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/ Ripretinib/瑞普替尼

Ripretinib/瑞普替尼 {[allProObj[0].p_purity_real_show]}

货号：A725907 同义名： 瑞派替尼 / DCC-2618

Ripretinib是一种口服生物利用的、选择性的 KIT 和 PDGFRA 抑制剂，通过作用于开关口袋结合位点，抑制激酶活性，同时对 FLT3 和 VEGFR-2 也有抑制作用，具有抗肿瘤活性并诱导细胞凋亡。

Ripretinib/瑞普替尼 化学结构 CAS号：1442472-39-0
Ripretinib/瑞普替尼 化学结构
CAS号：1442472-39-0
Ripretinib/瑞普替尼 3D分子结构
CAS号：1442472-39-0
Ripretinib/瑞普替尼 化学结构 CAS号：1442472-39-0
Ripretinib/瑞普替尼 3D分子结构 CAS号：1442472-39-0
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Ripretinib/瑞普替尼 纯度/质量文件 产品仅供科研

货号：A725907 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

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更多 >
产品名称 c-Kit ↓ 其他靶点 纯度
Tyrphostin AG1296 +

c-Kit (Swiss 3T3), IC50: 1.8 μM

 		PDGFR 99%+
Masitinib +

Kit, IC50: 200 nM

 		99%+
Motesanib Diphosphate +++

Kit, IC50: 8 nM

 		97%
Ki8751 ++

c-Kit, IC50: 40 nM

 		99%
Tivozanib ++

c-Kit, IC50: 78 nM

 		99%+
Pazopanib +

c-Kit, IC50: 140 nM

 		99%
Sitravatinib +++

Kit, IC50: 6 nM

 		99%+
Pexidartinib +++

Kit, IC50: 10 nM

 		99%+
Lactate ++++

c-Kit, IC50: 2 nM

 		FLT3 85%
Amuvatinib +++

c-Kit (D816H), IC50: 10 nM

 		99%+
Imatinib Mesylate +

c-Kit, IC50: 100 nM

 		PDGFR 99%
AZD2932 +++

c-Kit, IC50: 9 nM

 		99%
Axitinib ++++

Kit, IC50: 1.7 nM

 		98%
Dovitinib ++++

c-Kit, IC50: 2 nM

 		FLT3 99%+
Sunitinib ✔ FLT3 98%
OSI-930 +

Kit, IC50: 80 nM

 		99%+
Telatinib ++++

c-Kit, IC50: 1 nM

 		99%+
Dasatinib monohydrate ++

c-Kit (wt), IC50: 79 nM

c-Kit (D816V), IC50: 37 nM

 		Src 98%
Dasatinib ++

c-Kit (wt), IC50: 79 nM

c-Kit (D816V), IC50: 37 nM

 		Src 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
产品名称 PDGFR ↓ PDGFRα ↓ PDGFRβ ↓ 其他靶点 纯度
Tyrphostin A9 +

PDGFR, IC50: 0.5 μM

 		EGFR 98%
Tyrphostin AG1296 99%+
Motesanib Diphosphate ++

PDGFR, IC50: 84 nM

 		97%
Pazopanib ++

PDGFR, IC50: 84 nM

 		99%
Imatinib +

PDGFR, IC50: 100 nM

 		c-Kit 98%
Imatinib Mesylate +

PDGFR, IC50: 100 nM

 		c-Kit 99%
Sennoside B ✔ 99%+
PP121 ++++

PDGFR, IC50: 2 nM

 		VEGFR,mTOR 99%+
Crenolanib ++++

PDGFRα, Kd: 2.1 nM

 		++++

PDGFRβ, Kd: 3.2 nM

 		99%+
Masitinib +

PDGFRα, IC50: 540 nM

 		+

PDGFRβ, IC50: 800 nM

 		99%+
Ki8751 ++

PDGFRα, IC50: 67 nM

 		c-Kit 99%
Tivozanib ++

PDGFRα, IC50: 40 nM

 		++

PDGFRβ, IC50: 49 nM

 		99%+
Ponatinib ++++

PDGFRα, IC50: 1.1 nM

 		98%
Amuvatinib ++

PDGFRα (V561D), IC50: 40 nM

 		99%+
Axitinib +++

PDGFRα, IC50: 5.0 nM

 		++++

PDGFRβ, IC50: 1.6 nM

 		98%
CP-673451 +++

PDGFRα, IC50: 10 nM

 		++++

PDGFRβ, IC50: 1 nM

 		99%+
Telatinib +++

PDGFRα, IC50: 15 nM

 		c-Kit 99%+
Nintedanib ++

PDGFRα, IC50: 59 nM

 		++

PDGFRβ, IC50: 65 nM

 		99+%
Avapritinib ++++

PDGFRα (D842V), IC50: 0.5 nM

 		99%+
MK-2461 +++

PDGFRβ, IC50: 22 nM

 		98%+
Lactate +++

PDGFRβ, IC50: 27 nM

 		FLT3,c-Kit 85%
Linifanib ++

PDGFRβ, IC50: 66 nM

 		99%+
AZD2932 +++

PDGFRβ, IC50: 4 nM

 		c-Kit 99%
Dovitinib +++

PDGFRβ, IC50: 27 nM

 		FLT3,c-Kit 99%+
Sorafenib ++

PDGFRβ, IC50: 57 nM

mPDGFRβ, IC50: 57 nM

 		99%
Sunitinib ++++

PDGFRβ , IC50: 2 nM

 		FLT3 98%
Orantinib +++

PDGFRβ, Ki: 8 nM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Ripretinib/瑞普替尼 生物活性

描述 DCC-2618 is a pan-KIT and PDGFRA inhibitor, and has antitumor activity.

