Batoprotafib TNO155|cas:1801765-04-7|西域试剂

Batoprotafib TNO155,99.43%

产品编号：Bellancom-136173| CAS NO：1801765-04-7| 分子式：C₁₈H₂₄ClN₇OS| 分子量：421.95

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货号	价格	库存与货期
Bellancom-136173	￥2400.00	杭州北京（现货）
Bellancom-136173	￥3840.00	杭州北京（现货）
Bellancom-136173	￥8060.00	杭州北京（现货）
Bellancom-136173	￥12000.00	杭州北京（现货）

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Batoprotafib 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-type SHP2 (IC₅₀=0.011 µM). Batoprotafib has the potential for the study of RTK-dependent malignancies, especially advanced solid tumors.

体外研究

Batoprotafib shows an IC₅₀ of 0.008 µM in KYSE520 pERK assay and shows an IC₅₀ of 0.100 µM in KYSE520 5-day cell proliferation assay. The off-target IC₅₀ values are 18 µM, 6.9 µM, and 11 µM for Cav1.2, VMAT, and SST3, respectively.
Batoprotafib (0-1000 nM; 6 days) inhibits the viability of NCI-H3255, HCC827, and PC9 cells with IC₅₀ values lower than 1.5 μM. Batoprotafib is efficacious in EGFR-mutant NSCLC cell lines.
Batoprotafib is efficacious in acquired resistance models of EGFR inhibitors and demonstrates combination benefit with EGFR inhibitors.
Batoprotafib enhances the efficacy of KRAS^G12C inhibitors against KRAS^G12C lung and colorectal cancers.
Batoprotafib inhibits immune-suppressive macrophages and synergizes with PD1 blockade.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line:	PC-9, PC-9 EGFR^T790M/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 EGFR^T790M/C797S, HCC827 and HCC827-GR cells, respectively.

Western Blot Analysis

Cell Line:	PC-14 (EGFR^ex19del)
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.
Batoprotafib (20 mg/kg; p.o.; twice daily for 40 days) inhibits tumor growth and is more effective when combined with Dabrafenib (HY-14660) plus Trametinib (HY-10999) in nude mice bearing HT-29 xenografts.
Batoprotafib (7.5 mg/kg; p.o.; b.i.d. or q.d. for 36 days) plus JDQ-443 (HY-139612) (100 mg/kg; p.o.; q.d.) improves the single-agent activity of JDQ443 in KRAS^G12C-mutated cell-derived (CDX) models in nude mice.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female athymic nude mice bearing HT-29 xenografts
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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female athymic nude mice bearing HT-29 xenografts
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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female athymic nude mice bearing HT-29 xenografts
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.

性状

Solid

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 mg	5 mg	10 mg

1 mM	2.3699 mL	11.8497 mL	23.6995 mL
5 mM	0.4740 mL	2.3699 mL	4.7399 mL
10 mM	0.2370 mL	1.1850 mL	2.3699 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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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-CD in 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 μL 20% 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。