Ivosidenib
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MedKoo CAT#: 206507

CAS#: 1448347-49-6 (Ivosidenib)

Description: Ivosidenib, also known as AG-120 and RG-120, is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity. Ivosidenib specifically inhibits a mutated form of IDH1 in the cytoplasm, which inhibits the formation of the oncometabolite, 2-hydroxyglutarate (2HG). This may lead to both an induction of cellular differentiation and an inhibition of cellular proliferation in IDH1-expressing tumor cells.


Chemical Structure

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Ivosidenib
CAS# 1448347-49-6 (Ivosidenib)

Theoretical Analysis

MedKoo Cat#: 206507
Name: Ivosidenib
CAS#: 1448347-49-6 (Ivosidenib)
Chemical Formula: C28H22ClF3N6O3
Exact Mass: 582.1394
Molecular Weight: 582.97
Elemental Analysis: C, 57.69; H, 3.80; Cl, 6.08; F, 9.78; N, 14.42; O, 8.23

Price and Availability

Size Price Availability Quantity
50.0mg USD 150.0 Same day
100.0mg USD 250.0 Same day
200.0mg USD 450.0 Same day
500.0mg USD 950.0 Same day
1.0g USD 1650.0 Same day
2.0g USD 2950.0 Same day
5.0g USD 5850.0 2 Weeks
10.0g USD 9450.0 2 Weeks
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Related CAS #: 1448347-49-6 (Ivosidenib)   1448346-63-1 (AG-120 racemic)  

Synonym: Ivosidenib, AG-120; AG120; AG 120; RG-120; RG 120; RG120; Tibsovo;

IUPAC/Chemical Name: (S)-N-((S)-1-(2-chlorophenyl)-2-((3,3-difluorocyclobutyl)amino)-2-oxoethyl)-1-(4-cyanopyridin-2-yl)-N-(5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide

InChi Key: WIJZXSAJMHAVGX-DHLKQENFSA-N

InChi Code: InChI=1S/C28H22ClF3N6O3/c29-21-4-2-1-3-20(21)25(26(40)36-18-11-28(31,32)12-18)37(19-10-17(30)14-34-15-19)27(41)22-5-6-24(39)38(22)23-9-16(13-33)7-8-35-23/h1-4,7-10,14-15,18,22,25H,5-6,11-12H2,(H,36,40)/t22-,25-/m0/s1

SMILES Code: O=C([C@H](CC1)N(C2=NC=CC(C#N)=C2)C1=O)N([C@@H](C3=CC=CC=C3Cl)C(NC4CC(F)(F)C4)=O)C5=CC(F)=CN=C5

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 582.97 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Available from http://www.ncbi.nlm.nih.gov/books/NBK548827/ PubMed PMID: 31644134.

2: Hernandez Burgos P, Patel J, Chen A. Ivosidenib induction therapy complicated by myopericarditis and cardiogenic shock: A case report and literature review. J Oncol Pharm Pract. 2019 Aug 5:1078155219865934. doi: 10.1177/1078155219865934. [Epub ahead of print] PubMed PMID: 31382862.

3: Zakkula A, Dittakavi S, Maniyar MM, Syed N, Sulochana SP, Zainuddin M, Mullangi R. Validated HPLC method for simultaneous quantification of mutant IDH1/2 inhibitors (enasidenib, ivosidenib and vorasidenib) in mouse plasma: Application to a pharmacokinetic study. Biomed Chromatogr. 2019 Nov;33(11):e4658. doi: 10.1002/bmc.4658. Epub 2019 Sep 2. PubMed PMID: 31325170.

4: Lowery MA, Burris HA 3rd, Janku F, Shroff RT, Cleary JM, Azad NS, Goyal L, Maher EA, Gore L, Hollebecque A, Beeram M, Trent JC, Jiang L, Fan B, Aguado-Fraile E, Choe S, Wu B, Gliser C, Agresta SV, Pandya SS, Zhu AX, Abou-Alfa GK. Safety and activity of ivosidenib in patients with IDH1-mutant advanced cholangiocarcinoma: a phase 1 study. Lancet Gastroenterol Hepatol. 2019 Sep;4(9):711-720. doi: 10.1016/S2468-1253(19)30189-X. Epub 2019 Jul 9. PubMed PMID: 31300360.

5: Fan B, Mellinghoff IK, Wen PY, Lowery MA, Goyal L, Tap WD, Pandya SS, Manyak E, Jiang L, Liu G, Nimkar T, Gliser C, Prahl Judge M, Agresta S, Yang H, Dai D. Clinical pharmacokinetics and pharmacodynamics of ivosidenib, an oral, targeted inhibitor of mutant IDH1, in patients with advanced solid tumors. Invest New Drugs. 2019 Apr 26. doi: 10.1007/s10637-019-00771-x. [Epub ahead of print] PubMed PMID: 31028664.

6: Dai D, Yang H, Nabhan S, Liu H, Hickman D, Liu G, Zacher J, Vutikullird A, Prakash C, Agresta S, Bowden C, Fan B. Effect of itraconazole, food, and ethnic origin on the pharmacokinetics of ivosidenib in healthy subjects. Eur J Clin Pharmacol. 2019 Aug;75(8):1099-1108. doi: 10.1007/s00228-019-02673-6. Epub 2019 Apr 23. PubMed PMID: 31011758.

