Description
(R)-CCG-1423 is a stereoisomer of CCG-1423. CCG-1423 is a Rho inhibitor involved in blocking signaling through myocardin-related transcription factor A (MRTF-A) and serum response factor (SRF) . The Rho family of small GTPases plays an important role in cancer metastasis. Up-regulation of RhoA or RhoC has been associated with a poor clinical outcome. Rho GTPases are important for the actin cytoskeleton. The RhoA family plays an important role in multiple cellular processes central to tumor growth and metastasis . CCG-14223 was an inhibitor for Rho/SRF pathway and displayed activity in several in vitro cancer cell functional assays. In PC-3 prostate cancer cells, CCG-1423(< 1 μmol/L) potently inhibited lysophosphatidic acid–induced DNA synthesis. CCG-1423 inhibited the growth of RhoC-overexpressing melanoma lines (A375M2 and SK-Mel-147) at nanomolar concentrations. CCG-1423 selectively stimulated apoptosis of the metastasis-prone, RhoC-overexpressing melanoma cell line (A375M2) when compared with the parental cell line (A375). CCG-1423 inhibited Rho-dependent invasion by PC-3 prostate cancer cells . The R-isomer of CCG-1423 inhibited MRTF-A-dependent cellular events, including SRF-mediated gene expression and cell migration. The efficacy of (R)-CCG-1423 was less potent than the S-isomer .
Product information
Molecular Weight: 454.75
Formula: C18H13ClF6N2O3
Chemical Name: (2R)-2-({[3,5-bis(trifluoromethyl)phenyl]formamido}oxy)-N-(4-chlorophenyl)propanamide
Smiles: C[C@@H](ONC(=O)C1C=C(C=C(C=1)C(F)(F)F)C(F)(F)F)C(=O)NC1C=CC(Cl)=CC=1
InChiKey: DSMXVSGJIDFLKP-SECBINFHSA-N
InChi: InChI=1S/C18H13ClF6N2O3/c1-9(15(28)26-14-4-2-13(19)3-5-14)30-27-16(29)10-6-11(17(20,21)22)8-12(7-10)18(23,24)25/h2-9H,1H3,(H,26,28)(H,27,29)/t9-/m1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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