MedKoo Cat#: 407209 | Name: MELK-T1 HCl

Description:

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

MELK-T1 is a potent and selective inhibitor of protein kinase MELK. MELK-T1 decreases DNA-damage tolerance in proliferating cancer cells. MELK-T1 triggered a rapid and proteasome-dependent degradation of the MELK protein. Treatment of MCF-7 breast adenocarcinoma cells with MELK-T1 induced the accumulation of stalled replication forks and double-strand breaks that culminated in a replicative senescence phenotype. MELK-T1 induced a strong phosphorylation of p53, a prolonged upregulation of p21 and a downregulation of FOXM1 target genes.

Chemical Structure

MELK-T1 HCl
MELK-T1 HCl
CAS#1610536-69-0 (HCl)

Theoretical Analysis

MedKoo Cat#: 407209

Name: MELK-T1 HCl

CAS#: 1610536-69-0 (HCl)

Chemical Formula: C21H23ClN4O2

Exact Mass:

Molecular Weight: 398.89

Elemental Analysis: C, 63.23; H, 5.81; Cl, 8.89; N, 14.05; O, 8.02

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
1610536-69-0 (HCl) 1610586-62-3 (free base)
Synonym
MELK-T1; MELK-T 1; MELK-T-1; MELK-T1 HCl salt.
IUPAC/Chemical Name
2-methoxy-4-(1H-pyrazol-4-yl)-N-(2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-yl)benzamide hydrochloride
InChi Key
OXRWZUUCCUDKJJ-UHFFFAOYSA-N
InChi Code
InChI=1S/C21H22N4O2.ClH/c1-27-20-11-15(17-12-23-24-13-17)3-5-19(20)21(26)25-18-4-2-14-6-8-22-9-7-16(14)10-18;/h2-5,10-13,22H,6-9H2,1H3,(H,23,24)(H,25,26);1H
SMILES Code
O=C(NC1=CC=C2CCNCCC2=C1)C3=CC=C(C4=CNN=C4)C=C3OC.[H]Cl
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
More Info
Related CAS# 1610536-69-0 (HCl salt); 1610586-62-3 (free base) Maternal Embryonic Leucine Zipper Kinase (MELK), a Ser/Thr protein kinase, has oncogenic properties and is overexpressed in many cancer cells. The oncogenic function of MELK is attributed to its capacity to disable critical cell-cycle checkpoints and reduce replication stress. MELK is a key stimulator of proliferation by its ability to increase the threshold for DNA-damage tolerance.

Preparing Stock Solutions

The following data is based on the product molecular weight 398.89 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
1: Beke L, Kig C, Linders JT, Boens S, Boeckx A, Van Heerde E, Parade M, De Bondt A, Van Den Wyngaert I, Bashir T, Ogata S, Meerpoel L, Van Eynde A, Johnson CN, Beullens M, Brehmer D, Bollen M. MELK-T1, a small-molecule inhibitor of protein kinase MELK, decreases DNA-damage tolerance in proliferating cancer cells. Biosci Rep. 2015 Oct 2. pii: BSR20150194. [Epub ahead of print] PubMed PMID: 26431963.