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Altiratinib - 99%, high purity , Neurotrophic tyrosine kinase receptor inhibitor, CAS No.1345847-93-9, Neurotrophic tyrosine kinase receptor inhibitor

COA COA
In stock
Item Number
A413439
Grouped product items
SKU Size
Availability
 Price Qty
A413439-5mg
5mg
3
$59.90
A413439-25mg
25mg
2
$270.90
A413439-100mg
100mg
2
$489.90
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Bulk Order  SDS  DATASHEET  Specification Sheet

VEGFR2 Selective Inhibitors

View related series
c-Met/HGFR (76) FLT3 (103) kinase insert domain receptor Inhibitor (83) MET proto-oncogene，receptor tyrosine kinase Inhibitor (38) Neuronal Signaling (3320) Protein Tyrosine Kinase/RTK (1314) Receptor Tyrosine Kinase (1260) TEK receptor tyrosine kinase Inhibitor (11) Trk Receptor (42) VEGFR (187)

Basic Description

Synonyms NSC784590 | NSC-784590 | DCC-270 | J-690136 | Q27074416 | Altiratinib(DCC-2701) | s6412 | GNNDEPIMDAZHRQ-UHFFFAOYSA-N | AKOS026750329 | N-[4-[[2-[(Cyclopropylcarbonyl)amino]-4-pyridinyl]oxy]-2,5-difluorophenyl]-N'-(4-fluorophenyl)-1,1-cyclopropanedicarbox
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
This product requires cold chain shipping. Ground and other economy services are not available.
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 

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Organic oxygen compounds
Class Organooxygen compounds
Subclass Ethers
Intermediate Tree Nodes Not available
Direct Parent Diarylethers
Alternative Parents Anilides  Phenoxy compounds  Phenol ethers  N-arylamides  Fluorobenzenes  Aryl fluorides  Cyclopropanecarboxylic acids and derivatives  Pyridines and derivatives  Imidolactams  Heteroaromatic compounds  Secondary carboxylic acid amides  Azacyclic compounds  Hydrocarbon derivatives  Carbonyl compounds  Organofluorides  Organic oxides  
Molecular Framework Aromatic heteromonocyclic compounds
Substituents Diaryl ether - Anilide - Phenol ether - N-arylamide - Phenoxy compound - Fluorobenzene - Halobenzene - Aryl halide - Monocyclic benzene moiety - Imidolactam - Benzenoid - Aryl fluoride - Cyclopropanecarboxylic acid or derivatives - Pyridine - Heteroaromatic compound - Carboxamide group - Secondary carboxylic acid amide - Carboxylic acid derivative - Organoheterocyclic compound - Azacycle - Organonitrogen compound - Organic nitrogen compound - Hydrocarbon derivative - Organic oxide - Carbonyl group - Organohalogen compound - Organofluoride - Aromatic heteromonocyclic compound
Description This compound belongs to the class of organic compounds known as diarylethers. These are organic compounds containing the dialkyl ether functional group, with the formula ROR', where R and R' are aryl groups.
External Descriptors Not available

Product Properties

ALogP 3.867
hba_count 5
HBD Count 3
Rotatable Bond 8

Associated Targets(Human)

MET Tclin Hepatocyte growth factor receptor (4 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
TEK Tclin Angiopoietin-1 receptor (3 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
KDR Tclin Vascular endothelial growth factor receptor 2 (3 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
NTRK2 Tclin BDNF/NT-3 growth factors receptor (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
NTRK1 Tclin High affinity nerve growth factor receptor (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
NTRK3 Tclin NT-3 growth factor receptor (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
KDR Tclin Vascular endothelial growth factor receptor 2 (20924 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MET Tclin Hepatocyte growth factor receptor (10718 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
NTRK1 Tclin Nerve growth factor receptor Trk-A (7922 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
TEK Tclin Tyrosine-protein kinase TIE-2 (3348 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
K562 (73714 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KM12 (47707 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SK-N-SH (1499 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HepG2 (196354 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
NTRK2 Tclin Neurotrophic tyrosine kinase receptor type 2 (3279 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
NTRK3 Tclin NT-3 growth factor receptor (2338 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Names and Identifiers

Pubchem Sid 504771321
Pubchem Sid Url https://pubchem.ncbi.nlm.nih.gov/substance/504771321
IUPAC Name 1-N'-[4-[2-(cyclopropanecarbonylamino)pyridin-4-yl]oxy-2,5-difluorophenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
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)
InChIKey GNNDEPIMDAZHRQ-UHFFFAOYSA-N
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
Molecular Weight 510.46
Reaxy-Rn 21949406
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=21949406&ln=

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Find and download the COA for your product by matching the lot number on the packaging.

3 results found

Lot Number Certificate Type Date Item
G2206025 Certificate of Analysis Apr 07, 2025 A413439
G2206024 Certificate of Analysis Apr 07, 2025 A413439
G2206046 Certificate of Analysis Apr 07, 2025 A413439

Chemical and Physical Properties

Solubility Solubility (25°C) In vitro DMSO: 100 mg/mL (195.9 mM); Water: Insoluble; Ethanol: Insoluble;
DMSO(mg / mL) Max Solubility 100
DMSO(mM) Max Solubility 195.901735689378
Water(mg / mL) Max Solubility ＜1
Molecular Weight 510.500 g/mol
XLogP3 4.300
Hydrogen Bond Donor Count 3
Hydrogen Bond Acceptor Count 8
Rotatable Bond Count 8
Exact Mass 510.151 Da
Monoisotopic Mass 510.151 Da
Topological Polar Surface Area 109.000 Ų
Heavy Atom Count 37
Formal Charge 0
Complexity 863.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 0
Undefined Atom Stereocenter Count 0
Defined Bond Stereocenter Count 0
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 0
Covalently-Bonded Unit Count 1

Solution Calculators

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