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Dubermatinib(TP-0903) - 98%, high purity , CAS No.1341200-45-0, Inhibitor of aurora kinase A;Inhibitor of aurora kinase B;Inhibitor of AXL receptor tyrosine kinase

Item Number
D413851
Grouped product items
SKUSizeAvailabilityPrice Qty
D413851-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$75.90
D413851-10mg
10mg
In stock
$107.90
D413851-25mg
25mg
In stock
$243.90
D413851-50mg
50mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$314.90
D413851-100mg
100mg
In stock
$489.90

Axl Inhibitors

Basic Description

Synonyms2-((5-chloro-2-((4-((4-methylpiperazin-1-yl)methyl)phenyl)amino)pyrimidin-4-yl)amino)-N,N-dimethylbenzenesulfonamide | 2-((5Chloro-2-((4-((4-methylpiperazin-1-yl)methyl)phenyl)amino)pyrimidin-4-yl)amino)-N,N-dimethylbenzenesulfonamide | EX-A609 | AMY10826
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsTP-0903 is a potent and selective AXL Inhibitor with IC50 of 27 nM. TP-0903 is highly effective in inducing apoptosis.
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of aurora kinase A;Inhibitor of aurora kinase B;Inhibitor of AXL receptor tyrosine kinase
Product Description

Information

Dubermatinib(TP-0903) TP-0903 is a potent and selective AXL Inhibitor with IC50 of 27 nM. TP-0903 is highly effective in inducing apoptosis .


Targets

Axl (Cell-free assay) 27 nM


In vitro

In pancreatic cancer cells (PSN-1), TP-0903 shows strong antiproliferative activity with IC50 of 6 M. TP-0903 also induces strong G2/M arrest by potently inhibiting Aurora A and B. [1] In CLL B cells from all the patients with CLL, TP-0903 causes a dose-dependent induction of massive apoptosis by targeting phosphorylated Axl, and overcomes CLL BMSC-mediated protection of CLL B cells from apoptosis.


In vivo

In the adult rat hippocampus, the intracerebroventricular administration of SAG (2.5 nM) significantly increases the number of newly generated cells and extends survival of hippocampal cells. In mice, SAG (20 μg/g, i.p.) effectively prevents GC-induced neonatal cerebellar developmental abnormalities.


Cell Research(from reference)

Cell lines:PSN-1 cells 

Incubation Time:96 hours 

Product Properties

ALogP4.023
HBD Count2
Rotatable Bond8

Associated Targets(Human)

AURKA Tchem Aurora kinase A (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
AURKB Tchem Aurora kinase B (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
AXL Tchem Tyrosine-protein kinase receptor UFO (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ABL1 Tclin Tyrosine-protein kinase ABL (18331 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CSNK1D Tchem Casein kinase I delta (4546 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AURKB Tchem Serine/threonine-protein kinase Aurora-B (6805 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
JAK2 Tclin Tyrosine-protein kinase JAK2 (12915 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CDK2 Tchem Cyclin-dependent kinase 2 (9050 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CHEK1 Tchem Serine/threonine-protein kinase Chk1 (6846 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AURKA Tchem Serine/threonine-protein kinase Aurora-A (10240 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PSN1 (345 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
U2OS (164939 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HepG2 (196354 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AXL Tchem Tyrosine-protein kinase receptor UFO (3469 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ALK Tclin ALK tyrosine kinase receptor (7132 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TYRO3 Tchem Tyrosine-protein kinase receptor TYRO3 (2906 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MERTK Tchem Proto-oncogene tyrosine-protein kinase MER (2687 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BRD4 Tchem Bromodomain-containing protein 4 (13122 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TRIM24 Tchem Transcription intermediary factor 1-alpha (2087 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BRPF1 Tchem Peregrin (2217 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HEK-293T (167025 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Mapk1 MAP kinase ERK2 (650 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Fgfr3 Fibroblast growth factor receptor 3 (21 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences
Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

DailyMed: [1]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

DailyMed: [1]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

Expert: [1]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

Expert: [1]


FDA: [1]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

DailyMed: [1]


Wikipedia: [1]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

Other: [1] , [2]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

ClinicalTrials: [1]


PubMed: [1]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

PubMed: [1] , [2]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

DOI: [1]


Other: [1]


PubMed: [1]


