Ripretinib (DCC-2618)

別名: DCC-2618

目錄號：S8757 Purity: 99.82%

Ripretinib是一種具有口服活性的Kit (c-Kit)和PDGFR-alpha抑制劑，對WT Kit (c-Kit)、V654A Kit (c-Kit)、T670I Kit (c-Kit)、D816H Kit (c-Kit)和D816V Kit (c-Kit)的IC50分別為4 nM、8 nM、18 nM、5 nM和14 nM。

Ripretinib (DCC-2618) Chemical Structure

CAS: 1442472-39-0

規(guī)格	價格	庫存
10mM (1mL in DMSO)	3333.33	現貨
5mg	1859.41	現貨
25mg	5651.24	現貨
100mg	13022.99	現貨
1g	31900	現貨
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產品質控

批次：純度： 99.82%

99.82

Ripretinib (DCC-2618)相關產品

相關產品	Masitinib Amuvatinib (MP-470) Sitravatinib (MGCD516) OSI-930 PDGFR inhibitor 1 AZD3229 ISCK03 Masitinib mesylate	點擊展開
相關化合物庫	激酶抑制劑庫酪氨酸激酶抑制劑分子庫 PI3K/Akt 抑制劑庫細胞周期化合物庫血管生成相關化合物庫	點擊展開

細胞實驗數據示例

細胞系	實驗類型	孵育時間	活性描述	文獻信息(PMID)
Growth inhibition assay	BA/F3	72 hrs	Inhibition of Kit exon 11 deletion (557 to 558 residues) and A829P mutant and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.003 μM.	30204441
Growth inhibition assay	BA/F3	72 hrs	Inhibition of Kit exon 11 deletion (557 to 558 residues) and N822K mutant and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.004 μM.	30204441
Growth inhibition assay	BA/F3	72 hrs	Inhibition of Kit exon 11 deletion (557 to 558 residues) mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.004 μM.	30204441
Growth inhibition assay	BA/F3	72 hrs	Inhibition of Kit exon 11 deletion (557 to 558 residues) and D820A mutant and D820A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.006 μM.	30204441
Growth inhibition assay	BA/F3	72 hrs	Inhibition of Kit exon 11 deletion (557 to 558 residues) and D816H mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.013 μM.	30204441
Growth inhibition assay	BA/F3	72 hrs	Inhibition of Kit exon 11 deletion (557 to 558 residues) and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.014 μM.	30204441
Growth inhibition assay	BA/F3	72 hrs	Inhibition of Kit V560D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.023 μM.	30204441
Growth inhibition assay	BA/F3	72 hrs	Inhibition of Kit exon 11 deletion (557 to 558 residues) and V654A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.031 μM.	30204441
Growth inhibition assay	BA/F3	72 hrs	Inhibition of Kit exon 9 AY502 to 503 insertion mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.034 μM.	30204441
Growth inhibition assay	BA/F3	72 hrs	Inhibition of Kit D816V mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.037 μM.	30204441
Growth inhibition assay	BA/F3	72 hrs	Inhibition of Kit exon 11 deletion (557 to 558 residues) and D816H mutant and T670I mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.037 μM.	30204441
Growth inhibition assay	BA/F3	72 hrs	Inhibition of TEL-fused PDGFRalpha (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.04 μM.	30204441
Growth inhibition assay	BA/F3	72 hrs	Inhibition of TEL-fused PDGFRbeta (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.045 μM.	30204441
Growth inhibition assay	BA/F3	72 hrs	Inhibition of Kit V560D/D816H mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.048 μM.	30204441
Growth inhibition assay	BA/F3	72 hrs	Inhibition of Kit V560D/V654A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.075 μM.	30204441
Growth inhibition assay	BA/F3	72 hrs	Inhibition of Kit exon 9 AY502 to 503 insertion and D816 mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.078 μM.	30204441
Growth inhibition assay	BA/F3	72 hrs	Inhibition of KDR (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.098 μM.	30204441
Growth inhibition assay	BA/F3	72 hrs	Inhibition of Kit exon 11 deletion (560 to 578 residues) mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.13 μM.	30204441
Growth inhibition assay	BA/F3	72 hrs	Inhibition of PDGFRalpha V561D/D842V mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.188 μM.	30204441
Growth inhibition assay	BA/F3	72 hrs	Inhibition of Kit exon 9 AY502 to 503 insertion and V654 mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.205 μM.	30204441
Cytotoxicity assay	BA/F3	72 hrs	Cytotoxicity in mouse parental BA/F3 cells incubated for 72 hrs by MTS assay, GI50 = 8.037 μM.	30204441
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生物活性

產品描述

靶點

PDGFR	WT KIT (Cell-free assay)	D816H KIT (Cell-free assay)	V654A KIT (Cell-free assay)	D816V KIT (Cell-free assay)	點擊更多
	4 nM	5 nM	8 nM	14 nM	點擊更多