Ripretinib/瑞普替尼 细胞实验

Cell Line
Concentration Treated Time Description References
M3 cells 16, 64, 256 nM 5 days Ripretinib in combination with MEKi (trametinib) also showed significant synergy in M3 cells, effectively inhibiting MPNST cell growth. Clin Cancer Res. 2024 Nov 15;30(22):5154-5165.
ST88-14 cells 16, 64, 256 nM 5 days Ripretinib in combination with MEKi (trametinib) significantly enhanced the inhibitory effect on MPNST cell growth and showed strong synergy. Clin Cancer Res. 2024 Nov 15;30(22):5154-5165.
OCCC spheroid cells 1–5 µM 7 days Ripretinib significantly enhanced the inhibitory effect of carboplatin on OCCC cell proliferation when co-cultured with CAFs Cell Rep Med. 2024 May 21;5(5):101532.
CAFs 1–5 µM 7 days Inhibited CAF survival and enhanced the inhibitory effect of carboplatin on OCCC cell proliferation Cell Rep Med. 2024 May 21;5(5):101532.
32D KITD816V cells 0.7 nM Evaluate the anti-proliferative effect of compound 54 on 32D KITD816V cells, showing a GI50 value of 0.7 nM. Acta Pharm Sin B. 2022 Oct;12(10):4004-4007.
32D KITD816V cells 1010 nM Evaluate the anti-proliferative effect of compound 13 on 32D KITD816V cells, showing a GI50 value of 1010 nM. Acta Pharm Sin B. 2022 Oct;12(10):4004-4007.
GIST-RPR 80 nM 24 h To investigate the effect of USP5 knockdown on GIST cell proliferation, results showed that USP5 knockdown reduced cell proliferation ability. Adv Sci (Weinh). 2024 Sep;11(34):e2401171.
GIST-RPS 80 nM 24 h To investigate the effect of USP5 expression levels on GIST cell proliferation, results showed that USP5 overexpression increased cell proliferation ability. Adv Sci (Weinh). 2024 Sep;11(34):e2401171.
AKP cells 1 μM Tested the response of AKP cells under growth-factor-poor conditions, confirming their growth dependence on KIT signaling Nature. 2024 May;629(8011):450-457.

Ripretinib/瑞普替尼 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
CB17 SCID mice MPNST-2 PDX model Oral 25 mg/kg Once daily until the end of the experiment Ripretinib in combination with MEKi (trametinib) showed significant anti-tumor effects in the MPNST-2 PDX model, significantly inhibiting tumor growth and leading to tumor regression. Clin Cancer Res. 2024 Nov 15;30(22):5154-5165.
NOG mice OCCC xenograft model Oral 50 mg/kg Once daily for 28 days Ripretinib in combination with carboplatin significantly inhibited the growth of OCCC xenograft tumors Cell Rep Med. 2024 May 21;5(5):101532.
Mice 32D KITD816V xenograft mice model Oral 20, 40 mg/kg Twice daily for 12 days Evaluate the anti-tumor efficacy of compound 54 in the 32D KITD816V xenograft mice model, showing dose-dependent inhibition of tumor growth with TGI values of 45% and 71%. Acta Pharm Sin B. 2022 Oct;12(10):4004-4007.
Nude mice Subcutaneous xenograft model Oral 100 mg/kg Once daily until the end of the experiment To investigate the effect of USP5 overexpression and knockdown on tumor growth, results showed that USP5 overexpression promoted tumor growth, while USP5 knockdown reduced tumor growth. Adv Sci (Weinh). 2024 Sep;11(34):e2401171.

Ripretinib/瑞普替尼 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.96mL

0.39mL

0.20mL

9.80mL

1.96mL

0.98mL

19.59mL

3.92mL

1.96mL

Ripretinib/瑞普替尼 技术信息

CAS号1442472-39-0
分子式C24H21BrFN5O2
分子量 510.36
SMILES Code O=C(NC1=CC=CC=C1)NC2=CC(C3=CC4=C(N(CC)C3=O)C=C(NC)N=C4)=C(Br)C=C2F
MDL No. MFCD31657437
别名 瑞派替尼 ;DCC-2618
运输蓝冰
InChI Key CEFJVGZHQAGLHS-UHFFFAOYSA-N
Pubchem ID 71584930
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, sealed in dry, 2-8°C
溶解方案

DMSO: 25 mg/mL(48.99 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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案 一
方案 二
方案 三

Tags: Ripretinib | 1442472-39-0 | DCC-2618 | DCC2618 | DCC 2618 | KIT/PDGFRA Inhibitor | Protein Tyrosine Kinase/RTK | Apoptosis | c-Kit | PDGFR | FLT3 | VEGFR | Apoptosis | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Ripretinib/瑞普替尼 纯度/质量文件 | Ripretinib/瑞普替尼 亚型比较 | Ripretinib/瑞普替尼 生物活性 | Ripretinib/瑞普替尼 实验方案 | Ripretinib/瑞普替尼 技术信息

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