MedKoo Cat#: 207143 | Name: IACS-13909
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Description:

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

IACS-13909 is a specific and potent allosteric inhibitor of SHP2 that suppresses the signaling of RTK/MAPK pathway and overcomes multiple mechanisms underlying osimertinib resistance. IACS-13909 potently impedes the proliferation of tumors with a broad spectrum of RTKs as the oncogenic driver. Importantly, in NSCLC models with acquired resistance to osimertinib, IACS-13909 administered as a single agent or in combination with osimertinib potently reduces tumor cell proliferation in vitro and in vivo. Together, our findings provide preclinical evidence for using a SHP2 inhibitor as a therapeutic strategy in acquired EGFR inhibitor-resistant NSCLC.

Chemical Structure

 IACS-13909
IACS-13909
CAS#2160546-07-4

Theoretical Analysis

MedKoo Cat#: 207143

Name: IACS-13909

CAS#: 2160546-07-4

Chemical Formula: C17H18Cl2N6

Exact Mass: 376.0970

Molecular Weight: 377.27

Elemental Analysis: C, 54.12; H, 4.81; Cl, 18.79; N, 22.28

Price and Availability

Size Price Availability Quantity
50mg USD 550.00 2 Weeks
100mg USD 950.00 2 Weeks
200mg USD 1,650.00 2 Weeks
500mg USD 3,250.00 2 Weeks
1g USD 4,650.00 2 Weeks
2g USD 7,650.00 2 Weeks
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Synonym
IACS-13909; IACS 13909; IACS13909; BBP-398; BBP 398; BBP398;
IUPAC/Chemical Name
1-(3-(2,3-dichlorophenyl)-1H-pyrazolo[3,4-b]pyrazin-6-yl)-4-methylpiperidin-4-amine
InChi Key
AMADCPJVPLUGQO-UHFFFAOYSA-N
InChi Code
InChI=1S/C17H18Cl2N6/c1-17(20)5-7-25(8-6-17)12-9-21-15-14(23-24-16(15)22-12)10-3-2-4-11(18)13(10)19/h2-4,9H,5-8,20H2,1H3,(H,22,23,24)
SMILES Code
ClC1=CC=CC(C2=NNC3=C2N=CC(N4CCC(C)(N)CC4)=N3)=C1Cl
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

Preparing Stock Solutions

The following data is based on the product molecular weight 377.27 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: Sun Y, Meyers BA, Czako B, Leonard P, Mseeh F, Harris AL, Wu Q, Johnson S, Parker CA, Cross JB, Di Francesco ME, Bivona BJ, Bristow CA, Burke JP, Carrillo CC, Carroll CL, Chang Q, Feng N, Gao G, Gera S, Giuliani V, Huang JK, Jiang Y, Kang Z, Kovacs JJ, Liu CY, Lopez AM, Ma X, Mandal PK, McAfoos T, Miller MA, Mullinax RA, Peoples M, Ramamoorthy V, Seth S, Spencer ND, Suzuki E, Williams CC, Yu SS, Zuniga AM, Draetta GF, Marszalek JR, Heffernan TP, Kohl NE, Jones P. Allosteric SHP2 Inhibitor, IACS-13909, Overcomes EGFR-Dependent and EGFR- Independent Resistance Mechanisms toward Osimertinib. Cancer Res. 2020 Nov 1;80(21):4840-4853. doi: 10.1158/0008-5472.CAN-20-1634. Epub 2020 Sep 14. PMID: 32928921; PMCID: PMC11106563. 2: Larson KC, Martens LH, Marconi M, Dejesus C, Bruhn S, Miller TA, Tate B, Levenson JM. Preclinical translational platform of neuroinflammatory disease biology relevant to neurodegenerative disease. J Neuroinflammation. 2024 Jan 31;21(1):37. doi: 10.1186/s12974-024-03029-3. PMID: 38297405; PMCID: PMC10832185. 3: Chen M, Wang H, Shi S, Zhang H, Xu S, Jiang Y. miR-6071 inhibits hepatocellular carcinoma progression via targeting PTPN11. Arch Biochem Biophys. 2022 Sep 30;727:109345. doi: 10.1016/j.abb.2022.109345. Epub 2022 Jul 2. PMID: 35792156. 4: Xu WQ, Qi SZ, Zhao JF, Li LP, Ding CH, Liu WS. Discovery of 1H-pyrazolo[3,4-b]pyrazine derivatives as selective allosteric inhibitor of protein tyrosine phosphatase SHP2 for the treatment of KRASG12C-mutant non-small cell lung cancer. J Biomol Struct Dyn. 2024 Jan 23:1-9. doi: 10.1080/07391102.2024.2308771. Epub ahead of print. PMID: 38258435.