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MedKoo Cat#: 207008 | Name: Olutasidenib
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Olutasidenib, also known as FT-2102, is a potent, selective inhibitor of mutant Isocitrate dehydrogenase (IDH) for the treatment of acute myeloid leukemia. FT-2102 has excellent ADME/PK properties and reduces 2-hydroxyglutarate levels in an mIDH1 xenograft tumor model.

Chemical Structure

Olutasidenib
Olutasidenib
CAS#1887014-12-1

Theoretical Analysis

MedKoo Cat#: 207008

Name: Olutasidenib

CAS#: 1887014-12-1

Chemical Formula: C18H15ClN4O2

Exact Mass: 354.0884

Molecular Weight: 354.79

Elemental Analysis: C, 60.94; H, 4.26; Cl, 9.99; N, 15.79; O, 9.02

Price and Availability

Size Price Availability Quantity
10mg USD 250.00 2 Weeks
25mg USD 450.00 2 Weeks
50mg USD 750.00 2 Weeks
100mg USD 1,350.00 2 Weeks
200mg USD 2,350.00 2 Weeks
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Synonym
Olutasidenib; FT-2102; FT 2102; FT2102;
IUPAC/Chemical Name
5-[[(1S)-1-(6-Chloro-2-oxo-1,2-dihydroquinolin-3-yl)ethyl]amino]-1-methyl-6-oxo-1,6-dihydropyridine-2-carbonitrile
InChi Key
NEQYWYXGTJDAKR-JTQLQIEISA-N
InChi Code
InChI=1S/C18H15ClN4O2/c1-10(21-16-6-4-13(9-20)23(2)18(16)25)14-8-11-7-12(19)3-5-15(11)22-17(14)24/h3-8,10,21H,1-2H3,(H,22,24)/t10-/m0/s1
SMILES Code
N#CC1=CC=C(N[C@H](C2=CC3=C(NC2=O)C=CC(Cl)=C3)C)C(N1C)=O
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
Shelf Life
>3 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
More Info
On Dec 1, 2022, FDA approved olutasidenib for relapsed or refractory acute myeloid leukemia with a susceptible IDH1 mutation
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Olutasidenib (FT-2102) is a highly potent, orally active, brain penetrant and selective inhibitor of mutant Isocitrate dehydrogenase 1 (IDH1), with IC50 values of 21.2 nM and 114 nM for IDH1- R132H and IDH1- R132C.
In vitro activity:
Here this study describes the structure-based design and optimization of quinoline lead compounds to identify FT-2102, a potent, orally bioavailable, brain penetrant, and selective mIDH1 inhibitor. FT-2102 has excellent ADME/PK properties and reduces 2-hydroxyglutarate levels in an mIDH1 xenograft tumor model. Reference: J Med Chem. 2020 Feb 27;63(4):1612-1623. https://pubmed.ncbi.nlm.nih.gov/31971798/
In vivo activity:
Here this study describes the structure-based design and optimization of quinoline lead compounds to identify FT-2102, a potent, orally bioavailable, brain penetrant, and selective mIDH1 inhibitor. FT-2102 has excellent ADME/PK properties and reduces 2-hydroxyglutarate levels in an mIDH1 xenograft tumor model. Reference: J Med Chem. 2020 Feb 27;63(4):1612-1623. https://pubmed.ncbi.nlm.nih.gov/31971798/
Solvent mg/mL mM
Solubility
DMSO 98.0 276.22
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 354.79 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
Formulation protocol:
Caravella JA, Lin J, Diebold RB, Campbell AM, Ericsson A, Gustafson G, Wang Z, Castro J, Clarke A, Gotur D, Josephine HR, Katz M, Kershaw M, Yao L, Toms AV, Barr KJ, Dinsmore CJ, Walker D, Ashwell S, Lu W. Structure-Based Design and Identification of FT-2102 (Olutasidenib), a Potent Mutant-Selective IDH1 Inhibitor. J Med Chem. 2020 Feb 27;63(4):1612-1623. doi: 10.1021/acs.jmedchem.9b01423. Epub 2020 Feb 12. PMID: 31971798.
In vitro protocol:
