MDK5466
featured

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

Hodoodo CAT#: H563024

CAS#: 852045-46-6

Description: MDK5466, also known as Flt3 Inhibitor III, is a Flt3 inhibitor that acts by preventing glutamate-induced cell death. MDK5466 has CAS#852045-46-6. For the convenience of scientific communication, we temporally name it as MDK5466. The last four digit of the CAS# was used in the name.

Chemical Structure

img
MDK5466
CAS# 852045-46-6
Instruction

Theoretical Analysis

Hodoodo Cat#: H563024
Name: MDK5466
CAS#: 852045-46-6
Chemical Formula: C21H23N3OS
Exact Mass: 365.16
Molecular Weight: 365.490
Elemental Analysis: C, 69.01; H, 6.34; N, 11.50; O, 4.38; S, 8.77

Price and Availability

Size Price Availability Quantity
5mg USD 450 Back order
Bulk inquiry

Synonym: Flt3 Inhibitor III; E21; Flt3-IN-III; MDK5466; MDK-5466; MDK 5466;

IUPAC/Chemical Name: (5-Phenyl-thiazol-2-yl)-(4-(2-pyrrolidin-1-yl-ethoxy)-phenyl)-amine

InChi Key: FNZTULJDGIXMJJ-UHFFFAOYSA-N

InChi Code: InChI=1S/C21H23N3OS/c1-2-6-17(7-3-1)20-16-22-21(26-20)23-18-8-10-19(11-9-18)25-15-14-24-12-4-5-13-24/h1-3,6-11,16H,4-5,12-15H2,(H,22,23)

SMILES Code: C1(NC2=NC=C(C3=CC=CC=C3)S2)=CC=C(OCCN4CCCC4)C=C1

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: >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

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 365.49 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:
In vitro protocol:
In vivo protocol:

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: Cortes J, Perl AE, Döhner H, Kantarjian H, Martinelli G, Kovacsovics T, Rousselot P, Steffen B, Dombret H, Estey E, Strickland S, Altman JK, Baldus CD, Burnett A, Krämer A, Russell N, Shah NP, Smith CC, Wang ES, Ifrah N, Gammon G, Trone D, Lazzaretto D, Levis M. Quizartinib, an FLT3 inhibitor, as monotherapy in patients with relapsed or refractory acute myeloid leukaemia: an open-label, multicentre, single-arm, phase 2 trial. Lancet Oncol. 2018 May 30. pii: S1470-2045(18)30240-7. doi: 10.1016/S1470-2045(18)30240-7. [Epub ahead of print] PubMed PMID: 29859851.

2: Al-Fayoumi S, Hashiguchi T, Shirakata Y, Mascarenhas J, Singer JW. Pilot study of the antifibrotic effects of the multikinase inhibitor pacritinib in a mouse model of liver fibrosis. J Exp Pharmacol. 2018 May 9;10:9-17. doi: 10.2147/JEP.S150729. eCollection 2018. PubMed PMID: 29785143; PubMed Central PMCID: PMC5953271.

3: Osanto S, van der Hulle T. Cabozantinib in the treatment of advanced renal cell carcinoma in adults following prior vascular endothelial growth factor targeted therapy: clinical trial evidence and experience. Ther Adv Urol. 2018 Jan 9;10(3):109-123. doi: 10.1177/1756287217748867. eCollection 2018 Mar. Review. PubMed PMID: 29662541; PubMed Central PMCID: PMC5896860.

4: Gorcea CM, Burthem J, Tholouli E. ASP2215 in the treatment of relapsed/refractory acute myeloid leukemia with FLT3 mutation: background and design of the ADMIRAL trial. Future Oncol. 2018 Mar 2. doi: 10.2217/fon-2017-0582. [Epub ahead of print] PubMed PMID: 29498296.

5: Jetani H, Garcia-Cadenas I, Nerreter T, Thomas S, Rydzek J, Meijide JB, Bonig H, Herr W, Sierra J, Einsele H, Hudecek M. CAR T-cells targeting FLT3 have potent activity against FLT3(-)ITD(+) AML and act synergistically with the FLT3-inhibitor crenolanib. Leukemia. 2018 May;32(5):1168-1179. doi: 10.1038/s41375-018-0009-0. Epub 2018 Feb 5. PubMed PMID: 29472720.

