AK-2292

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Hodoodo CAT#: H122718

CAS#: N/A

Description: AK-2292 is a Potent and Selective STAT5 PROTAC Degrader with Strong Antitumor Activity In Vivo in Acute Myeloid Leukemia. AK-2292 effectively induces degradation of STAT5A, STAT5B, and phosphorylated STAT5 proteins in a concentration- and time-dependent manner in acute myeloid leukemia (AML) cell lines and demonstrates excellent degradation selectivity for STAT5 over all other STAT members. It exerts potent and specific cell growth inhibitory activity in AML cell lines with high levels of phosphorylated STAT5. AK-2292 effectively reduces STAT5 protein in vivo and achieves strong antitumor activity in mice at well-tolerated dose schedules.

Chemical Structure

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AK-2292
CAS# N/A
Instruction

Theoretical Analysis

Hodoodo Cat#: H122718
Name: AK-2292
CAS#: N/A
Chemical Formula: C52H54F2N7O10PS2
Exact Mass: 1,069.31
Molecular Weight: 1,070.130
Elemental Analysis: C, 58.36; H, 5.09; F, 3.55; N, 9.16; O, 14.95; P, 2.89; S, 5.99

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 @hodoodo.com or click below button.
Note: Price will be listed if it is available in the future.

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Synonym: AK2292; AK-2292; AK 2292

IUPAC/Chemical Name: ((2-(((2S)-1-((2S)-2-((3-((5-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)pent-4-yn-1-yl)(methyl)amino)-3-oxopropyl)(4-(thiazol-2-yl)phenyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)carbamoyl)benzo[b]thiophen-5-yl)difluoromethyl)phosphonic acid

InChi Key: LOPYPDQOHNOVBM-QOIUHGAOSA-N

InChi Code: InChI=1S/C52H54F2N7O10PS2/c1-51(2,3)44(57-46(65)41-29-33-28-34(16-20-40(33)74-41)52(53,54)72(69,70)71)50(68)60-25-9-13-39(60)49(67)59(35-17-14-32(15-18-35)47-55-23-27-73-47)26-22-43(63)58(4)24-7-5-6-10-31-11-8-12-36-37(31)30-61(48(36)66)38-19-21-42(62)56-45(38)64/h8,11-12,14-18,20,23,27-29,38-39,44H,5,7,9,13,19,21-22,24-26,30H2,1-4H3,(H,57,65)(H,56,62,64)(H2,69,70,71)/t38?,39-,44+/m0/s1

SMILES Code: FC(P(O)(O)=O)(F)C1=CC2=C(SC(C(N[C@@H](C(C)(C)C)C(N3CCC[C@H]3C(N(C4=CC=C(C5=NC=CS5)C=C4)CCC(N(C)CCCC#CC6=CC=CC7=C6CN(C8C(NC(CC8)=O)=O)C7=O)=O)=O)=O)=O)=C2)C=C1

Appearance: To be determined

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: To be determined

Shelf Life: >2 years if stored properly

Drug Formulation: To be determined

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:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 1,070.13 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: Kaneshige A, Bai L, Wang M, McEachern D, Meagher JL, Xu R, Wang Y, Jiang W,
Metwally H, Kirchhoff PD, Zhao L, Jiang H, Wang M, Wen B, Sun D, Stuckey JA,
Wang S. A selective small-molecule STAT5 PROTAC degrader capable of achieving
tumor regression in vivo. Nat Chem Biol. 2023 Feb 2. doi:
10.1038/s41589-022-01248-4. Epub ahead of print. PMID: 36732620.

2: Kaneshige A, Bai L, Wang M, McEachern D, Meagher JL, Xu R, Kirchhoff PD, Wen
B, Sun D, Stuckey JA, Wang S. Discovery of a Potent and Selective STAT5 PROTAC
Degrader with Strong Antitumor Activity In Vivo in Acute Myeloid
Leukemia. J Med Chem. 2023 Feb 3. doi: 10.1021/acs.jmedchem.2c01665. Epub ahead
of print. PMID: 36735833.