Midostaurin
featured

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

MedKoo CAT#: 201850

CAS#: 120685-11-2

Description: Midostaurin, also known as PKC-412, PKC-412A and CGP 41251; is a synthetic indolocarbazole multikinase inhibitor with potential antiangiogenic and antineoplastic activities. Midostaurin inhibits protein kinase C alpha (PKCalpha), vascular endothelial growth factor receptor 2 (VEGFR2), c-kit, platelet-derived growth factor receptor (PDGFR) and FMS-like tyrosine kinase 3 (FLT3) tyrosine kinases, which may result in disruption of the cell cycle, inhibition of proliferation, apoptosis, and inhibition of angiogenesis in susceptible tumors. Midostaurin was approved in 2017.


Chemical Structure

img
Midostaurin
CAS# 120685-11-2

Theoretical Analysis

MedKoo Cat#: 201850
Name: Midostaurin
CAS#: 120685-11-2
Chemical Formula: C35H30N4O4
Exact Mass: 570.22671
Molecular Weight: 570.6371
Elemental Analysis: C, 73.67; H, 5.30; N, 9.82; O, 11.22

Price and Availability

Size Price Availability Quantity
10.0mg USD 190.0 Same day
25.0mg USD 350.0 Same day
50.0mg USD 550.0 Same day
100.0mg USD 950.0 Same day
200.0mg USD 1650.0 Same day
500.0mg USD 3250.0 Same day
1.0g USD 4650.0 2 Weeks
2.0g USD 7650.0 2 Weeks
Click to view more sizes and prices
Bulk inquiry

Synonym: PKC-412; PKC412; PKC 412; PKC412A; PKC-412A; PKC 412A; CGP41251; CGP 41251; CGP-41251; Midostaurin; Rydapt

IUPAC/Chemical Name: N-((5R,7R,8R,9S)-8-methoxy-9-methyl-16-oxo-6,7,8,9,15,16-hexahydro-5H,14H-17-oxa-4b,9a,15-triaza-5,9-methanodibenzo[b,h]cyclonona[jkl]cyclopenta[e]-as-indacen-7-yl)-N-methylbenzamide

InChi Key: BMGQWWVMWDBQGC-IIFHNQTCSA-N

InChi Code: InChI=1S/C35H30N4O4/c1-35-32(42-3)25(37(2)34(41)19-11-5-4-6-12-19)17-26(43-35)38-23-15-9-7-13-20(23)28-29-22(18-36-33(29)40)27-21-14-8-10-16-24(21)39(35)31(27)30(28)38/h4-16,25-26,32H,17-18H2,1-3H3,(H,36,40)/t25-,26-,32-,35+/m1/s1

SMILES Code: C[C@@]12[C@H](OC)[C@H](N(C(C3=CC=CC=C3)=O)C)C[C@H](N4C5=CC=CC=C5C6=C7C(CNC7=O)=C8C9=CC=CC=C9N2C8=C64)O1

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 soluble in water.

Shelf Life: >5 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 570.6371 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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

1: Wang ES. Beyond midostaurin: Which are the most promising FLT3 inhibitors in AML? Best Pract Res Clin Haematol. 2019 Dec;32(4):101103. doi: 10.1016/j.beha.2019.101103. Epub 2019 Oct 18. Review. PubMed PMID: 31779982.

2: 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/NBK548874/ PubMed PMID: 31644181.

3: Midostaurin for acute myeloid leukaemia, mastocytosis, and mast cell leukaemia. Aust Prescr. 2019 Apr;42(2):73-74. doi: 10.18773/austprescr.2019.017. Epub 2019 Feb 28. Review. PubMed PMID: 31048943; PubMed Central PMCID: PMC6478956.

4: Sly N, Gaspar K. Midostaurin for the management of FLT3-mutated acute myeloid leukemia and advanced systemic mastocytosis. Am J Health Syst Pharm. 2019 Feb 9;76(5):268-274. doi: 10.1093/ajhp/zxy050. Review. PubMed PMID: 30753289.

5: Drugs and Lactation Database (LactMed) [Internet]. Bethesda (MD): National Library of Medicine (US); 2006-. Available from http://www.ncbi.nlm.nih.gov/books/NBK500909/ PubMed PMID: 29999968.

6: Stone RM, Manley PW, Larson RA, Capdeville R. Midostaurin: its odyssey from discovery to approval for treating acute myeloid leukemia and advanced systemic mastocytosis. Blood Adv. 2018 Feb 27;2(4):444-453. doi: 10.1182/bloodadvances.2017011080. Review. Erratum in: Blood Adv. 2018 Apr 10;2(7):787. PubMed PMID: 29487059; PubMed Central PMCID: PMC5858474.

