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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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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
Synonyms | 2-((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 |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | TP-0903 is a potent and selective AXL Inhibitor with IC50 of 27 nM. TP-0903 is highly effective in inducing apoptosis. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor 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 |
ALogP | 4.023 |
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HBD Count | 2 |
Rotatable Bond | 8 |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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Tyrosine-protein kinase ABL inhibitor | INHIBITOR | ALA1862 | Tyrosine-protein kinase ABL | SINGLE PROTEIN | Homo sapiens | DailyMed: [1] | |
Tyrosine-protein kinase ABL inhibitor | INHIBITOR | ALA1862 | Tyrosine-protein kinase ABL | SINGLE PROTEIN | Homo sapiens | DailyMed: [1] | |
Tyrosine-protein kinase ABL inhibitor | INHIBITOR | ALA1862 | Tyrosine-protein kinase ABL | SINGLE PROTEIN | Homo sapiens | Expert: [1] | |
Tyrosine-protein kinase ABL inhibitor | INHIBITOR | ALA1862 | Tyrosine-protein kinase ABL | SINGLE PROTEIN | Homo sapiens | ||
Tyrosine-protein kinase ABL inhibitor | INHIBITOR | ALA1862 | Tyrosine-protein kinase ABL | SINGLE PROTEIN | Homo sapiens | ||
Tyrosine-protein kinase ABL inhibitor | INHIBITOR | ALA1862 | Tyrosine-protein kinase ABL | SINGLE PROTEIN | Homo sapiens | ||
Tyrosine-protein kinase ABL inhibitor | INHIBITOR | ALA1862 | Tyrosine-protein kinase ABL | SINGLE PROTEIN | Homo sapiens | ||
Tyrosine-protein kinase ABL inhibitor | INHIBITOR | ALA1862 | Tyrosine-protein kinase ABL | SINGLE PROTEIN | Homo sapiens | ||
Tyrosine-protein kinase ABL inhibitor | INHIBITOR | ALA1862 | Tyrosine-protein kinase ABL | SINGLE PROTEIN | Homo sapiens | ||
Tyrosine-protein kinase ABL inhibitor | INHIBITOR | ALA1862 | Tyrosine-protein kinase ABL | SINGLE PROTEIN | Homo sapiens | PubMed: [1] |
IUPAC Name | 2-[[5-chloro-2-[4-[(4-methylpiperazin-1-yl)methyl]anilino]pyrimidin-4-yl]amino]-N,N-dimethylbenzenesulfonamide |
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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 |
Find and download the COA for your product by matching the lot number on the packaging.
4 results found
Lot Number | Certificate Type | Date | Item |
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H2206407 | Certificate of Analysis | Jun 02, 2022 | D413851 |
H2206455 | Certificate of Analysis | Jun 02, 2022 | D413851 |
H2206460 | Certificate of Analysis | Jun 02, 2022 | D413851 |
H2206469 | Certificate of Analysis | Jun 02, 2022 | D413851 |
Solubility | Solubility (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; |
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DMSO(mg / mL) Max Solubility | 3 |
DMSO(mM) Max Solubility | 5.813277526 |
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. 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, 2 (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, 5 (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, 9 (98): (37173-37184). [PMID:30647852] [10.1021/op500134e] |