Caravella JA, Lin J, Diebold RB, Campbell AM, Ericsson A, Gustafson G, Wang Z, Castro J, Clarke A, Gotur D, Josephine HR, Katz M, Kershaw M, Yao L, Toms AV, Barr KJ, Dinsmore CJ, Walker D, Ashwell S, Lu W. Structure-Based Design and Identification of FT-2102 (Olutasidenib), a Potent Mutant-Selective IDH1 Inhibitor. J Med Chem. 2020 Feb 27;63(4):1612-1623. doi: 10.1021/acs.jmedchem.9b01423. Epub 2020 Feb 12. PMID: 31971798.
In vivo protocol:
Caravella JA, Lin J, Diebold RB, Campbell AM, Ericsson A, Gustafson G, Wang Z, Castro J, Clarke A, Gotur D, Josephine HR, Katz M, Kershaw M, Yao L, Toms AV, Barr KJ, Dinsmore CJ, Walker D, Ashwell S, Lu W. Structure-Based Design and Identification of FT-2102 (Olutasidenib), a Potent Mutant-Selective IDH1 Inhibitor. J Med Chem. 2020 Feb 27;63(4):1612-1623. doi: 10.1021/acs.jmedchem.9b01423. Epub 2020 Feb 12. PMID: 31971798.
1: Venugopal S, Sekeres MA. Contemporary Management of Acute Myeloid Leukemia: A Review. JAMA Oncol. 2024 Aug 8. doi: 10.1001/jamaoncol.2024.2662. Epub ahead of print. PMID: 39115831. 2: Ivanov S, Nano O, Hana C, Bonano-Rios A, Hussein A. Molecular Targeting of the Isocitrate Dehydrogenase Pathway and the Implications for Cancer Therapy. Int J Mol Sci. 2024 Jul 4;25(13):7337. doi: 10.3390/ijms25137337. PMID: 39000443; PMCID: PMC11242572. 3: Cortes JE. Olutasidenib: a novel mutant IDH1 inhibitor for the treatment of relapsed or refractory acute myeloid leukemia. Expert Rev Hematol. 2024 Jun;17(6):211-221. doi: 10.1080/17474086.2024.2354486. Epub 2024 May 21. PMID: 38747392. 4: Le RQ, Przepiorka D, Chen H, Shen YL, Pulte ED, Norsworthy K, Theoret MR, De Claro RA. Complete remission with partial hematological recovery as a palliative endpoint for treatment of acute myeloid leukemia. Blood. 2024 Jul 11;144(2):206-215. doi: 10.1182/blood.2023023313. PMID: 38728428. 5: Cortes J, Jonas BA, Schiller G, Mims A, Roboz GJ, Wei AH, Montesinos P, Ferrell PB, Yee KW, Fenaux P, Schwarer A, Watts JM. Olutasidenib in post- venetoclax patients with mutant isocitrate dehydrogenase 1 (mIDH1) acute myeloid leukemia (AML). Leuk Lymphoma. 2024 Aug;65(8):1145-1152. doi: 10.1080/10428194.2024.2333451. Epub 2024 Mar 27. PMID: 38538632. 6: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012–. Olutasidenib. 2024 Feb 20. PMID: 38386942. 7: Venugopal S, Shallis RM, Zeidan AM. Oral therapy for myelodysplastic syndromes/neoplasms and acute myeloid leukemia: a revolution in progress. Expert Rev Anticancer Ther. 2023 Jul-Dec;23(9):903-911. doi: 10.1080/14737140.2023.2238897. Epub 2023 Jul 20. PMID: 37470508. 8: Sangwan K, Sharma V, Goyal PK. Pharmacological Profile of Novel Anti-cancer Drugs Approved by USFDA in 2022: A Review. Curr Mol Med. 2024;24(6):734-750. doi: 10.2174/1566524023666230622151034. PMID: 37350009. 9: Patel SA. Precision and strategic targeting of novel mutation-specific vulnerabilities in acute myeloid leukemia: the semi-centennial of 7 + 3. Leuk Lymphoma. 2023 Sep;64(9):1503-1513. doi: 10.1080/10428194.2023.2224473. Epub 2023 Jun 16. PMID: 37328939; PMCID: PMC10913147. 10: Venugopal S, Watts J. Olutasidenib: from bench to bedside. Blood Adv. 2023 Aug 22;7(16):4358-4365. doi: 10.1182/bloodadvances.2023009854. PMID: 37196640; PMCID: PMC10432604. 11: Olutasidenib (Rezlidhia) for acute myeloid leukemia. Med Lett Drugs Ther. 2023 Apr 3;65(1673):e58-e59. doi: 10.58347/tml.2023.1673e. PMID: 37020343. 