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Chemical Structure| 1442472-39-0 Chemical Structure| 1442472-39-0

Structure of Ripretinib
CAS No.: 1442472-39-0

Chemical Structure| 1442472-39-0

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

Synonyms: DCC-2618

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Product Details of Ripretinib

CAS No. :1442472-39-0
Formula : C24H21BrFN5O2
M.W : 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
Synonyms :
DCC-2618
MDL No. :MFCD31657437
InChI Key :CEFJVGZHQAGLHS-UHFFFAOYSA-N
Pubchem ID :71584930

Safety of Ripretinib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Ripretinib

RTK

Isoform Comparison

Biological Activity

In Vitro:

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.

In Vivo:

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.

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT06619275 GIST - Gastrointestinal Stroma... More >>l Tumor Less << RECRUITING 2025-11-27 Praxis für interdisziplin?re O... More >>nkologie und H?matologie, Freiburg, Germany Less <<
NCT04282980 Gastrointestinal Stromal Tumor... More >>s Less << PHASE2 COMPLETED 2022-08-23 Beijing Cancer Hospital, Beiji... More >>ng, Beijing, China|Chinese People's Liberation Army General Hospital, Beijing, Beijing, China|Union Medical College Hospital, Chongqing Medical University, Chongqing, Chongqing, China|Union Medical College Hospital, Fujian Medical University, Fuzhou, Fujian, China|The First Affiliated Hospital of Sun Yat-sen University, Guangzhou, Guangdong, China|The Sixth Affiliated Hospital of Sun Yat-sen University, Guangzhou, Guangdong, China|Fudan University Cancer Hospital, Shanghai, Shanghai, China|Renji Hospital, Shanghai Jiaotong University School of Medicine, Shanghai, Shanghai, China|West China Hospital of Sichuan University, Chengdu, Sichuan, China Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 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

 

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