Tyrosine-protein kinase ABL inhibitorINHIBITORALA1862Tyrosine-protein kinase ABLSINGLE PROTEINHomo sapiens

PubMed: [1]


Names and Identifiers

IUPAC Name 2-[[5-chloro-2-[4-[(4-methylpiperazin-1-yl)methyl]anilino]pyrimidin-4-yl]amino]-N,N-dimethylbenzenesulfonamide
INCHI InChI=1S/C24H30ClN7O2S/c1-30(2)35(33,34)22-7-5-4-6-21(22)28-23-20(25)16-26-24(29-23)27-19-10-8-18(9-11-19)17-32-14-12-31(3)13-15-32/h4-11,16H,12-15,17H2,1-3H3,(H2,26,27,28,29)
InChi Key YUAALFPUEOYPNX-UHFFFAOYSA-N
Canonical SMILES CN1CCN(CC1)CC2=CC=C(C=C2)NC3=NC=C(C(=N3)NC4=CC=CC=C4S(=O)(=O)N(C)C)Cl
Isomeric SMILES CN1CCN(CC1)CC2=CC=C(C=C2)NC3=NC=C(C(=N3)NC4=CC=CC=C4S(=O)(=O)N(C)C)Cl
PubChem CID 56839178
Molecular Weight 516.06

Certificates

C of A & Other Certificates

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

4 results found

Lot NumberCertificate TypeDateItem
H2206407Certificate of AnalysisJun 02, 2022 D413851
H2206455Certificate of AnalysisJun 02, 2022 D413851
H2206460Certificate of AnalysisJun 02, 2022 D413851
H2206469Certificate of AnalysisJun 02, 2022 D413851

Chemical and Physical Properties

SolubilitySolubility (25°C) In vitro DMSO: 3 mg/mL warmed with 50ºC Water: bath (5.81 mM); Ethanol: 2 mg/mL warmed with 50ºC Water: bath (3.87 mM); Water: Insoluble;
DMSO(mg / mL) Max Solubility3
DMSO(mM) Max Solubility5.813277526
Water(mg / mL) Max Solubility<1

Safety and Hazards(GHS)

Pictogram(s) GHS07
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.

Related Documents

References

1. Mollard A, Warner SL, Call LT, Wade ML, Bearss JJ, Verma A, Sharma S, Vankayalapati H, Bearss DJ.  (2011)  Design, Synthesis and Biological Evaluation of a Series of Novel Axl Kinase Inhibitors..  ACS Med Chem Lett,  (12): (907-912).  [PMID:22247788] [10.1021/op500134e]
2. Patel V, Keating MJ, Wierda WG, Gandhi V.  (2016)  Preclinical combination of TP-0903, an AXL inhibitor and B-PAC-1, a procaspase-activating compound with ibrutinib in chronic lymphocytic leukemia..  Leuk Lymphoma,  57  (6): (1494-7).  [PMID:26440741] [10.1021/op500134e]
3. Sinha S, Boysen J, Nelson M, Secreto C, Warner SL, Bearss DJ, Lesnick C, Shanafelt TD, Kay NE, Ghosh AK.  (2015)  Targeted Axl Inhibition Primes Chronic Lymphocytic Leukemia B Cells to Apoptosis and Shows Synergistic/Additive Effects in Combination with BTK Inhibitors..  Clin Cancer Res,  21  (9): (2115-26).  [PMID:25673699] [10.1021/op500134e]
4. Jeon JY, Buelow DR, Garrison DA, Niu M, Eisenmann ED, Huang KM, Zavorka Thomas ME, Weber RH, Whatcott CJ, Warner SL et al..  (2020)  TP-0903 is active in models of drug-resistant acute myeloid leukemia..  JCI Insight,  (23): (1755-70).  [PMID:33268594] [10.1172/jci.insight.140169]
5. Sinha S, Boysen JC, Chaffee KG, Kabat BF, Slager SL, Parikh SA, Secreto CR, Call T, Shanafelt TD, Leis JF et al..  (2018)  Chronic lymphocytic leukemia cells from ibrutinib treated patients are sensitive to Axl receptor tyrosine kinase inhibitor therapy..  Oncotarget,  (98): (37173-37184).  [PMID:30647852] [10.1021/op500134e]

Solution Calculators