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MedKoo Cat#: 407859 | Name: CRT0066854 HCl
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Description:

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

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
CRT0066854 HCl
CAS#2250019-91-9 (HCl)

Theoretical Analysis

MedKoo Cat#: 407859

Name: CRT0066854 HCl

CAS#: 2250019-91-9 (HCl)

Chemical Formula: C24H27Cl2N5S

Exact Mass: 0.0000

Molecular Weight: 488.48

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 600.00 2 Weeks
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Related CAS #
1438881-19-6 (free base) 2250019-91-9 (HCl)
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.

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.

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: 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.