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MedKoo Cat#: 562908 | Name: KRCA-0008
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Description:

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

KRCA-0008 is a potent dual inhibitor of Ack1 and anaplastic lymphoma kinase (ALK).

Chemical Structure

KRCA-0008
KRCA-0008
CAS#1472795-20-2

Theoretical Analysis

MedKoo Cat#: 562908

Name: KRCA-0008

CAS#: 1472795-20-2

Chemical Formula: C30H37ClN8O4

Exact Mass: 608.2626

Molecular Weight: 609.13

Elemental Analysis: C, 59.16; H, 6.12; Cl, 5.82; N, 18.40; O, 10.51

Price and Availability

Size Price Availability Quantity
10mg USD 285.00 2 Weeks
25mg USD 550.00 2 Weeks
50mg USD 850.00 2 Weeks
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Related CAS #
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Synonym
KRCA-0008; KRCA 0008; KRCA0008;
IUPAC/Chemical Name
1,1'-[(5-Chloro-2,4-pyrimidinediyl)bis[imino(3-methoxy-4,1-phenylene)-4,1-piperazinediyl]]bisethanone
InChi Key
TXDIRJCYNAWBOS-UHFFFAOYSA-N
InChi Code
InChI=1S/C30H37ClN8O4/c1-20(40)36-9-13-38(14-10-36)22-5-7-25(27(17-22)42-3)33-29-24(31)19-32-30(35-29)34-26-8-6-23(18-28(26)43-4)39-15-11-37(12-16-39)21(2)41/h5-8,17-19H,9-16H2,1-4H3,(H2,32,33,34,35)
SMILES Code
ClC1=CN=C(NC2=CC=C(N3CCN(C(C)=O)CC3)C=C2OC)N=C1NC4=CC=C(N5CCN(C(C)=O)CC5)C=C4OC
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
Product Data
Product Data
Instruction
View handling instruction
Biological target:
KRCA-0008 is a selective ALK/Ack1 inhibitor with IC50s of 12 and 4 nM for ALK and Ack1, respectively.
In vitro activity:
KRCA-0008 strongly suppressed the proliferation and survival of NPM-ALK-positive ALCL cells. Additionally, it induced G0/G1 cell cycle arrest and apoptosis by blocking downstream signals including STAT3, Akt, and ERK1/2. Reference: Invest New Drugs. 2020 Oct;38(5):1282-1291. https://pubmed.ncbi.nlm.nih.gov/31956933/
In vivo activity:
KRCA-0008 demonstrates in vivo efficacy comparable to Crizotinib in xenograft mice model. Reference: Bioorg Med Chem Lett. 2013 Nov 15;23(22):6192-6. https://pubmed.ncbi.nlm.nih.gov/24095090/
Solvent mg/mL mM
Solubility
DMSO 145.5 238.79
Ethanol 60.9 100.00
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 609.13 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:
1. Hwang J, Song I, Lee K, Kim HR, Hong EH, Hwang JS, Ahn SH, Lee J. KRCA-0008 suppresses ALK-positive anaplastic large-cell lymphoma growth. Invest New Drugs. 2020 Oct;38(5):1282-1291. doi: 10.1007/s10637-020-00896-4. Epub 2020 Jan 20. PMID: 31956933. 2. Park CH, Choe H, Jang IY, Kwon SY, Latif M, Lee HK, Lee HJ, Yang EH, Yun JI, Chae CH, Cho SY, Choi SU, Ha JD, Jung H, Kim HR, Kim P, Lee CO, Yun CS, Lee K. Novel bis-ortho-alkoxy-para-piperazinesubstituted-2,4-dianilinopyrimidines (KRCA-0008) as potent and selective ALK inhibitors for anticancer treatment. Bioorg Med Chem Lett. 2013 Nov 15;23(22):6192-6. doi: 10.1016/j.bmcl.2013.08.090. Epub 2013 Sep 4. PMID: 24095090.
