WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H406777
CAS#: 1956343-52-4
Description: TM608 is a potent and selectiv c-MET inhibitor which targets Mitochondrial and Kills Erlotinib-Resistant Lung Cancer Cells. TM608 is the first TPP-TKI conjugate, can rapidly accumulates in mitochondria and suppresses the activation of MET in high MET expressing, erlotinib-resistant HCC827B cells (total cell lysates and mitochondrial fractions). TM608 was as potent and apoptogenic as PHA665752 in abrogating NSCLC cell viability. Directed accessibility to the mitochondria as afforded by a targeting moiety like TPP could conceivably compensate for deficient activity if uptake is rapid, cumulative, and selective.
Hodoodo Cat#: H406777
Name: TM608
CAS#: 1956343-52-4
Chemical Formula: C43H37BrCl2N3O4PS
Exact Mass: 0.00
Molecular Weight: 873.624
Elemental Analysis: C, 59.12; H, 4.27; Br, 9.15; Cl, 8.12; N, 4.81; O, 7.33; P, 3.55; S, 3.67
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Synonym: TM608; TM-608; TM 608.
IUPAC/Chemical Name: (Z)-(2-(5-((5-((2,6-dichlorobenzyl)sulfonyl)-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamido)ethyl)triphenylphosphonium bromide
InChi Key: ZVAUXGZLUPOFNR-UHFFFAOYSA-N
InChi Code: InChI=1S/C43H36Cl2N3O4PS.BrH/c1-28-40(26-35-34-25-33(21-22-39(34)48-42(35)49)54(51,52)27-36-37(44)19-12-20-38(36)45)47-29(2)41(28)43(50)46-23-24-53(30-13-6-3-7-14-30,31-15-8-4-9-16-31)32-17-10-5-11-18-32;/h3-22,25-26H,23-24,27H2,1-2H3,(H2-,46,47,48,49,50);1H
SMILES Code: O=C1NC2=C(C=C(S(=O)(CC3=C(Cl)C=CC=C3Cl)=O)C=C2)/C1=C/C4=C(C)C(C(NCC[P+](C5=CC=CC=C5)(C6=CC=CC=C6)C7=CC=CC=C7)=O)=C(C)N4.[Br-]
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
More Info: Related CAS# 1956343-52-4 (TM608 bromide) 1956343-51-3 (TM608 cation)
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 873.62 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: |
Mitochondrial-Targeting MET Kinase Inhibitor Kills Erlotinib-Resistant Lung Cancer Cells
Tianming Yang, Wai Har Ng, Huan Chen, Kamon Chomchopbun, The Hung Huynh, Mei Lin Go, and Oi Lian Kon
Publication Date (Web): June 23, 2016 (Letter)
DOI: 10.1021/acsmedchemlett.6b00223