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首页-小分子抑制剂&激动剂-Tyrosine Kinase-TAM Receptor (Tyro3-Axl-Mer)-TP-0903
TP-0903

Chemical Structure : TP-0903

CAS No.: 1341200-45-0

TP-0903 (TP0903;Dubermatinib)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 516.0587
分子式 C24H30ClN7O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
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-

参考文献

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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