體外研究(In Vitro)
體外研究活性	DCC-2618有效并廣泛地抑制KIT原發(fā)性和耐藥性突變體，如發(fā)生在外顯子9、11、13、14、17和18的突變，以及發(fā)生在PDGFRA外顯子12、14、18的原發(fā)性突變。DCC-2618以納摩爾級別的效力抑制多種性質的KIT：WT (IC50 4 nM), V654A (8 nM), T670I (18 nM), D816H (5 nM), D816V (14 nM)。在瞬時轉染了KIT原發(fā)性突變體和二次突變的CHO細胞中，DCC-2618抑制了外顯子17、外顯子9/13、外顯子9/14，外顯子9/17，外顯子11/17突變的KIT，包括位于外顯子17的D816V, D816G, D820A, D820E, D820Y, N822K, N822Y, N822H和Y823D原發(fā)性或二次突變。在MO7e細胞系中，DCC-2618抑制野生型KIT的磷酸化（IC50=36 nM）。在人源GIST細胞系中，包括GIST T1(缺失外顯子11)、GIST 430（缺失外顯子11/外顯子13 V654A）和GIST 48（外顯子11 V560D/外顯子17 D820A）, DCC-2618也能有效抑制KIT的激活。在小鼠肥大細胞增多癥中，DCC-2618可有效抑制P815細胞(表達外顯子17 D816Y 突變KIT)的增殖，IC50為2 nM。在多種人類肥大細胞系（HMC-1, ROSA, MCPV-1）和從晚期系統性肥大細胞增多癥患者體內分離的原代腫瘤肥大細胞中，DCC-2618可抑制其增殖和生存。
細胞實驗	細胞系	HMC-1.1, HMC-1.2, ROSA (KIT WT)和 ROSA (KIT D816V)細胞
	濃度	0.5-5 μM
	孵育時間	4 h
	方法	將細胞培養(yǎng)于對照組培養(yǎng)基中或加入0.5-5 μM DCC-2618，置于37℃培養(yǎng)4小時。結束后，收集細胞提取蛋白質，進行Western blotting分析。
實驗圖片	檢測方法	檢測指標	實驗圖片	PMID
實驗圖片	Western blot	KIT / BTK STAT5 / AKT / ERK		29439183

體內研究(In Vivo)
體內研究活性	在體內，50 mg/kg DCC-2618可在GIST T1移植瘤模型抑制KIT磷酸化，達到90%的有效劑量（ED90），EC50約為470 ng/mL。每日兩次口服給藥，DCC-2618可幾乎完全地造成腫瘤瘀滯。在移植瘤模型中，DCC-2618可阻止KIT和PFGFRA驅動的腫瘤生長。
動物實驗	Animal Models	小鼠移植瘤模型
	Dosages	100 mg/kg/day 或 25 mg/kg/day 或 50 mg/kg BID
	Administration	口服

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05080621	Withdrawn	Gastrointestinal Stromal Tumors	Deciphera Pharmaceuticals LLC	November 2021	Phase 1\|Phase 2
NCT04633122	Completed	Gastrointestinal Stromal Tumor(GIST)	Zai Lab (Shanghai) Co. Ltd.\|Zai Lab (Hong Kong) Ltd.	November 25 2020	Phase 2
NCT02571036	Completed	Gastrointestinal Stromal Tumors\|Advanced Systemic Mastocytosis\|Advanced Cancers	Deciphera Pharmaceuticals LLC	November 2015	Phase 1

參考文獻
[1]http://cancerres.aacrjournals.org/content/75/15_Supplement/2690 [2]https://pubmed.ncbi.nlm.nih.gov/29439183/ [3]https://www.deciphera.com/wp-content/uploads/2018/04/DCC-2618-Pre-Clinical-AACR-2018.pdf

參考文獻

[1]http://cancerres.aacrjournals.org/content/75/15_Supplement/2690
[2]https://pubmed.ncbi.nlm.nih.gov/29439183/
[3]https://www.deciphera.com/wp-content/uploads/2018/04/DCC-2618-Pre-Clinical-AACR-2018.pdf

化學信息&溶解度

分子量	510.36	分子式	C₂₄H₂₁BrFN₅O₂
CAS號	1442472-39-0	SDF	--
Smiles	CCN1C2=CC(=NC=C2C=C(C1=O)C3=CC(=C(C=C3Br)F)NC(=O)NC4=CC=CC=C4)NC
儲存條件(自收到貨起)	3年 -20°C 粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年 -20°C 粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1個月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 100 mg/mL ( (195.94 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 100 mg/mL ( (195.94 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計算器

體內溶解配方
批次：

現配現用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

動物體內配方計算器

實驗計算

摩爾濃度計算器

質量	濃度	體積	分子量
=	×	×

稀釋計算器分子量計算器

動物體內配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

給藥劑量 mg/kg 動物平均體重 g 每只動物給藥體積 μL 動物數量只

第二步：請輸入動物體內配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計算結果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯系Selleck）；

體內配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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操作手冊

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C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

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