- BFH772
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- $38.00 / 2mg
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2025-04-29
- CAS:890128-81-1
- Min. Order:
- Purity: 97.71%
- Supply Ability: 10g
- BFH772
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- $1.00 / 1g
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2019-12-23
- CAS:890128-81-1
- Min. Order: 1g
- Purity: 99.99%
- Supply Ability: 200kg
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| Product Name: | BFH772 | | Synonyms: | BFH772;Bfh-722;CS-2412;BFH-772; BFH 772;1-Naphthalenecarboxamide, 6-[[6-(hydroxymethyl)-4-pyrimidinyl]oxy]-N-[3-(trifluoromethyl)phenyl]-;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;BFH772, 10 mM in DMSO | | CAS: | 890128-81-1 | | MF: | C23H16F3N3O3 | | MW: | 439.39 | | EINECS: | | | Product Categories: | | | Mol File: | 890128-81-1.mol |  |
| | BFH772 Chemical Properties |
| Boiling point | 541.2±50.0 °C(Predicted) | | 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 |
| | BFH772 Usage And Synthesis |
| 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. | | Uses | BFH772 is a potent oral VEGFR2 inhibitor, which is highly effective at targeting VEGFR2 kinase with an IC50 value of 3 nM[1]. | | 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 |
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