Tozasertib
Synonym(s):;N-[4-[[4-(4-Methyl-1-piperazinyl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-pyrimidinyl]thio]phenyl]cyclopropanecarboxamide;Tozasertib;
- CAS NO.:639089-54-6
- Empirical Formula: C23H28N8OS
- Molecular Weight: 464.59
- MDL number: MFCD13185152
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-19 23:02:33
What is Tozasertib?
Description
The Aurora kinases (A, B, and C) are a family of serine-
Chemical properties
White Solid
The Uses of Tozasertib
Tozasertib is used as a multikinase inhibitor once used for cancer treatment.
What are the applications of Application
Tozasertib is a potent and selective pan-ARK inhibitor
Definition
ChEBI: N-[4-[[4-(4-methyl-1-piperazinyl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-pyrimidinyl]thio]phenyl]cyclopropanecarboxamide is a N-arylpiperazine.
Biochem/physiol Actions
VX-680 is an ATP site-targeting potent aurora kinase inhibitor (Aurara A/B/C Ki(app) = 0.6/18/4.6 nM) that affects FLT3, BCR-Abl, BCR-Abl (T315I), Lck, ITK, Src, and Fyn only at higher concentrations (Ki(app) = 30, 30, 42, 80, 220, 350, 520 nM, respectively) and exhibits little inhibitory potency toward 52 other kinases (Ki(app) >1 μM). VX-680 exhibits potent antiproliferation activity in a wide variety of cancer cultures (IC50 from 15 to 113 nM) as a result of cell cycle arrest and apoptosis induction, as well as causes tumor retardation (by 98% on day 13; 75 mg/kg b.i.d i.p.; HL-60 in mice) and regression (2 mg/kg/h 3 d/wk i.v. infusion; HCT116 in rats) in vivo. Crystallography data reveal a tight association of VX-680 with a hydrophobic pocket present only in a closed, inactive kinase conformation, which forms the basis of its selectivity profile, including its activity toward wild-type and the Imatinib-resistant (T315I) Abl.
References
1) Harrington et al. (2004), VX-680, a potent and selective small molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo; Nat. Med., 10 262 2) Fei et al. (2010), Activity of the Aurora kinase inhibitor VX-680 against Bcr/Abl-positive acute lymphoblastic leukemias; Mol. Cancer Ther., 9 1318 3) Dewerth et al. (2012), In vitro evaluation of the Aurora kinase inhibitor VX-680 for Hepatoblastoma; Pediatr. Surg. Int., 28 579
Properties of Tozasertib
Melting point: | 248-253°C (dec.) |
Density | 1.40±0.1 g/cm3(Predicted) |
storage temp. | 2-8°C |
solubility | Soluble in DMSO (up to 100 mg/ml). |
form | powder |
pka | 14.09±0.70(Predicted) |
color | white to beige |
Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
Safety information for Tozasertib
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral |
Precautionary Statement Codes |
P280:Wear protective gloves/protective clothing/eye protection/face protection. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for Tozasertib
New Products
4-Aminotetrahydropyran-4-carbonitrile Hydrochloride (R)-3-Aminobutanenitrile Hydrochloride 4-AMINO-TETRAHYDRO-PYRAN-4-CARBOXYLIC ACID HCL 4-(Dimethylamino)tetrahydro-2H-pyran-4-carbonitrile 3-((Dimethylamino)methyl)-5-methylhexan-2-one oxalate 1,4-Dioxa-8-azaspiro[4.5]decane 5-Bromo-2-nitropyridine Nimesulide BP Aceclofenac IP/BP/EP Diclofenac Sodium IP/BP/EP/USP Mefenamic Acid IP/BP/EP/USP Ornidazole IP Diclofenac Potassium SODIUM AAS SOLUTION ZINC AAS SOLUTION BUFFER SOLUTION PH 10.0(BORATE) GOOCH CRUCIBLE SINTERED AQUANIL 5 BERYLLIUM AAS SOLUTION 2-Bromo-1-(bromomethyl)-3-chloro-5-nitrobenzene 2-Bromo-3-nitroaniline N-(3-Hydroxypropyl)-N-methylacetamide 3-Bromo-6-chloropyridazine 4-ethyl-3-nitrobenzoic acidRelated products of tetrahydrofuran
You may like
-
Tozasertib 98% (HPLC) CAS 639089-54-6View Details
639089-54-6 -
VX-680 CAS 639089-54-6View Details
639089-54-6 -
1823368-42-8 98%View Details
1823368-42-8 -
2-(3-(tert-butyl)phenoxy)-2-methylpropanoic acid 1307449-08-6 98%View Details
1307449-08-6 -
Ethyl 3-(furan-2-yl)-3-hydroxypropanoate 25408-95-1 98%View Details
25408-95-1 -
2-Chloro-5-fluoro-1-methoxy-3-methylbenzene 98%View Details
1805639-70-6 -
1784294-80-9 98%View Details
1784294-80-9 -
Lithium ClavulanateView Details
61177-44-4