Altiratinib
This product is for research use only, not for human use. We do not sell to patients.
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Size | Price | Stock |
---|---|---|
250mg | $700 | Check With Us |
500mg | $1200 | Check With Us |
1g | $1800 | Check With Us |
Cat #: V2885 CAS #: 1345847-93-9 Purity ≥ 98%
Description: Altiratinib (also known as DCC-2701 and DP-5164) is an orally active, highly potent and selective multi-kinase inhibitor with IC50 values of 2.7, 8, 9.2, 9.3, 0.85, 4.6, 0.83 nM for MET, TIE2, VEGFR2, FLT3, Trk1, Trk2, and Trk3.
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Molecular Weight (MW) | 510.46 |
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Molecular Formula | C26H21F3N4O4 |
CAS No. | 1345847-93-9 |
Storage | -20℃ for 3 years in powder formr |
-80℃ for 2 years in solvent | |
Solubility In Vitro | DMSO: ≥ 33 mg/mLr |
Water: <1 mg/mL | |
SMILES Code | O=C(C1(C(NC2=CC=C(F)C=C2)=O)CC1)NC3=CC(F)=C(OC4=CC(NC(C5CC5)=O)=NC=C4)C=C3F |
Synonyms | Altiratinib; DCC2701; DCC 2701; DCC-2701; DP 5164; DP5164; DP-5164 |
Protocol | In Vitro | Altiratinib also inhibits MET isoforms METD1228H, METD1228N, METY1230C, METY1230D, METY1230H, METM1250T with IC50s of 3.6, 1.3, 1.2, 0.37, 1.5 and 6 nM, respectively. Altiratinib inhibits MET phosphorylation with IC50 values of 0.85 and 2.2 nM, respectively. In the U-87 glioblastoma cell line, MET and HGF are both expressed. Altiratinib blocks autocrine activation of MET phosphorylation in these cells (IC50=6.2 nM). Altiratinib potently inhibits cellular proliferation in MET-amplified EBC-1 and MKN-45 cells, as well as TPM3-TRKA fusion KM-12 cells. Activation of MET is known to increase the motility and invasiveness of cancer cells: Altiratinib inhibits HGF-induced A549 cell migration, with an IC50 of 13 nM. Altiratinib also inhibits FLT3-ITD mutant MV-4-11 cell proliferation with an IC50 of 12 nM. |
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In Vivo | A single oral dose of 30 mg/kg Altiratinib leads to >95% inhibition of MET phosphorylation for the entire 24-hour period. A single 10 mg/kg oral dose of Altiratinib exhibits complete inhibition of MET phosphorylation through 12 hours and 73% inhibition at 24 hours postdose. Altiratinib dosed at 10 mg/kg twice a day leads to a significant 90% decrease in BLI signal. Altiratinib exhibits properties amenable to oral administration and exhibits substantial blood–brain barrier penetration, an attribute of significance for eventual treatment of brain cancers and brain metastases. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
Solvent volume to be added | Mass (the weight of a compound) | |||
---|---|---|---|---|
Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 1.9590 mL | 9.7951 mL | 19.5902 mL | 39.1803 mL |
5mM | 0.3918 mL | 1.9590 mL | 3.9180 mL | 7.8361 mL |
10mM | 0.1959 mL | 0.9795 mL | 1.9590 mL | 3.9180 mL |
20mM | 0.0980 mL | 0.4898 mL | 0.9795 mL | 1.9590 mL |
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