DT-061

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

MedKoo CAT#: 407947

CAS#: 1809427-19-7

Description: DT-061, also known as SMAP, is a potent and orally active activator of PP2A. Treatment with DT-061, in combination with the MEK inhibitor AZD6244, resulted in suppression of both p-AKT and MYC, as well as tumor regression in two KRAS-driven lung cancer mouse models. DT-061 therapy also abrogated MYC-driven tumorigenesis.

Chemical Structure

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DT-061
CAS# 1809427-19-7
Instruction

Theoretical Analysis

MedKoo Cat#: 407947
Name: DT-061
CAS#: 1809427-19-7
Chemical Formula: C25H23F3N2O5S
Exact Mass: 520.13
Molecular Weight: 520.523
Elemental Analysis: C, 57.69; H, 4.45; F, 10.95; N, 5.38; O, 15.37; S, 6.16

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
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Related CAS #: 1809427-18-6 (SSR isomer)   1809427-19-7    

Synonym: DT-061; DT061; DT 061; SMAP.

IUPAC/Chemical Name: N-((1R,2R,3S)-2-hydroxy-3-(10H-phenoxazin-10-yl)cyclohexyl)-4-(trifluoromethoxy)benzenesulfonamide

InChi Key: WGKGADVPRVLHHZ-ZHRMCQFGSA-N

InChi Code: InChI=1S/C25H23F3N2O5S/c26-25(27,28)35-16-12-14-17(15-13-16)36(32,33)29-18-6-5-9-21(24(18)31)30-19-7-1-3-10-22(19)34-23-11-4-2-8-20(23)30/h1-4,7-8,10-15,18,21,24,29,31H,5-6,9H2/t18-,21+,24+/m1/s1

SMILES Code: O=S(C1=CC=C(OC(F)(F)F)C=C1)(N[C@H]2[C@H](O)[C@@H](N3C4=C(C=CC=C4)OC5=CC=CC=C35)CCC2)=O

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: >3 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: 2934.99.03.00

More Info: Kinase inhibitor resistance constitutes a major unresolved clinical challenge in cancer. Furthermore, the role of serine/threonine phosphatase deregulation as a potential cause for resistance to kinase inhibitors has not been thoroughly addressed. PP2A activity modulation alters cancer cell sensitivities to a large number of kinase inhibitors. Specifically, PP2A inhibition ablated mitogen-activated protein kinase kinase (MEK) inhibitor response through the collateral activation of AKT/mammalian target of rapamycin (mTOR) signaling. Combination of mTOR and MEK inhibitors induced cytotoxicity in PP2A-inhibited cells, but even this drug combination could not abrogate MYC up-regulation in PP2A-inhibited cells.

Biological target:
In vitro activity:
In vivo activity:

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
Soluble in DMSO 0.0 100.00

Preparing Stock Solutions

The following data is based on the product molecular weight 520.52 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:
In vitro protocol:
In vivo protocol:

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1: Westermarck J. Targeted therapies don't work for a reason; the neglected tumor
suppressor phosphatase PP2A strikes back. FEBS J. 2018 Jul 28. doi:
10.1111/febs.14617. [Epub ahead of print] PubMed PMID: 30055114.


2: Kauko O, O'Connor CM, Kulesskiy E, Sangodkar J, Aakula A, Izadmehr S, Yetukuri
L, Yadav B, Padzik A, Laajala TD, Haapaniemi P, Momeny M, Varila T, Ohlmeyer M,
Aittokallio T, Wennerberg K, Narla G, Westermarck J. PP2A inhibition is a
druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells.
Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. doi:
10.1126/scitranslmed.aaq1093. PubMed PMID: 30021885.