AAL-993
- CAS No.
- 269390-77-4
- Chemical Name:
- AAL-993
- Synonyms
- CS-2315;AAL-993;2-(Pyridin-4-ylmethylamino)-N-[3-(trifluoromethyl)phenyl]benzamide;2-[(4-Pyridinylmethyl)amino]-N-[3-(trifluoromethyl)phenyl]benzami de;Benzamide, 2-[(4-pyridinylmethyl)amino]-N-[3-(trifluoromethyl)phenyl]-;VEGFR Tyrosine Kinase Inhibitor VI, AAL-993 - CAS 269390-77-4 - Calbiochem;antiangiogenic,antitumor properties,AAL 993,VEGFR1,VEGFR2,orally active,VEGFR,AAL993,VEGFR3,Inhibitor,VEGFR inhibitor,AAL-993,Vascular endothelial growth factor receptor,inhibit
- CBNumber:
- CB13070432
- Molecular Formula:
- C20H16F3N3O
- Molecular Weight:
- 371.36
- MDL Number:
- MFCD18251410
- MOL File:
- 269390-77-4.mol
- MSDS File:
- SDS
Melting point | 158-160 °C |
---|---|
Boiling point | 441.3±45.0 °C(Predicted) |
Density | 1.349±0.06 g/cm3(Predicted) |
storage temp. | +2C to +8C |
solubility | Soluble in DMSO (up to 25 mg/ml) or in Ethanol (up to 15 mg/ml). |
form | Off-white powder |
pka | 12.95±0.70(Predicted) |
color | Pale yellow |
Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. |
AAL-993 price More Price(9)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Sigma-Aldrich | 676504 | VEGFR Tyrosine Kinase Inhibitor VI, AAL-993 - CAS 269390-77-4 - Calbiochem | 269390-77-4 | 10mg | $201 | 2024-03-01 | Buy |
Cayman Chemical | 16351 | AAL-993 ≥95% | 269390-77-4 | 1mg | $73 | 2024-03-01 | Buy |
Cayman Chemical | 16351 | AAL-993 ≥95% | 269390-77-4 | 5mg | $128 | 2024-03-01 | Buy |
TRC | A104490 | AAL-993 | 269390-77-4 | 100mg | $1450 | 2021-12-16 | Buy |
ApexBio Technology | C3730 | AAL-993 | 269390-77-4 | 5mg | $143 | 2021-12-16 | Buy |
AAL-993 Chemical Properties,Uses,Production
Description
AAL-993 (269390-77-4) inhibits VEGFR-1 (IC50 = 130 nM), VEGFR-2 (IC50 = 23 nM), and VEGFR-3 (IC50 = 18 nM). PDGFR-β, cKit, and CSF-1R are also inhibited at higher concentrations (IC50‘s 640 nM, 236 nM and 380 nM respectively). Screening studies have shown no inhibitory activity against a range of other kinases. X-Ray crystallography has shown that AAL-993 binds to the catalytic domain of VEGFR-2 when the protein is in an inactive conformation. Cell permeable, active in vivo and in whole animal studies.
Uses
AAL-993 is a VEGFR tyrosine kinase inhibitor that possess dual inhibition of VEGFR signaling and HIF-1α expression through ERK inhibition without affecting Akt phosphorylation.
General Description
A cell-permeable anthranilamide that acts as a potent VEGFR inhibitor (IC50 = 130, 23, and 18 nM against VEGFR-1, -2, and -3, respectively; IC50 = 1.24 nM against VEGF-induced human VEGFR-2 phosphorylation in CHO cells) by targeting the ATP-binding site of VEGFR in its inactive "DFG-out" conformation and effectively suppresses tumor growths (50 to 100 mg/kg; p.o.) via its anti-angiogenesis activity in mice and rats in vivo, while inhibiting c-kit, CSF-1R/c-Fms, PDGFR-β, and c-Abl only at higher concentrations (IC50 = 236, 380, 640, and 2820 nM, respectively). AAL933 and two other VEGFR inhibitors, KRN633 and SU5416, are also shown to inhibit hypoxia-induced HIF-1α expression (by <90% at 30 M) and transcription activation. Unlike KRN633 and SU5416, AAL933 prevents only hypoxia-induced Erk, but not Akt, phosphorylation in HeLa cells.
in vitro
aal-993 was found to be a highly potent and selective inhibitor of the recombinant vegfr-2 and vegfr-3 kinases. at 3- to 5-fold higher concentration, aal-993 also inhibited vegfr-1 and, although it possessed some activity against other members of the pdgfr kinase family at submicromolar concentrations, aal-993 did not significantly inhibit any of the other kinases tested at concentrations
in vivo
animal efficacy study found that aal-993 was able to potently inhibit vegf-induced angiogenesis in an implant model, with ed50 values of 7 mg/kg. moreover, in a mouse orthotopic model of melanoma, aal-993 could potently inhibit both the growth of the primary tumor as well as the formation of spontaneous peripheral metastases [1].
IC 50
130, 23, and 18 nm for vegfr1, 2, and 3, respectively
References
1) Manley et al. (2002), Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors; J. Med. Chem., 45 5687 2) Manley et al. (2004), Advances in the structural biology, design and clinical development of VEGF-R kinase inhibitors for the treatment of angiogenesis; Biochim. Biophys. Acta, 1697 17
AAL-993 Preparation Products And Raw materials
Raw materials
Preparation Products
AAL-993 Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10522 | 58 |
InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |
Shanghai Boyle Chemical Co., Ltd. | sales@boylechem.com | China | 2923 | 55 | |
Sigma-Aldrich | 021-61415566 800-8193336 | orderCN@merckgroup.com | China | 51471 | 80 |
Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696,15000506266 15000506266 | China | 4334 | 55 | |
Shanghai EFE Biological Technology Co., Ltd. | 021-65675885 18964387627 | info@efebio.com | China | 9806 | 58 |
ShangHai Biochempartner Co.,Ltd | 17754423994 17754423994 | 2853530910@QQ.com | China | 8014 | 62 |
Chuzhou KeMail Chemical Technology Co., Ltd | 0550-5196001 15000891977 | wj520wjxby@126.com | China | 1841 | 55 |