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Batoprotafib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Batoprotafib图片
CAS NO:1801765-04-7
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议

产品名称
TNO155
产品介绍
Batoprotafib (TNO155) 是一种有效的,选择性的,和具有口服活性野生型SHP2的变构抑制剂 (IC50= 0.011 μM)。Batoprotafib 有研究 RTK 依赖性恶性肿瘤的潜力,尤其是晚期实体瘤。
生物活性

Batoprotafib (TNO155) is a potent selective and orally active allosteric inhibitor of wild-typeSHP2(IC50=0.011 μM). Batoprotafib has the potential for the study of RTK-dependent malignancies, especially advanced solid tumors[1].

IC50& Target

IC50: 0.011 μM (SHP2)[1]

体外研究
(In Vitro)

Batoprotafib shows an IC50of 0.008 μM in KYSE520 pERK assay and shows an IC50of 0.100 μM in KYSE520 5-day cell proliferation assay. The off-target IC50values are 18 μM, 6.9 μM, and 11 μM for Cav1.2, VMAT, and SST3, respectively[1].
Batoprotafib (0-1000 nM; 6 days) inhibits the viability of NCI-H3255, HCC827, and PC9 cells with IC50values lower than 1.5 μM. Batoprotafib is efficacious in EGFR-mutant NSCLC cell lines[2].
Batoprotafib is efficacious in acquired resistance models of EGFR inhibitors and demonstrates combination benefit with EGFR inhibitors[2].
Batoprotafib enhances the efficacy of KRASG12Cinhibitors against KRASG12Clung and colorectal cancers[2].
Batoprotafib inhibits immune-suppressive macrophages and synergizes with PD1 blockade[2].

Cell Proliferation Assay[2]

Cell Line:PC-9, PC-9 EGFRT790M/C797S, HCC827, HCC827-GR (gefinitib-resistant)
Concentration:0-1000 nM
Incubation Time:6 days
Result:Inhibited cell viability with IC50s of 1.56, 1.38, 0.77 and 1.38 μM against PC-9 and PC-9 EGFRT790M/C797S, HCC827 and HCC827-GR cells, respectively.

Western Blot Analysis[2]

Cell Line:PC-14 (EGFRex19del)
Concentration:3 μM
Incubation Time:4h and 24 h
Result:Effectively reduced p-ERK levels at 4 hours but suffered a rebound at 24 hours.
体内研究
(In Vivo)

The oral bioavailability in mouse, rat and money are 78%, 86%, and 60%, respectively[1].
Batoprotafib (20 mg/kg; p.o.; twice daily for 40 days) inhibits tumor growth and is more effective when combined withDabrafenib(HY-14660) plusTrametinib(HY-10999) in nude mice bearing HT-29 xenografts[2].
Batoprotafib (7.5 mg/kg; p.o.; b.i.d. or q.d. for 36 days) plusJDQ-443(HY-139612) (100 mg/kg; p.o.; q.d.) improves the single-agent activity of JDQ443 inKRASG12C-mutated cell-derived (CDX) models in nude mice[3].

Animal Model:Female athymic nude mice bearing HT-29 xenografts[2]
Dosage:20 mg/kg alone or 10 mg/kg in combination with Dabrafenib and Trametinib
Administration:PO, twice daily for 40 days
Result:Resulted in moderate tumor growth inhibition. Maintained tumor stasis for more than 40 days when combined with Dabrafenib plus Trametinib.
Clinical Trial
分子量

421.95

性状

Solid

Formula

C18H24ClN7OS

CAS 号

1801765-04-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL(236.99 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.3699 mL11.8497 mL23.6995 mL
5 mM0.4740 mL2.3699 mL4.7399 mL
10 mM0.2370 mL1.1850 mL2.3699 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.5 mg/mL (5.92 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.92 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.5 mg/mL (5.92 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.92 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 5% DMSO    40%PEG300   5%Tween-80   50% saline

    Solubility: ≥ 2.5 mg/mL (5.92 mM); Clear solution

  • 4.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.08 mg/mL (4.93 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.93 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。