7: Dittakavi S, Jat RK, Mullangi R. Quantitation of Ivosidenib, A Novel Mutant IDH1 Inhibitoron Mice DBS: Application to a Pharmacokinetic Study. Drug Res (Stuttg). 2019 Sep;69(9):505-511. doi: 10.1055/a-0857-6591. Epub 2019 Mar 1. PubMed PMID: 30822797.

8: Prakash C, Fan B, Altaf S, Agresta S, Liu H, Yang H. Pharmacokinetics, absorption, metabolism, and excretion of [(14)C]ivosidenib (AG-120) in healthy male subjects. Cancer Chemother Pharmacol. 2019 May;83(5):837-848. doi: 10.1007/s00280-019-03793-7. Epub 2019 Feb 13. PubMed PMID: 30758648.

9: Norsworthy KJ, Luo L, Hsu V, Gudi R, Dorff SE, Przepiorka D, Deisseroth A, Shen YL, Sheth CM, Charlab R, Williams GM, Goldberg KB, Farrell AT, Pazdur R. FDA Approval Summary: Ivosidenib for Relapsed or Refractory Acute Myeloid Leukemia with an Isocitrate Dehydrogenase-1 Mutation. Clin Cancer Res. 2019 Jun 1;25(11):3205-3209. doi: 10.1158/1078-0432.CCR-18-3749. Epub 2019 Jan 28. PubMed PMID: 30692099.

10: Nassereddine S, Lap CJ, Tabbara IA. Evaluating ivosidenib for the treatment of relapsed/refractory AML: design, development, and place in therapy. Onco Targets Ther. 2018 Dec 28;12:303-308. doi: 10.2147/OTT.S182443. eCollection 2019. Review. PubMed PMID: 30643428; PubMed Central PMCID: PMC6314316.

11: Dhillon S. Correction to: Ivosidenib: First Global Approval. Drugs. 2019 Jan;79(1):107. doi: 10.1007/s40265-018-1050-z. PubMed PMID: 30610623; PubMed Central PMCID: PMC6338699.

12: Yun S, Vincelette ND. Ivosidenib in IDH1-Mutated Acute Myeloid Leukemia. N Engl J Med. 2018 Sep 20;379(12):1186. doi: 10.1056/NEJMc1809507. PubMed PMID: 30260155.

13: Sahin I. Ivosidenib in IDH1-Mutated Acute Myeloid Leukemia. N Engl J Med. 2018 Sep 20;379(12):1186. doi: 10.1056/NEJMc1809507. PubMed PMID: 30260154.

14: DiNardo CD. Ivosidenib in IDH1-Mutated Acute Myeloid Leukemia. N Engl J Med. 2018 Sep 20;379(12):1186. doi: 10.1056/NEJMc1809507. PubMed PMID: 30231226.

15: Drugs and Lactation Database (LactMed) [Internet]. Bethesda (MD): National Library of Medicine (US); 2006-. Available from http://www.ncbi.nlm.nih.gov/books/NBK525498/ PubMed PMID: 30222290.

16: Dhillon S. Ivosidenib: First Global Approval. Drugs. 2018 Sep;78(14):1509-1516. doi: 10.1007/s40265-018-0978-3. Review. Erratum in: Drugs. 2019 Jan;79(1):107. PubMed PMID: 30209701; PubMed Central PMCID: PMC6315051.

17: Ivosidenib Gets Go-Ahead for AML. Cancer Discov. 2018 Sep;8(9):OF3. doi: 10.1158/2159-8290.CD-NB2018-107. Epub 2018 Aug 9. PubMed PMID: 30093505.

18: Ivosidenib Deemed Safe, Effective in AML. Cancer Discov. 2018 Aug;8(8):OF1. doi: 10.1158/2159-8290.CD-NB2018-082. Epub 2018 Jun 22. PubMed PMID: 29934313.

19: Sidaway P. Ivosidenib effective in IDH1-mutant AML. Nat Rev Clin Oncol. 2018 Aug;15(8):472. doi: 10.1038/s41571-018-0057-4. PubMed PMID: 29925981.

20: DiNardo CD, Stein EM, de Botton S, Roboz GJ, Altman JK, Mims AS, Swords R, Collins RH, Mannis GN, Pollyea DA, Donnellan W, Fathi AT, Pigneux A, Erba HP, Prince GT, Stein AS, Uy GL, Foran JM, Traer E, Stuart RK, Arellano ML, Slack JL, Sekeres MA, Willekens C, Choe S, Wang H, Zhang V, Yen KE, Kapsalis SM, Yang H, Dai D, Fan B, Goldwasser M, Liu H, Agresta S, Wu B, Attar EC, Tallman MS, Stone RM, Kantarjian HM. Durable Remissions with Ivosidenib in IDH1-Mutated Relapsed or Refractory AML. N Engl J Med. 2018 Jun 21;378(25):2386-2398. doi: 10.1056/NEJMoa1716984. Epub 2018 Jun 2. PubMed PMID: 29860938.



Additional Information

AC120 and Ivosidenib have the same molecule formula and molecule weight.
Ivosidenib has CAS#1448347-49-6, is a S,S-isomer.
AC120 has CAS#1448346-63-1, is a racemic.