1. Cell Cycle/DNA Damage
  2. Topoisomerase

TAS-103 dihydrochloride (Synonyms: BMS-247615 dihydrochloride)

Cat. No.: HY-13758A Purity: 98.53%
Data Sheet SDS Handling Instructions

TAS-103 2Hcl(BMS-247615 2Hcl) is a dual inhibitor of topoisomerase-I (topo-I) and topoisomerase-II (topoII).

For research use only. We do not sell to patients.
TAS-103 dihydrochloride Chemical Structure

TAS-103 dihydrochloride Chemical Structure

CAS No. : 174634-09-4

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in Water USD 158 In-stock
5 mg USD 144 In-stock
10 mg USD 228 In-stock
50 mg USD 660 In-stock
100 mg USD 1140 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Other Forms of TAS-103 dihydrochloride:

  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

TAS-103 2Hcl(BMS-247615 2Hcl) is a dual inhibitor of topoisomerase-I (topo-I) and topoisomerase-II (topoII). IC50 value: Target: Topoisomerase in vitro: TAS-103 was effective in inhibiting in vitro proliferation of human SCLC (SBC-3 and H69) cells and their drug-resistant variants SBC-3/ADM or SBC-3/CDDP and H-69/VP, respectively. SBC-3/ADM and H-69/VP expressed high P-gp, whereas SBC-3/CDDP did not [1]. TAS-103 disrupts SRP complex formation and reduces the amount of SRP14 and SRP19. TAS-103 treatment and RNAi-mediated knockdown of SRP54 or SRP14 promoted accumulation of the exogenously expressed chimeric protein interleukin-6-FLAG inside cells [2]. In 13 human cancer cell lines, MGMT expression correlated with IC50 for TAS-103, whereas gamma-GCS expression inversely correlated with the IC50 value, suggesting MGMT may work to decrease TAS-103 activity but gamma-GCS may increase it [3]. in vivo: TAS-103 also effectively reduced the tumor growth (more than 50% inhibition) of the parental as well as MDR SCLC cells grown SC in nude mice [1]. Thirty-two patients were treated with escalating doses (50 to 200 mg/m(2)) of TAS-103, administered intravenously over 1 hour each week for 3 weeks. Pharmacokinetic analysis was performed at the 130-, 160-, and 200-mg/m(2) dose levels [4].

References
Molecular Weight

406.31

Formula

C₂₀H₂₁Cl₂N₃O₂

CAS No.

174634-09-4

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

H2O: 15.3 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 98.53%

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Product Name:
TAS-103 dihydrochloride
Cat. No.:
HY-13758A
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