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MedKoo Cat#: 122718 | Name: AK-2292

Description:

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

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

AK-2292
AK-2292
CAS#2984506-77-4

Theoretical Analysis

MedKoo Cat#: 122718

Name: AK-2292

CAS#: 2984506-77-4

Chemical Formula: C52H54F2N7O10PS2

Exact Mass: 1069.3100

Molecular Weight: 1070.13

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 currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
No Data
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

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
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.