CRT-0066854 HCl | PKCι and PKCζ inhibitor

CRT0066854 HCl
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 407859

CAS#: 1438881-19-6 (free base)

Description: CRT-0066854 is a PKCι and PKCζ inhibitor. CRT0066854, was able to restore polarized morphogenesis in the dysplastic H-Ras spheroids. These results show that tightly regulated PKCι is required for normal-polarized morphogenesis in mammalian cells and that H-Ras and ErbB2 cooperate with PKCι for loss of polarization and dysplasia. The identification of a PKCι inhibitor that can restore polarized morphogenesis has implications for the treatment of Ras and ErbB2 driven malignancies.

Chemical Structure

CRT0066854 HCl

CAS# 1438881-19-6 (free base)

Instruction

Theoretical Analysis

MedKoo Cat#: 407859
Name: CRT0066854 HCl
CAS#: 1438881-19-6 (free base)
Chemical Formula: C24H27Cl2N5S
Exact Mass: 0.00
Molecular Weight: 488.475
Elemental Analysis: C, 59.01; H, 5.57; Cl, 14.51; N, 14.34; S, 6.56

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 500	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Related CAS #: 1438881-19-6 (free base),

Synonym: CRT0066854; CRT-0066854; CRT 0066854; CRT-0066854 HCl

IUPAC/Chemical Name: (2S)-3-Phenyl-N1-[5,6,7,8-tetrahydro-2-(4-pyridinyl)[1]benzothieno[2,3-d]pyrimidin-4-yl]-1,2-propanediamine dihydrochloride

InChi Key: NYUVOWXZRBZQBA-NTEVMMBTSA-N

InChi Code: InChI=1S/C24H25N5S.2ClH/c25-18(14-16-6-2-1-3-7-16)15-27-23-21-19-8-4-5-9-20(19)30-24(21)29-22(28-23)17-10-12-26-13-11-17;;/h1-3,6-7,10-13,18H,4-5,8-9,14-15,25H2,(H,27,28,29);2*1H/t18-;;/m0../s1

SMILES Code: N[C@@H](CC1=CC=CC=C1)CNC2=C(C3=C(CCCC3)S4)C4=NC(C5=CC=NC=C5)=N2.[H]Cl.[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

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: The aPKC [atypical PKC (protein kinase C)] isoforms ι and ζ play crucial roles in the formation and maintenance of cell polarity and represent attractive anti-oncogenic drug targets in Ras-dependent tumours.

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 488.48 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.

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:

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1: Linch M, Sanz-Garcia M, Rosse C, Riou P, Peel N, Madsen CD, Sahai E, Downward
J, Khwaja A, Dillon C, Roffey J, Cameron AJ, Parker PJ. Regulation of polarized
morphogenesis by protein kinase C iota in oncogenic epithelial spheroids.
Carcinogenesis. 2014 Feb;35(2):396-406. doi: 10.1093/carcin/bgt313. Epub 2013 Sep
26. PubMed PMID: 24072773; PubMed Central PMCID: PMC3908745.

2: Kjær S, Linch M, Purkiss A, Kostelecky B, Knowles PP, Rosse C, Riou P, Soudy
C, Kaye S, Patel B, Soriano E, Murray-Rust J, Barton C, Dillon C, Roffey J,
Parker PJ, McDonald NQ. Adenosine-binding motif mimicry and cellular effects of a
thieno[2,3-d]pyrimidine-based chemical inhibitor of atypical protein kinase C
isoenzymes. Biochem J. 2013 Apr 15;451(2):329-42. doi: 10.1042/BJ20121871. PubMed
PMID: 23418854.

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CRT0066854 HCl featured