MELK-T1 HCl

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MedKoo CAT#: 407209

CAS#: 1610536-69-0 (HCl)

Description: 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

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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

Size Price Shipping out time Quantity
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Pricing updated 2021-02-24. Prices are subject to change without notice.

MELK-T1 hydrochloride is not in stock, but may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.

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

Handling Instructions:

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.

Select a batch to recalculate based on the batch molecular weight:
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: 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.



Additional Information

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.