Sitravatinib(Synonyms: MGCD516; MG-516)

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Sitravatinib (Synonyms: MGCD516; MG-516) 纯度: 99.59%

Sitravatinib (MGCD516) 是一种有口服活性的受体酪氨酸激酶 (RTK) 抑制剂。抑制 Axl，MER，VEGFR3，VEGFR2，VEGFR1，KIT，FLT3，DDR2，DDR1，TRKA，和 TRKB，IC50 分别为 1.5 nM，2 nM，2 nM，5 nM，6 nM，6 nM，8 nM，0.5 nM，29 nM，5 nM，和 9 nM。Sitravatinib 单独使用即具有有效的抗肿瘤功效，且通过促进抗肿瘤免疫微环境增强了 PD-1 阻断的活性。

Sitravatinib(Synonyms: MGCD516; MG-516)

Sitravatinib Chemical Structure

CAS No. : 1123837-84-2

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Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥1219 In-stock
5 mg ￥880 In-stock
10 mg ￥1350 In-stock
50 mg ￥3900 In-stock
100 mg ￥6200 In-stock
200 mg ￥9950 In-stock
500 mg   询价  
1 g   询价  

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生物活性

Sitravatinib (MGCD516) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively[1]. Sitravatinib shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment[2].

IC50 & Target

VEGFR3

2 nM (IC50)

VEGFR1

6 nM (IC50)

VEGFR2

5 nM (IC50)

TrkA

5 nM (IC50)

TrkB

9 nM (IC50)

DDR1

29 nM (IC50)

DDR2

0.5 nM (IC50)

Axl

1.5 nM (IC50)

MER

2 nM (IC50)

FLT3

8 nM (IC50)

KIT

6 nM (IC50)

体外研究
(In Vitro)

Sitravatinib (0.01 nM-10 μM; 14 days) reduces colony formation in a dose-dependent manner in KLN205 and E0771 cell lines[2].
Sitravatinib (0.001-10 μM; 5 days) inhibits tumor cell viability with IC50s of approximately 1 μM in KLN205, E0771 and CT1B-A5 cell lines[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: KLN205, E0771, CT1B-A5 cells
Concentration: 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 5 days
Result: Inhibited KLN205, E0771, CT1B-A5 cells with IC50s of approximately 1 μM.

体内研究
(In Vivo)

Sitravatinib (20 mg/kg; p.o.; once per day for 6 days) significantly inhibits tumor progression and induces tumor regression in C57BL/6 mice bearing CT1B-A5 cells model[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 6-week-old C57BL/6 mice (bearing CT1B-A5 cells) [2]
Dosage: 20 mg/kg
Administration: Oral administration; once per day for 6 days
Result: Significantly inhibited tumor progression and induced tumor regression.

Clinical Trial

分子量

629.68

Formula

C33H29F2N5O4S
CAS 号

1123837-84-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 32 mg/mL (50.82 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.5881 mL 7.9405 mL 15.8811 mL
5 mM 0.3176 mL 1.5881 mL 3.1762 mL
10 mM 0.1588 mL 0.7941 mL 1.5881 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： 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: 2.75 mg/mL (4.37 mM); Suspended solution; Need ultrasonic

  • 2.

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

    Solubility: 2.5 mg/mL (3.97 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (3.97 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    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

  • 3.

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

    Solubility: 2.5 mg/mL (3.97 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (3.97 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    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
  • 4.

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

    Solubility: ≥ 2.5 mg/mL (3.97 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.97 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 25.0 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 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Patwardhan PP et al. Significant blockade of multiple receptor tyrosine kinases by MGCD516 (Sitravatinib), a novel small molecule inhibitor, shows potent anti-tumor activity in preclinical models of sarcoma. Oncotarget, 2016 Jan 26;7(4):4093-109.

    [2]. Du W, et al. Sitravatinib potentiates immune checkpoint blockade in refractory cancer models. JCI Insight. 2018 Nov 2;3(21). pii: 124184.

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