In vitro protocol:
1. Hwang J, Song I, Lee K, Kim HR, Hong EH, Hwang JS, Ahn SH, Lee J. KRCA-0008 suppresses ALK-positive anaplastic large-cell lymphoma growth. Invest New Drugs. 2020 Oct;38(5):1282-1291. doi: 10.1007/s10637-020-00896-4. Epub 2020 Jan 20. PMID: 31956933. 2. Park CH, Choe H, Jang IY, Kwon SY, Latif M, Lee HK, Lee HJ, Yang EH, Yun JI, Chae CH, Cho SY, Choi SU, Ha JD, Jung H, Kim HR, Kim P, Lee CO, Yun CS, Lee K. Novel bis-ortho-alkoxy-para-piperazinesubstituted-2,4-dianilinopyrimidines (KRCA-0008) as potent and selective ALK inhibitors for anticancer treatment. Bioorg Med Chem Lett. 2013 Nov 15;23(22):6192-6. doi: 10.1016/j.bmcl.2013.08.090. Epub 2013 Sep 4. PMID: 24095090.
In vivo protocol:
1. Hwang J, Song I, Lee K, Kim HR, Hong EH, Hwang JS, Ahn SH, Lee J. KRCA-0008 suppresses ALK-positive anaplastic large-cell lymphoma growth. Invest New Drugs. 2020 Oct;38(5):1282-1291. doi: 10.1007/s10637-020-00896-4. Epub 2020 Jan 20. PMID: 31956933. 2. Park CH, Choe H, Jang IY, Kwon SY, Latif M, Lee HK, Lee HJ, Yang EH, Yun JI, Chae CH, Cho SY, Choi SU, Ha JD, Jung H, Kim HR, Kim P, Lee CO, Yun CS, Lee K. Novel bis-ortho-alkoxy-para-piperazinesubstituted-2,4-dianilinopyrimidines (KRCA-0008) as potent and selective ALK inhibitors for anticancer treatment. Bioorg Med Chem Lett. 2013 Nov 15;23(22):6192-6. doi: 10.1016/j.bmcl.2013.08.090. Epub 2013 Sep 4. PMID: 24095090.
1: Kang CH, Yun JI, Lee K, Lee CO, Lee HK, Yun CS, Hwang JY, Cho SY, Jung H, Kim P, Ha JD, Jeon JH, Choi SU, Jeong HG, Kim HR, Park CH. Development of potent ALK inhibitor and its molecular inhibitory mechanism against NSCLC harboring EML4-ALK proteins. Biochem Biophys Res Commun. 2015 Aug 28;464(3):762-7. doi: 10.1016/j.bbrc.2015.07.027. Epub 2015 Jul 10. PubMed PMID: 26168728. 2: Lee HJ, Latif M, Choe H, Ali I, Lee HK, Yang EH, Yun JI, Chae CH, Jung JK, Kim HR, Lee CO, Park CH, Lee K. ALK inhibitors of bis-ortho-alkoxy-para-piperazinesubstituted-pyrimidines and -triazines for cancer treatment. Arch Pharm Res. 2014;37(9):1130-8. doi: 10.1007/s12272-013-0323-z. Epub 2014 Jan 21. PubMed PMID: 24446111. 3: Park CH, Choe H, Jang IY, Kwon SY, Latif M, Lee HK, Lee HJ, Yang EH, Yun JI, Chae CH, Cho SY, Choi SU, Ha JD, Jung H, Kim HR, Kim P, Lee CO, Yun CS, Lee K. Novel bis-ortho-alkoxy-para-piperazinesubstituted-2,4-dianilinopyrimidines (KRCA-0008) as potent and selective ALK inhibitors for anticancer treatment. Bioorg Med Chem Lett. 2013 Nov 15;23(22):6192-6. doi: 10.1016/j.bmcl.2013.08.090. Epub 2013 Sep 4. PubMed PMID: 24095090.