MA242 TFA

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MedKoo CAT#: 407937

CAS#: 1049704-18-8 (TFA)

Description: MA242 is a Dual Inhibitors of MDM2 and NFAT1 for Pancreatic Cancer Therapy. MA242 decreased cell proliferation and induced apoptosis in pancreatic cancer cell lines regardless of p53 status. MA242 alone or in combination with gemcitabine inhibited pancreatic tumor growth and metastasis without any host toxicity. Our data indicate that targeting both MDM2 and NFAT1 represents a novel and effective strategy to treat pancreatic cancer.

Chemical Structure

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MA242 TFA
CAS# 1049704-18-8 (TFA)
Instruction

Theoretical Analysis

MedKoo Cat#: 407937
Name: MA242 TFA
CAS#: 1049704-18-8 (TFA)
Chemical Formula: C26H21ClF3N3O5S
Exact Mass: 0.00
Molecular Weight: 579.975
Elemental Analysis: C, 53.84; H, 3.65; Cl, 6.11; F, 9.83; N, 7.25; O, 13.79; S, 5.53

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.
Note: Price will be listed if it is available in the future.

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Related CAS #: 1049704-18-8 (TFA)   1049704-17-7 (free base)    

Synonym: MA242 TFA; MA242; MA-242; MA 242;

IUPAC/Chemical Name: 7-((4-chlorobenzyl)amino)-1-tosyl-3,4-dihydropyrrolo[4,3,2-de]quinolin-8(1H)-one 2,2,2-trifluoroacetate

InChi Key: YTSFRIUMZUCDMV-UHFFFAOYSA-N

InChi Code: InChI=1S/C24H20ClN3O3S.C2HF3O2/c1-15-2-8-19(9-3-15)32(30,31)28-14-17-10-11-26-20-12-21(24(29)23(28)22(17)20)27-13-16-4-6-18(25)7-5-16;3-2(4,5)1(6)7/h2-9,12,14,27H,10-11,13H2,1H3;(H,6,7)

SMILES Code: O=C1C2=C3C(CCN=C3C=C1NCC4=CC=C(Cl)C=C4)=CN2S(=O)(C5=CC=C(C)C=C5)=O.O=C(O)C(F)(F)F

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: 2934.99.9001

More Info: Overexpression and activation of the murine double minute 2 (MDM2) or nuclear factor of activated T cells 1 (NFAT1) oncoproteins frequently occur in pancreatic cancer. Most MDM2 inhibitors under development target MDM2-p53 binding and have little or no effect on cancers without functional p53, including pancreatic cancer. Some available compounds indirectly inhibit NFAT1 activity by interfering with calcineurin activity, but there are currently no specific inhibitors

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 579.98 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: Wang W, Qin JJ, Voruganti S, Nijampatnam B, Velu SE, Ruan KH, Hu M, Zhou J,
Zhang R. Discovery and Characterization of Dual Inhibitors of MDM2 and NFAT1 for
Pancreatic Cancer Therapy. Cancer Res. 2018 Oct 1;78(19):5656-5667. doi:
10.1158/0008-5472.CAN-17-3939. Epub 2018 Sep 14. PubMed PMID: 30217928.