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TP-0903

Chemical Structure : TP-0903

CAS No.: 1341200-45-0

TP-0903 (TP0903;Dubermatinib)

Catalog No.: PC-43297Not For Human Use, Lab Use Only.

TP-0903 (Dubermatinib, TP0903) is a potent, selective, orally bioavailable Axl inhibitor with IC50 of 27 nM inhibits cell viability of pncreactic cancer cells (PSN1) with IC50 of 6 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

TP-0903 (Dubermatinib, TP0903) is a potent, selective, orally bioavailable Axl inhibitor with IC50 of 27 nM inhibits cell viability of pncreactic cancer cells (PSN1) with IC50 of 6 nM.
TP-0903 also strongly inhibits related TAM family members MER and TYRO3, Aurora A/B (IC50=3.0/12.4 nM), JAK2, ALK, ABL1, and CHEK1 in a panel of 75 kinases (11/75 >50% inhibition at 200 nM)。
TP-0903 induces robust levels of apoptosis in CLL B-cells from all the CLL patients with mean LD50 of 0.14 uM; inhibits neuroblastoma cell growth, reduces NB cells intravasation in vitro and in vivo and enhances the sensitivity to conventional chemotherapy.

Physicochemical Properties

M.Wt 516.0587
Formula C24H30ClN7O2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 30 mg/mL

Chemical Name/SMILES

Benzenesulfonamide, 2-[[5-chloro-2-[[4-[(4-methyl-1-piperazinyl)methyl]phenyl]amino]-4-pyrimidinyl]amino]-N,N-dimethyl-

References

1. Sinha S, et al. Clin Cancer Res. 2015 May 1;21(9):2115-26.

2. Park IK, et al. Leukemia. 2015 Dec;29(12):2382-9.

3. Mollard A, et al. ACS Med Chem Lett. 2011 Dec 8;2(12):907-912.

4. Aveic S, et al. Eur J Pharmacol. 2018 Jan 5;818:435-448.

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