12: Kang C. Olutasidenib: First Approval. Drugs. 2023 Mar;83(4):341-346. doi: 10.1007/s40265-023-01844-1. PMID: 36848032. 13: Olutasidenib. Am J Health Syst Pharm. 2023 Mar 21;80(7):398-400. doi: 10.1093/ajhp/zxad002. PMID: 36779331. 14: de Botton S, Fenaux P, Yee K, Récher C, Wei AH, Montesinos P, Taussig DC, Pigneux A, Braun T, Curti A, Grove C, Jonas BA, Khwaja A, Legrand O, Peterlin P, Arnan M, Blum W, Cilloni D, Hiwase DK, Jurcic JG, Krauter J, Thomas X, Watts JM, Yang J, Polyanskaya O, Brevard J, Sweeney J, Barrett E, Cortes J. Olutasidenib (FT-2102) induces durable complete remissions in patients with relapsed or refractory IDH1-mutated AML. Blood Adv. 2023 Jul 11;7(13):3117-3127. doi: 10.1182/bloodadvances.2022009411. PMID: 36724515; PMCID: PMC10362540. 15: Drugs and Lactation Database (LactMed®) [Internet]. Bethesda (MD): National Institute of Child Health and Human Development; 2006–. Olutasidenib. 2023 Jan 15. PMID: 36701506. 16: Watts JM, Baer MR, Yang J, Prebet T, Lee S, Schiller GJ, Dinner SN, Pigneux A, Montesinos P, Wang ES, Seiter KP, Wei AH, De Botton S, Arnan M, Donnellan W, Schwarer AP, Récher C, Jonas BA, Ferrell PB Jr, Marzac C, Kelly P, Sweeney J, Forsyth S, Guichard SM, Brevard J, Henrick P, Mohamed H, Cortes JE. Olutasidenib alone or with azacitidine in IDH1-mutated acute myeloid leukaemia and myelodysplastic syndrome: phase 1 results of a phase 1/2 trial. Lancet Haematol. 2023 Jan;10(1):e46-e58. doi: 10.1016/S2352-3026(22)00292-7. Epub 2022 Nov 10. Erratum in: Lancet Haematol. 2023 Jan;10(1):e9. doi: 10.1016/S2352-3026(22)00381-7. PMID: 36370742. 17: Weber V, Arnaud L, Dukic-Stefanovic S, Wenzel B, Roux V, Chezal JM, Lai TH, Teodoro R, Kopka K, Miot-Noirault E, Deuther-Conrad W, Maisonial-Besset A. Novel Radioiodinated and Radiofluorinated Analogues of FT-2102 for SPECT or PET Imaging of mIDH1 Mutant Tumours. Molecules. 2022 Jun 11;27(12):3766. doi: 10.3390/molecules27123766. PMID: 35744895; PMCID: PMC9228733. 18: de la Fuente MI, Colman H, Rosenthal M, Van Tine BA, Levacic D, Walbert T, Gan HK, Vieito M, Milhem MM, Lipford K, Forsyth S, Guichard SM, Mikhailov Y, Sedkov A, Brevard J, Kelly PF, Mohamed H, Monga V. Olutasidenib (FT-2102) in patients with relapsed or refractory IDH1-mutant glioma: A multicenter, open- label, phase Ib/II trial. Neuro Oncol. 2023 Jan 5;25(1):146-156. doi: 10.1093/neuonc/noac139. PMID: 35639513; PMCID: PMC9825299. 19: Maschmeyer G, Bullinger L, Garcia-Vidal C, Herbrecht R, Maertens J, Menna P, Pagano L, Thiebaut-Bertrand A, Calandra T. Infectious complications of targeted drugs and biotherapies in acute leukemia. Clinical practice guidelines by the European Conference on Infections in Leukemia (ECIL), a joint venture of the European Group for Blood and Marrow Transplantation (EBMT), the European Organization for Research and Treatment of Cancer (EORTC), the International Immunocompromised Host Society (ICHS) and the European Leukemia Net (ELN). Leukemia. 2022 May;36(5):1215-1226. doi: 10.1038/s41375-022-01556-7. Epub 2022 Apr 2. Erratum in: Leukemia. 2022 May;36(5):1450. doi: 10.1038/s41375-022-01570-9. PMID: 35368047; PMCID: PMC9061290. 20: Rizzo A, Ricci AD, Brandi G. IDH inhibitors in advanced cholangiocarcinoma: Another arrow in the quiver? Cancer Treat Res Commun. 2021;27:100356. doi: 10.1016/j.ctarc.2021.100356. Epub 2021 Mar 24. PMID: 33799004.

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