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

China 125 India 4 United States 14 Global 143

Changzhou Chenhong Biotechnology Co., Ltd.

Tel: 0519-85788828 13775037613
Email: sales@chemrenpharm.com
Country: China
ProdList: 3600
Advantage: 58

Shanghai Chaolan Chemical Technology Center

Tel: 021-QQ：65489617 15618227136
Fax: 21-5161 9052
Email: Sales@ATKchemical.com
Country: China
ProdList: 7295
Advantage: 58

Olix (Shanghai) Pharmaceutical Technology Co., Ltd

Tel: 17316404525
Email: 209533805@qq.com
Country: China
ProdList: 9906
Advantage: 58

Shanghai Boyle Chemical Co., Ltd.

Tel
Fax: 86-21-57758967
Email: sales@boylechem.com
Country: China
ProdList: 2922
Advantage: 55

Daicel Chiral Technologies (China)CO.,LTD

Tel: 021-50460086-9 15921403865
Fax: +86-21-50462321
Email: han_yajun@dctc.daicel.com
Country: China
ProdList: 7195
Advantage: 65

Dalian Meilun Biotech Co., Ltd.

Tel: 0411-62910999 13889544652
Email: sales@meilune.com
Country: China
ProdList: 4727
Advantage: 58

NCE Biomedical Co.,Ltd.

Tel: 4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
Fax: +86-27-87599188
Country: China
ProdList: 1493
Advantage: 55

Haoyuan Chemexpress Co., Ltd.

Tel: 021-58950125
Fax: (86) 21-58955996
Email: info@chemexpress.com
Country: China
ProdList: 7552
Advantage: 61

MedChemexpress LLC

Tel: 021-58955995
Fax: 609-228-5909
Email: sales@medchemexpress.cn
Country: United States
ProdList: 4861
Advantage: 58

AdooQ BioScience, LLC

Tel: +1 (866) 930-6790
Fax: +1 (866) 333-9607
Email: info@adooq.com
Country: United States
ProdList: 2782
Advantage: 58

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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

1229705-06-9, RG-7388Related Search:

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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