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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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A413439-5mg | 5mg | In stock | $59.90 | |
A413439-25mg | 25mg | In stock | $270.90 | |
A413439-100mg | 100mg | In stock | $489.90 |
VEGFR2 Selective Inhibitors
Synonyms | Altiratinib|1345847-93-9|DCC-2701|DP-5164|Altiratinib [USAN]|Altiratinib(DCC-2701)|Altiratinib (USAN)|1,1-Cyclopropanedicarboxamide, N-[4-[[2-[(cyclopropylcarbonyl)amino]-4-pyridinyl]oxy]-2,5-difluorophenyl]-N'-(4-fluorophenyl)-|1,1-Cyclopropanedicarboxam |
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Specifications & Purity | Moligand™, ≥99% |
Biochemical and Physiological Mechanisms | Altiratinib (DCC-2701) is a potent single-digit nanomolar inhibitor of TRK, Met (c-Met), TIE2, and VEGFR2 kinases with IC50 vaules of 0.9 nM, 4.6 nM, and 0.8 nM for TRKA, B, and C, respectively. It inhibits Met (c-Met) and Met (c-Met) mutant with IC50 val |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Neurotrophic tyrosine kinase receptor inhibitor |
Product Description | Information Altiratinib (DCC-2701) is a potent single-digit nanomolar inhibitor ofTRK, Met (c-Met), TIE2, and VEGFR2 kinaseswith IC50 vaules of 0.9 nM, 4.6 nM, and 0.8 nM for TRKA, B, and C, respectively. It inhibits Met (c-Met) and Met (c-Met) mutant with IC50 values in the range of 0.3-6 nM. Targets MET Y1230C (Cell-free assay); TrkA (Cell-free assay); TrkC (Cell-free assay); MET Y1230C (Cell-free assay); MET D1228N (Cell-free assay) 31650,0.37 nM; 0.85 nM; 0.85 nM; 1.2 nM; 1.3 nM In vitro Altiratinib is >10-fold selective for MET versus FMS and KIT, and >50-fold selective for MET versus ABL1, FYN, HER1 (EGFR), p38α (MAPK14), PDGFRα, PDGFRβ, RET, and SRC. Altiratinib exhibits IC50s of 0.69 nmol/L in K562 cells, 1.2 nmol/L in SK-N-SH cells for inhibition of NGF-stimulated TRKA phosphorylation. Altiratinib inhibits constitutive TRKA phosphorylation with an IC50 of 1.4 nmol/L in KM-12 cells. Altiratinib inhibits HGF-stimulated MET phosphorylation in HUVECs, exhibiting an IC50 of 2.3 nmol/L. In ANG1-stimulated HUVECs and EA.hy926 cells, altiratinib exhibits IC50 values of 1.0 nmol/L and 2.6 nmol/L, respectively, for inhibition of TIE2 phosphorylation. In VEGF-stimulated HUVECs, altiratinib inhibits VEGFR2 phosphorylation with an IC50 of 4.7 nmol/L. Altiratinib potently inhibits cellular proliferation in MET-amplified EBC-1 and MKN-45 cells, as well as TPM3-TRKA fusion KM-12 cells, but only weakly inhibits other cancer cell lines, including proliferation of M-NFS-60 (IC50, 770 nmol/L); A375, BT-474, HCT-116, PC-3, SK-MEL-28, U87, and A549 cells (IC50s > 1,000 nmol/L). Cell Research(from reference) Cell lines:EBC-1, M-NFS-60, SK-MEL-28, MKN-45, MV-4-11, A375, HCT-116, BT-474, KM-12, PC-3, and U-87-MG cells Incubation Time:72 h |
ALogP | 3.867 |
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HBD Count | 3 |
Rotatable Bond | 8 |
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IUPAC Name | 1-N'-[4-[2-(cyclopropanecarbonylamino)pyridin-4-yl]oxy-2,5-difluorophenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide |
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INCHI | InChI=1S/C26H21F3N4O4/c27-15-3-5-16(6-4-15)31-24(35)26(8-9-26)25(36)32-20-12-19(29)21(13-18(20)28)37-17-7-10-30-22(11-17)33-23(34)14-1-2-14/h3-7,10-14H,1-2,8-9H2,(H,31,35)(H,32,36)(H,30,33,34) |
InChi Key | GNNDEPIMDAZHRQ-UHFFFAOYSA-N |
Canonical SMILES | C1CC1C(=O)NC2=NC=CC(=C2)OC3=C(C=C(C(=C3)F)NC(=O)C4(CC4)C(=O)NC5=CC=C(C=C5)F)F |
Isomeric SMILES | C1CC1C(=O)NC2=NC=CC(=C2)OC3=C(C=C(C(=C3)F)NC(=O)C4(CC4)C(=O)NC5=CC=C(C=C5)F)F |
PubChem CID | 54576299 |
Molecular Weight | 510.46 |
CAS Registry No. | 1345847-93-9 |
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PubChem CID | 54576299 |
ChEMBL Ligand | CHEMBL3545365 |
RCSB PDB Ligand | A9I, A9I |
Enter Lot Number to search for COA:
To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section
Lot Number | Certificate Type | Date | Item |
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G2206024 | Certificate of Analysis | Jun 07, 2022 | A413439 |
G2206025 | Certificate of Analysis | Jun 07, 2022 | A413439 |
G2206046 | Certificate of Analysis | Jun 07, 2022 | A413439 |
Solubility | Solubility (25°C) In vitro DMSO: 100 mg/mL (195.9 mM); Water: Insoluble; Ethanol: Insoluble; |
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DMSO(mg / mL) Max Solubility | 100 |
DMSO(mM) Max Solubility | 195.901735689378 |
Water(mg / mL) Max Solubility | <1 |
Pictogram(s) | GHS07 |
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Signal | Warning |
Hazard Statements | H315:Causes skin irritation H319:Causes serious eye irritation H335:May cause respiratory irritation H302:Harmful if swallowed |
Precautionary Statements | P261:Avoid breathing dust/fume/gas/mist/vapors/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing. |
1. Swale C, Bellini V, Bowler MW, Flore N, Brenier-Pinchart MP, Cannella D, Belmudes L, Mas C, Couté Y, Laurent F et al.. (2022) Altiratinib blocks Toxoplasma gondii and Plasmodium falciparum development by selectively targeting a spliceosome kinase.. Sci Transl Med, 14 (656): (eabn3231). [PMID:35921477] |