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首页-小分子抑制剂&激动剂-Tyrosine Kinase-c-Fms (CSF1R)-Elzovantinib
Elzovantinib

Chemical Structure : Elzovantinib

CAS No.: 2271119-26-5

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Elzovantinib (TPX-0022, CSF1R-IN-2)

货号: PC-73167Not For Human Use, Lab Use Only.

Elzovantinib (TPX-0022, CSF1R-IN-2) is a potent inhibitor of MET/CSF1R/SRC with biochemical IC50 of 0.14, 0.76 and 0.12 nM, respectively.

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10 mg ￥1980 In stock
25 mg ￥3580 In stock
100 mg ￥9580 In stock
250 mg ￥16800 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Elzovantinib (TPX-0022, CSF1R-IN-2) is a potent inhibitor of MET/CSF1R/SRC with biochemical IC50 of 0.14, 0.76 and 0.12 nM, respectively.
Elzovantinib (TPX-0022) inhibited both autophosphorylation of CSF1R with an IC50 <3 nM and cell growth with an IC50 of 14 nM in Ba/F3 ETV6-CSF1R cell model.
TPX-0022 effectively inhibited the growth of Ba/F3 ETV6-CSF1R xenograft tumors in vivo.
TPX-0022 not only exhibited potency with an IC50 of 0.3 nM, but also potently inhibited the growth of M-NFS-60 cells with an IC50 of 11.6 nM in the presence of exogenous CSF1 at 1 ng/mL in CSF1/CSF1R signaling-dependent M-NFS-60 model.
TPX-0022 effectively reduced tumor associated macrophages (TAMs), altered the polarity of TAMs toward a more M1 phenotype, increased cytotoxic T cells and inhibited the growth of MC38 tumors in MC38 syngeneic mouse model.

物理化学性质&存储条件

分子量 409.42
分子式 C20H20FN7O2
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 Month
Shipping
Solubility

Chemical Name/SMILES

参考文献

1. Vikas K. Goel, et al. Cancer Res (2021) 81 (13_Supplement): 1444.

2. Wei Deng, et al. Cancer Res (2019) 79 (13_Supplement): 1325.

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