292 | 2024-03-01 | Buy |
Cayman Chemical | 21386 | BFH-772 | 890128-81-1 | 25mg | $593 | 2024-03-01 | Buy |
ApexBio Technology | B6199 | BFH772 | 890128-81-1 | 50mg | $709 | 2021-12-16 | Buy |
BFH772 Chemical Properties,Uses,Production
Description
BFH772 is an inhibitor of VEGF receptor 2 (VEGFR2; IC50 = 0.0027 μM for the human receptor). It is selective for human VEGFR2 over mouse VEGFR2 and human VEGFR1 and VEGFR3 (IC50s = 1.5, 1.7, and 1.1 μM, respectively), as well as 40-fold selective over B-RAF, RET, and Tie2. BFH772 inhibits VEGF-induced proliferation of human umbilical vein endothelial cells (HUVECs; IC50 = <0.01 nM). It inhibits VEGF-induced increases in tissue weight and Tie2 levels in an angiogenesis chamber implant model in mice when administered at doses of 1 and 3 mg/kg per day. BFH772 (3 mg/kg per day) inhibits primary tumor and metastasis growth in a B16 melanoma mouse model.
in vitro
bfh772 was highly effective at targeting vegfr2 kinase, however, lost 500-fold potency on flk-1, flt-1, and flt-4. bfh772 also targeted b-raf, ret, and tie-2, albeit with at least 40-fold lower potency. bfh772 inhibited the ligand induced autophosphorylation of ret, pdgfr, and kit kinases. bfh772 was selective against the kinases of egfr, erbb2, ins-r, and igf-1r and against the cytoplasmic bcr-abl kinase [1].
in vivo
the dose response curves of bfh772 at 0.3, 1, and 3 mg/kg showed that even at the lowest concentrations, this naphthalene-1-carboxamide inhibited vegf induced tissue weight and tie-2 levels but only reached statistical significance at 1 mg/kg and above. moreover, bfh772 at 3 mg/kg orally dosed once per day could potently inhibit melanoma growth (54-90% for primary tumor and 71-96% for metastasis tumor) when compared with control ratios [1].
IC 50
3 nm
References
[1] bold g, et al. a novel potent oral series of vegfr2 inhibitors abrogate tumor growth by inhibiting angiogenesis. j med chem. 2016 jan 14;59(1):132-46.
[2] http://adisinsight. springer.com/trials/700244037
BFH772 Preparation Products And Raw materials
Raw materials
Preparation Products
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32820 | 60 |
career henan chemical co | +86-0371-86658258 +8613203830695 | factory@coreychem.com | China | 29815 | 58 |
SHANGHAI T&W PHARMACEUTICAL CO., LTD. | +86-021-61551413 +8618813727289 | contact@trustwe.com | China | 5738 | 58 |
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32002 | 58 |
Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10473 | 58 |
InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
Hangzhou MolCore BioPharmatech Co.,Ltd. | +86-057181025280; +8617767106207 | sales@molcore.com | China | 49734 | 58 |
TargetMol Chemicals Inc. | support@targetmol.com | United States | 38460 | 58 | |
ShenZhen Trendseen Biological Technology Co.,Ltd. | 13417589054 | trendseenbio@gmail.com | China | 11681 | 58 |
Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 57505 | 58 |