Alternate TextTo enhance service speed and avoid tariff delays, we've opened a US warehouse. All US orders ship directly from our US facility.
Home > Products > Novel inhibitors

RBN-2397

  Cat. No.:  DC31069   Featured
Chemical Structure
2381037-82-5
For research use only. We do not sell to patients.
We match the best price and quality on market.
Email:order@dcchemicals.com  sales@dcchemicals.com
Tel:+86-021-58447131
Get Quotation Now
We are official vendor of:
  • 20
  • 19
  • 18
  • 17
  • 16
  • 15
  • 14
  • 12
  • 11
  • 10
  • 9
  • 8
  • 13
  • 6
  • 5
  • 4
  • 3
  • 2
  • 1
More than 5000 active chemicals with high quality for research!
Field of application
RBN-2397 is a potent, accross species and orally active NAD+ competitive inhibitor of PARP7 (IC50<3 nM). RBN-2397 selectively binds to PARP7 (Kd=0.001 μM) and restores interferon (Type I) signaling. RBN-2397 has the potential for the study of advanced or
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2381037-82-5
Chemical Name: RBN-2397
Synonyms: RBN-2397,RBN 2397，RBN2397
SMILES: O=C1NN=CC(N[C@H](COCCC(=O)N2CCN(C3N=CC(C(F)(F)F)=CN=3)CC2)C)=C1C(F)(F)F
Formula: C20H23F6N7O3
M.Wt: 523.43
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: [1]. RBN-2397-Inhibiting PARP7, a Key monoPARP Cancer Dependency [2]. Melissa Vasbinder, et al. RBN-2397: A First-in-Class PARP7 Inhibitor Targeting a Newly Discovered Cancer Vulnerability in Stress-Signaling Pathways.
Description: RBN-2397 is a potent, accross species and orally active NAD+ competitive inhibitor of PARP7 (IC50<3 nM). RBN-2397 selectively binds to PARP7 (Kd=0.001 μM) and restores interferon (Type I) signaling. RBN-2397 has the potential for the study of advanced or metastatic solid tumors[1][2].
In Vivo: RBN-2397 (oral administration; 3-100 mg/kg; once daily; 24-32 days) induces tumor-specific adaptive immune memory in CT26 syngeneic model with durable complete responses in CT26 tumor-bearing BALB/c mice[2]. RBN-2397 (oral administration; 3-100 mg/kg; once daily; 32 days) causes complete regressions at the dose 100 mg/kg and exerts a dose-dependent effects on tumor growth at dose levels of ≥30 mg/kg[2]. The half-life (t1/2) of RBN-2397 in vivo is 325 mins[2]. Animal Model: CB17 SCID mice with NCI-H1373 xenografts[2] Dosage: 3 mg/kg, 10mg/kg, 30 mg/kg, 100 mg/kg Administration: Oral administration; once daily; 24-32 days Result: Decreased tumor volume and exerted anti-tumor effects.
In Vitro: RBN-2397 (0.0001-100 μM; 24 hours) inhibits cells proliferation with an IC50 value of 20 nM in NCI-H1373 lung cancer cells[2]. RBN-2397 (0.4 nM-1 μM; 24 hours) shows a restoration of type I IFN response by an increase in STAT1 phosphorylation as a dose-dependent manner in NCI-H1373 human lung cancer cells[2]. RBN-2397 (0.0001-1 μM; 24 hours) inhibits cell MARylation in a cell biochemial assay with an EC50 value of 1 nM[2]. Cell Proliferation Assay[2] Cell Line: NCI-H1373 lung cancer cells Concentration: 0.0001 μM; 0.001 μM; 0.001 μM; 0.1 μM; 1 μM; 10 μM; 100 μM Incubation Time: 24 hours Result: Blocked cell proliferation. Western Blot Analysis[2] Cell Line: NCI-H1373 lung cancer cells Concentration: 0.4 nM-1 μM Incubation Time: 24 hours Result: Increased p-STAT1 protein expression.
MSDS
TITLE DOWNLOAD
MSDS_13389_DC31069_2381037-82-5
COA
LOT NO. DOWNLOAD
Cat. No. Product name Field of application
DC60859 MT-125(MT 125) MT125​​ is a brain-penetrant small-molecule inhibitor selectively targeting non-muscle myosin IIA/B (NMIIA/B) with >20-fold specificity over cardiac myosin. It demonstrates potent anti-glioblastoma activity by: (1) blocking tumor invasion and cytokinesis (inducing polyploidy), (2) disrupting mitochondrial dynamics to elevate ROS and trigger ferroptosis, and (3) sensitizing tumors to radiotherapy/kinase inhibitors via ROS-driven PDGFR/mTOR pathway activation. Subcutaneous administration achieves brain concentrations twice plasma levels (t1/2~10.5 hr) with no toxicity observed at 15× the therapeutic dose in rats. MT-125 monotherapy extends survival in GBM models, while combinations with PDGFR/PI3K inhibitors induce long-term remission (>40% mice). Its first-in-class mechanism, safety profile, and CNS bioavailability support clinical development for glioblastoma.
DC60781 TRPC6 activator compound 2 TRPC6 activator compound 2 is selective activator of TRPC6 that does not potentiate TRPC3 and mTRPC7. Comp2 is able to cross BBB.
DC66546 R-Sirpiglenastat R-Sirpiglenastat is the R- isomer of Sirpiglenastat(DRP-104).Sirpiglenastat (DRP104) is a broad acting glutamine antagonist. Sirpiglenastat has anticancer effects by directly targeting tumor metabolism and simultaneously inducing a potent antitumor immune response.
DC60597 AZD0780 AZD0780 is the first oral small molecule PCSK9 inhibitor for the treatment of hypercholesterolemia.
DC90056 PLX-5622 HCl form (water solubility form) PLX5622 is the HCl salt form of PLX-5622, which has better water solubility.PLX-5622 is a highly selective brain-penetrant CSF1R inhibitor (IC50=0.016 µM; Ki=5.9 nM) allowing for extended and specific microglial elimination, preceding and during pathology development.
DC65830 1-M-PES(1-Methoxy-5-methylphenazinium ethyl sulfate) 1-m-PES is an electron mediator which has higher stability of solutions than 1-Methoxy PMS. The stability in neutral to alkali conditions has been extremely improved with 1-Methoxy PES. 1-M-PES is a stable small-molecular compound and it has an equal or higher thermal stability than diaphorase. The 1-Methoxy PES solution can be stored long term.
DC65821 Upadacitinib hemihydrate Upadacitinib (ABT-494) is a potent and selective Janus kinase (JAK) 1 inhibitor with an IC50 of 43 nM, being developed for the treatment of several autoimmune disorders.
DC65697 HDAC6 inhibitor 4510 A novel and seletive HDAC6 inhibitor.
DC65676 Fenretinide Glucuronide Monosodium Salt Fenretinide Glucuronide Monosodium Salt, is the metabolite of Fenretinide (F250000), which is a synthetic retinoid deriverative, substances related to vitamin A. They are also shown to be used for the treatment of cancer, as well as in the treatment of cystic fibrosis, rheumatoid arthritis, acne, and psoriasis.
DC89083 Pacritinib citrate Pacritinib Citrate is the citrate salt form of pacritinib, an orally bioavailable inhibitor of Janus kinase 2 (JAK2).
X
Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.
Site Map|Privacy PolicyCopyright © 2018-2020 All Rights Reserved. Technical Support:KuuJia