7: Weisberg E, Sattler M, Manley PW, Griffin JD. Spotlight on midostaurin in the treatment of FLT3-mutated acute myeloid leukemia and systemic mastocytosis: design, development, and potential place in therapy. Onco Targets Ther. 2017 Dec 29;11:175-182. doi: 10.2147/OTT.S127679. eCollection 2018. Review. PubMed PMID: 29343975; PubMed Central PMCID: PMC5749544.

8: Garcia JS, Percival ME. Midostaurin for the treatment of adult patients with newly diagnosed acute myeloid leukemia that is FLT3 mutation-positive. Drugs Today (Barc). 2017 Oct;53(10):531-543. doi: 10.1358/dot.2017.53.10.2717625. Review. PubMed PMID: 29286055.

9: Kim M, Williams S. Midostaurin in Combination With Standard Chemotherapy for Treatment of Newly Diagnosed FMS-Like Tyrosine Kinase 3 (FLT3) Mutation-Positive Acute Myeloid Leukemia. Ann Pharmacother. 2018 Apr;52(4):364-369. doi: 10.1177/1060028017747900. Epub 2017 Dec 12. Review. PubMed PMID: 29231051.

10: Luskin MR, DeAngelo DJ. Midostaurin/PKC412 for the treatment of newly diagnosed FLT3 mutation-positive acute myeloid leukemia. Expert Rev Hematol. 2017 Dec;10(12):1033-1045. doi: 10.1080/17474086.2017.1397510. Epub 2017 Oct 30. Review. PubMed PMID: 29069942.

11: Gallogly MM, Lazarus HM, Cooper BW. Midostaurin: a novel therapeutic agent for patients with FLT3-mutated acute myeloid leukemia and systemic mastocytosis. Ther Adv Hematol. 2017 Sep;8(9):245-261. doi: 10.1177/2040620717721459. Epub 2017 Aug 19. Review. PubMed PMID: 29051803; PubMed Central PMCID: PMC5639976.

12: Wei AH, Tiong IS. Midostaurin, enasidenib, CPX-351, gemtuzumab ozogamicin, and venetoclax bring new hope to AML. Blood. 2017 Dec 7;130(23):2469-2474. doi: 10.1182/blood-2017-08-784066. Epub 2017 Oct 19. Review. PubMed PMID: 29051180.

13: Stansfield LC, Pollyea DA. Midostaurin: A New Oral Agent Targeting FMS-Like Tyrosine Kinase 3-Mutant Acute Myeloid Leukemia. Pharmacotherapy. 2017 Dec;37(12):1586-1599. doi: 10.1002/phar.2039. Epub 2017 Nov 23. Review. PubMed PMID: 28976600.

14: Kayser S, Levis MJ, Schlenk RF. Midostaurin treatment in FLT3-mutated acute myeloid leukemia and systemic mastocytosis. Expert Rev Clin Pharmacol. 2017 Nov;10(11):1177-1189. doi: 10.1080/17512433.2017.1387051. Epub 2017 Oct 10. Review. PubMed PMID: 28960095.

15: Valent P, Akin C, Hartmann K, George TI, Sotlar K, Peter B, Gleixner KV, Blatt K, Sperr WR, Manley PW, Hermine O, Kluin-Nelemans HC, Arock M, Horny HP, Reiter A, Gotlib J. Midostaurin: a magic bullet that blocks mast cell expansion and activation. Ann Oncol. 2017 Oct 1;28(10):2367-2376. doi: 10.1093/annonc/mdx290. Review. PubMed PMID: 28945834.

16: Kim ES. Midostaurin: First Global Approval. Drugs. 2017 Jul;77(11):1251-1259. doi: 10.1007/s40265-017-0779-0. Review. PubMed PMID: 28612232.

17: Patnaik MM. Midostaurin for the treatment of acute myeloid leukemia. Future Oncol. 2017 Sep;13(21):1853-1871. doi: 10.2217/fon-2017-0160. Epub 2017 Jun 14. Review. PubMed PMID: 28610444.

18: Levis M. Midostaurin approved for FLT3-mutated AML. Blood. 2017 Jun 29;129(26):3403-3406. doi: 10.1182/blood-2017-05-782292. Epub 2017 May 25. Review. PubMed PMID: 28546144.

19: Chandesris MO, Damaj G, Lortholary O, Hermine O. Clinical potential of midostaurin in advanced systemic mastocytosis. Blood Lymphat Cancer. 2017 May 3;7:25-35. doi: 10.2147/BLCTT.S87186. eCollection 2017. Review. PubMed PMID: 31360083; PubMed Central PMCID: PMC6467340.

20: Tvedt TH, Nepstad I, Bruserud Ø. Antileukemic effects of midostaurin in acute myeloid leukemia - the possible importance of multikinase inhibition in leukemic as well as nonleukemic stromal cells. Expert Opin Investig Drugs. 2017 Mar;26(3):343-355. doi: 10.1080/13543784.2017.1275564. Epub 2016 Dec 28. Review. PubMed PMID: 28001095.



Additional Information