RG-7388

ChemicalBook > CAS DataBase List > RG-7388

Clinical trials

Product Name: RG-7388
CAS No.: 1229705-06-9
Chemical Name: RG-7388
Synonyms: Idasanutlin;RG7388;Pexidartinib Hydrochloride;RG-7388;RG 7388;Ro 5503781;RG-7388 USP/EP/BP;RG-7388, Idasanutlin;Idasanutlin (RG-7388);RG 7388; RG-7388; RG7388
CBNumber: CB32666681
Molecular Formula: C31H29Cl2F2N3O4
Formula Weight: 616.48
MOL File: 1229705-06-9.mol

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RG-7388 Property

Melting point:: >261° (dec.)
Boiling point:: 737.3±60.0 °C(Predicted)
Density: 1.40±0.1 g/cm3(Predicted)
storage temp.: -20°C Freezer
solubility: DMSO (Slightly), Methanol (Slightly)
pka: 4.11±0.10(Predicted)
form: Solid
color: White to Off-White
InChIKey: TVTXCJFHQKSQQM-LJQIRTBHSA-N
SMILES: C(O)(=O)C1=CC=C(NC([C@H]2[C@H](C3=CC=CC(Cl)=C3F)[C@](C3=CC=C(Cl)C=C3F)(C#N)[C@H](CC(C)(C)C)N2)=O)C(OC)=C1

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 21532
Product name: RG7388
Purity: ≥98%
Packaging: 1mg
Price: $47
Updated: 2024/03/01

Cayman Chemical

Product number: 21532
Product name: RG7388
Purity: ≥98%
Packaging: 5mg
Price: $206
Updated: 2024/03/01

Cayman Chemical

Product number: 21532
Product name: RG7388
Purity: ≥98%
Packaging: 10mg
Price: $339
Updated: 2024/03/01

Cayman Chemical

Product number: 21532
Product name: RG7388
Purity: ≥98%
Packaging: 25mg
Price: $564
Updated: 2024/03/01

Tocris

Product number: 6904
Product name: Idasanutlin
Purity: ≥98%(HPLC)
Packaging: 50
Price: $609
Updated: 2021/12/16

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RG-7388 Chemical Properties,Usage,Production

Clinical trials

Idasanutlin (RG-7388) is a potent (Kd = 0.15 nM), selective small-molecule MDM2 antagonist that has demonstrated tolerable safety and encouraging clinical activity in an open-label, phase 1/1b trial in patients with AML, alone and in combination with cytarabine (composite CR rate, 35.6%). The phase 3 MIRROS (MDM2 antagonist Idasanutlin in Relapsed or Refractory acute myeloid leukemia [AML] for Overall Survival) trial (NCT02545283) evaluated the efficacy and safety of the small-molecule MDM2 antagonist idasanutlin plus cytarabine in patients with relapsed/refractory (R/R) AML. Adults (n = 447) with R/R AML whose disease relapsed or was refractory after ≤2 prior induction regimens as initial treatment or following salvage chemotherapy regimen, with Eastern Cooperative Oncology Group performance status ≤2 were enrolled regardless of TP53 mutation status and randomly assigned 2:1 to idasanutlin 300 mg or placebo orally twice daily plus cytarabine 1 g/m2 IV on days 1 to 5 of 28-day cycles. At primary analysis (cutoff, November 2019), 436 patients were enrolled, including 355 in the TP53 wild-type intention-to-treat (TP53WT-ITT) population. The primary endpoint, overall survival in the TP53WT-ITT population, was not met (median, 8.3 vs 9.1 months with idasanutlin-cytarabine vs placebo-cytarabine; stratified hazard ratio [HR], 1.08; 95% confidence interval [CI], 0.81-1.45; P = .58). The complete remission (CR) rate, a key secondary endpoint, was 20.3% vs 17.1% (odds ratio [OR], 1.23; 95% CI, 0.70-2.18). The overall response rate (ORR) was 38.8% vs 22.0% (OR, 2.25; 95% CI, 1.36-3.72). Common any-grade adverse events (≥10% incidence in any arm) were diarrhea (87.0% vs 32.9%), febrile neutropenia (52.8% vs 49.3%), and nausea (52.5% vs 31.5%). In summary, despite improved ORR, adding idasanutlin to cytarabine did not improve overall survival or CR rates in patients with R/R AML[1].