6: Mathew NR, Baumgartner F, Braun L, O'Sullivan D, Thomas S, Waterhouse M, Müller TA, Hanke K, Taromi S, Apostolova P, Illert AL, Melchinger W, Duquesne S, Schmitt-Graeff A, Osswald L, Yan KL, Weber A, Tugues S, Spath S, Pfeifer D, Follo M, Claus R, Lübbert M, Rummelt C, Bertz H, Wäsch R, Haag J, Schmidts A, Schultheiss M, Bettinger D, Thimme R, Ullrich E, Tanriver Y, Vuong GL, Arnold R, Hemmati P, Wolf D, Ditschkowski M, Jilg C, Wilhelm K, Leiber C, Gerull S, Halter J, Lengerke C, Pabst T, Schroeder T, Kobbe G, Rösler W, Doostkam S, Meckel S, Stabla K, Metzelder SK, Halbach S, Brummer T, Hu Z, Dengjel J, Hackanson B, Schmid C, Holtick U, Scheid C, Spyridonidis A, Stölzel F, Ordemann R, Müller LP, Sicre-de-Fontbrune F, Ihorst G, Kuball J, Ehlert JE, Feger D, Wagner EM, Cahn JY, Schnell J, Kuchenbauer F, Bunjes D, Chakraverty R, Richardson S, Gill S, Kröger N, Ayuk F, Vago L, Ciceri F, Müller AM, Kondo T, Teshima T, Klaeger S, Kuster B, Kim DDH, Weisdorf D, van der Velden W, Dörfel D, Bethge W, Hilgendorf I, Hochhaus A, Andrieux G, Börries M, Busch H, Magenau J, Reddy P, Labopin M, Antin JH, Henden AS, Hill GR, Kennedy GA, Bar M, Sarma A, McLornan D, Mufti G, Oran B, Rezvani K, Shah O, Negrin RS, Nagler A, Prinz M, Burchert A, Neubauer A, Beelen D, Mackensen A, von Bubnoff N, Herr W, Becher B, Socié G, Caligiuri MA, Ruggiero E, Bonini C, Häcker G, Duyster J, Finke J, Pearce E, Blazar BR, Zeiser R. Sorafenib promotes graft-versus-leukemia activity in mice and humans through IL-15 production in FLT3-ITD-mutant leukemia cells. Nat Med. 2018 Mar;24(3):282-291. doi: 10.1038/nm.4484. Epub 2018 Feb 12. Erratum in: Nat Med. 2018 Apr 10;24(4):526. PubMed PMID: 29431743.

7: Garz AK, Wolf S, Grath S, Gaidzik V, Habringer S, Vick B, Rudelius M, Ziegenhain C, Herold S, Weickert MT, Smets M, Peschel C, Oostendorp RAJ, Bultmann S, Jeremias I, Thiede C, Döhner K, Keller U, Götze KS. Azacitidine combined with the selective FLT3 kinase inhibitor crenolanib disrupts stromal protection and inhibits expansion of residual leukemia-initiating cells in FLT3-ITD AML with concurrent epigenetic mutations. Oncotarget. 2017 Oct 16;8(65):108738-108759. doi: 10.18632/oncotarget.21877. eCollection 2017 Dec 12. PubMed PMID: 29312564; PubMed Central PMCID: PMC5752477.

8: Lange A, Jaskula E, Lange J, Dworacki G, Nowak D, Simiczyjew A, Mordak-Domagala M, Sedzimirska M. The sorafenib anti-relapse effect after alloHSCT is associated with heightened alloreactivity and accumulation of CD8+PD-1+ (CD279+) lymphocytes in marrow. PLoS One. 2018 Jan 5;13(1):e0190525. doi: 10.1371/journal.pone.0190525. eCollection 2018. PubMed PMID: 29304116; PubMed Central PMCID: PMC5755786.

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. PubMed PMID: 29231051.

