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Batoprotafib {[allProObj[0].p_purity_real_show]}

货号:A1258268 同义名: TNO155 Ambeed 开学季,买赠积分,赢豪礼

TNO155 is a potent selective and orally active allosteric inhibitor of wild-type SHP2 (IC50=0.011 µM). TNO155 has the potential for the study of RTK-dependent malignancies, especially advanced solid tumors[1].

Batoprotafib 化学结构 CAS号:1801765-04-7
Batoprotafib 化学结构
CAS号:1801765-04-7
Batoprotafib 3D分子结构
CAS号:1801765-04-7
Batoprotafib 化学结构 CAS号:1801765-04-7
Batoprotafib 3D分子结构 CAS号:1801765-04-7
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Batoprotafib 纯度/质量文件 产品仅供科研

货号:A1258268 标准纯度: {[allProObj[0].p_purity_real_show]}
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Batoprotafib 生物活性

描述 Batoprotafib (TNO155) is a highly potent, selective, and orally active allosteric inhibitor of wild-type SHP2, with an IC50 of 0.011 µM. It holds promise for investigating RTK-dependent malignancies, particularly advanced solid tumors [1].
体内研究

The oral bioavailability in mouse, rat, and monkey is 78%, 86%, and 60%, respectively [1].

Batoprotafib (20 mg/kg; oral administration; twice daily for 40 days) suppresses tumor growth and exhibits enhanced efficacy when administered in combination with Dabrafenib plus Trametinib in nude mice harboring HT-29 xenografts [2].

Batoprotafib (7.5 mg/kg; pO.; b.iD. or qD. for 36 days) in combination with JDQ-443 (100 mg/kg; pO.; qD.) enhances the efficacy of JDQ443 alone in KRASG12C-mutated cell-derived (CDX) models in nude mice [3].

体外研究

Batoprotafib exhibits an IC50 of 0.008 μM in the KYSE520 pERK assay and a 0.100 μM IC50 in the KYSE520 5-day cell proliferation assay. Off-target IC50 values are 18 μM, 6.9 μM, and 11 μM for Cav1.2, VMAT, and SST3, respectively [1].

Batoprotafib (0-1000 nM; 6 days) demonstrates inhibition of NCI-H3255, HCC827, and PC9 cell viability with IC50 values below 1.5 μM. It exhibits efficacy in EGFR-mutant NSCLC cell lines [2].

Batoprotafib is effective in acquired resistance models of EGFR inhibitors and shows synergistic effects when combined with EGFR inhibitors [2].

Batoprotafib improves the effectiveness of KRASG12C inhibitors in treating KRASG12C lung and colorectal cancers [2].

Batoprotafib suppresses immune-suppressive macrophages and enhances the effects of PD1 blockade [2].

Batoprotafib 参考文献

[1]TNO155: SHP2 inhibitor

[2]Liu C, et al. Combinations with Allosteric SHP2 Inhibitor TNO155 to Block Receptor Tyrosine Kinase Signaling. Clin Cancer Res. 2021 Jan 1;27(1):342-354.

[3]Weiss A, et al. Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRASG12C. Cancer Discov. 2022 Jun 2;12(6):1500-1517.

Batoprotafib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.37mL

0.47mL

0.24mL

11.85mL

2.37mL

1.18mL

23.70mL

4.74mL

2.37mL

Batoprotafib 技术信息

CAS号1801765-04-7
分子式C18H24ClN7OS
分子量 421.947
别名 TNO155
运输蓝冰
存储条件

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 105 mg/mL(248.85 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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