Description

Potent MDM2 inhibitor with an IC50 = 6 nM in binding assay and 30 nM in cancer cell proliferation assay. Induces p53 stabilisation, cell cycle arrest and apoptosis in cancer cells expression wildtype p53. Displays inhibition of tumor growth in the SJSA1 tumor xenograft model. Also inhibits MDR-1 at high concentrations.

Uses

Idasanutlin is an MDM2 inihibtor, blocking the p53 protein-protein interaction and may be used in anti-cancer treatments.

Side effects

Adverse events (AEs) reported across treatment cohorts included gastrointestinal events, hematologic events or events related to infections or infestations. Grade ≥3 AEs included hypokalemia, diarrhea, nausea and febrile aplasia or neutropenia. No unexpected toxicities were reported with the combination regimen compared with other relapse regimens containing cytarabine[2].

storage

Store at -20°C

References

[1] M. Konopleva. “Idasanutlin plus cytarabine in relapsed or refractory acute myeloid leukemia: results of the MIRROS trial.” Blood advances 6 1 (2022): 4147–4156.
[2] Pau Montesinos. “MIRROS: a randomized, placebo-controlled, Phase III trial of cytarabine ± idasanutlin in relapsed or refractory acute myeloid leukemia.” Future oncology 16 13 (2020): 807–815.

RG-7388 Preparation Products And Raw materials

Raw materials

Preparation Products

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RG-7388 Suppliers

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View Lastest Price from RG-7388 manufacturers

Career Henan Chemical Co

Product: RG-7388 1229705-06-9
Price: US $2.00/KG
Min. Order: 1KG
Purity: 98%
Supply Ability: 100g , 1kg, 5kg , 50kg
Release date: 2020-01-07

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Idasanutlin

4-[[[(2R,3S,4R,5S)-3-(3-Chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-(2,2-dimethylpropyl)-2-pyrrolidinyl]carbonyl]amino]-3-methoxybenzoic acid

RG 7388

RG7388

RG-7388

RG-7388, Idasanutlin

Idasanutlin (RG-7388)

RG 7388; RG-7388; RG7388

Pexidartinib Hydrochloride

4-[[(2R,3S,4R,5S)-3-(3-Chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-(2,2-dimet

4-{[(2R,3S,4R,5S)-4-(4-Chloro-2-fluoro-phenyl)-3-(3-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-3-methoxy-benzoic acid

Ro 5503781

Benzoic acid, 4-[[[(2R,3S,4R,5S)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-(2,2-dimethylpropyl)-2-pyrrolidinyl]carbonyl]amino]-3-methoxy-

4-{[(3s,4r,5s)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-(2,2-dimethylpropyl)-D-prolyl]amino}-3-methoxybenzoic acid

RG-7388 USP/EP/BP

4-[(2R,3S,4R,5S)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-(2,2-dimethylpropyl)pyrrolidine-2-amido]-3-methoxybenzoic acid

4-((2R,3S,4R,5S)-3-(3-Chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-neopentylpyrrolidine-2-carboxamido)-3-methoxybenzoic acid

4-{(3S,4R,5S)-3-(3-Chloro-2-fluorophenyl)-4-(2-fluoro-4-chlorophenyl)-4-cyano-5-(2,2-dimethylpropyl)-D-prolylamino}-3-methoxy-benzoic acid

4-[(3S,4R,5S)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-(2,2-dimethylpropyl)pyrrolidine-2-amido]-3-methoxybenzoic acid

1229705-06-9

C31H29Cl2F2N3O4

Inhibitors