10: Li J, Kumar P, Anreddy N, Zhang YK, Wang YJ, Chen Y, Talele TT, Gupta K, Trombetta LD, Chen ZS. Quizartinib (AC220) reverses ABCG2-mediated multidrug resistance: In vitro and in vivo studies. Oncotarget. 2017 Sep 16;8(55):93785-93799. doi: 10.18632/oncotarget.21078. eCollection 2017 Nov 7. PubMed PMID: 29212189; PubMed Central PMCID: PMC5706835.

11: Kampa-Schittenhelm KM, Frey J, Haeusser LA, Illing B, Pavlovsky AA, Blumenstock G, Schittenhelm MM. Crenolanib is a type I tyrosine kinase inhibitor that inhibits mutant KIT D816 isoforms prevalent in systemic mastocytosis and core binding factor leukemia. Oncotarget. 2017 Aug 7;8(47):82897-82909. doi: 10.18632/oncotarget.19970. eCollection 2017 Oct 10. PubMed PMID: 29137311; PubMed Central PMCID: PMC5669937.

12: 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. PubMed PMID: 29069942.

13: 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.

14: Ferrari SM, Centanni M, Virili C, Miccoli M, FerrariPaola P, Ruffilli I, Ragusa F, Antonelli A, Fallahi P. Sunitinib in the treatment of thyroid cancer. Curr Med Chem. 2017 Oct 6. doi: 10.2174/0929867324666171006165942. [Epub ahead of print] PubMed PMID: 28990511.

15: 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. PubMed PMID: 28976600.

16: Lan QY, Zhi YL, Heng H, Tian JY, Guo XX, Liu HC, Chen YD, Lu T, Lu S. Chemical Space of FLT3 Inhibitors as Potential Anti-AML Drugs. Recent Pat Anticancer Drug Discov. 2017 Nov 20;12(4):296-322. doi: 10.2174/1574892812666170727154643. PubMed PMID: 28748750.

17: B Peters ML, Miksad RA. Cabozantinib in the treatment of hepatocellular carcinoma. Future Oncol. 2017 Jul 13. doi: 10.2217/fon-2017-0169. [Epub ahead of print] PubMed PMID: 28703624.

18: Stone RM, Mandrekar SJ, Sanford BL, Laumann K, Geyer S, Bloomfield CD, Thiede C, Prior TW, Döhner K, Marcucci G, Lo-Coco F, Klisovic RB, Wei A, Sierra J, Sanz MA, Brandwein JM, de Witte T, Niederwieser D, Appelbaum FR, Medeiros BC, Tallman MS, Krauter J, Schlenk RF, Ganser A, Serve H, Ehninger G, Amadori S, Larson RA, Döhner H. Midostaurin plus Chemotherapy for Acute Myeloid Leukemia with a FLT3 Mutation. N Engl J Med. 2017 Aug 3;377(5):454-464. doi: 10.1056/NEJMoa1614359. Epub 2017 Jun 23. PubMed PMID: 28644114; PubMed Central PMCID: PMC5754190.

19: Peschel I, Podmirseg SR, Taschler M, Duyster J, Götze KS, Sill H, Nachbaur D, Jäkel H, Hengst L. FLT3 and FLT3-ITD phosphorylate and inactivate the cyclin-dependent kinase inhibitor p27(Kip1) in acute myeloid leukemia. Haematologica. 2017 Aug;102(8):1378-1389. doi: 10.3324/haematol.2016.160101. Epub 2017 May 18. PubMed PMID: 28522571; PubMed Central PMCID: PMC5541872.

20: Roolf C, Dybowski N, Sekora A, Mueller S, Knuebel G, Tebbe A, Murua Escobar H, Godl K, Junghanss C, Schaab C. Phosphoproteome Analysis Reveals Differential Mode of Action of Sorafenib in Wildtype and Mutated FLT3 Acute Myeloid Leukemia (AML) Cells. Mol Cell Proteomics. 2017 Jul;16(7):1365-1376. doi: 10.1074/mcp.M117.067462. Epub 2017 Apr 27. PubMed PMID: 28450419; PubMed Central PMCID: PMC5500767.