CWI1-2 is an IGF2BP2 inhibitor that binds IGF2BP2 and inhibits its interaction with m6A-modified target transcripts. It can cause apoptosis and differentiation, and shows good anti-leukemia effects.

Physicochemical Properties

Molecular Formula	C22H17CL3N6O3
Molecular Weight	519.77
Exact Mass	518.042
CAS #	2408590-36-1
Related CAS #	CWI1-2 hydrochloride;2408590-37-2
PubChem CID	155905758
Appearance	Light yellow to yellow solid powder
LogP	5.4
Hydrogen Bond Donor Count	5
Hydrogen Bond Acceptor Count	7
Rotatable Bond Count	8
Heavy Atom Count	34
Complexity	715
Defined Atom Stereocenter Count	0
SMILES	C1=CC(=C(C=C1Cl)/C=N/NC(=N/N=C/C2=C(C=CC(=C2)Cl)O)N/N=C\C3=C(C=CC(=C3)Cl)O)O
InChi Key	ZNYMTTHEJHXHNS-FGORHZQOSA-N
InChi Code	InChI=1S/C22H17Cl3N6O3/c23-16-1-4-19(32)13(7-16)10-26-29-22(30-27-11-14-8-17(24)2-5-20(14)33)31-28-12-15-9-18(25)3-6-21(15)34/h1-12,32-34H,(H2,29,30,31)/b26-10-,27-11+,28-12+
Chemical Name	1-[(Z)-(5-chloro-2-hydroxyphenyl)methylideneamino]-2,3-bis[(E)-(5-chloro-2-hydroxyphenyl)methylideneamino]guanidine
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro	CWI1-2 (0-1 μM, 24 h) exhibits good anti-leukemia efficacy [1].
ln Vivo	In BMT receptor B6.SJL (CD45.1) mice, CWI1-2 (5 mg/kg, iv, once daily, 7–10 days) can greatly postpone the onset and survival duration of leukemia without having a significant effect on body weight [1].
Cell Assay	Apoptosis Analysis[1] Cell Types: MonoMac6, MOLM13 Tested Concentrations: 0-1 μM Incubation Duration: 24 h Experimental Results: Induced significant cell differentiation and apoptosis in a concentration-dependent manner in IGF2BP2-high cells but not in IGF2BP2-low cells. decreased Gln uptake and impaired mitochondrial function, resulting in decreased ATP production in AML cells. Dramatically inhibited the colony-forming ability of MA9-induced leukemic mouse blasts and greatly impairs the self-renewal of LSC/LIC.
Toxicity/Toxicokinetics	Effects During Pregnancy and Lactation ◉ Summary of Use during Lactation No information is available on the clinical use of polatuzumab vedotin during breastfeeding. Because polatuzumab is a large protein molecule with a molecular weight of about 150,000 Da, the amount in milk is likely to be very low. It is also likely to be partially destroyed in the infant's gastrointestinal tract and absorption by the infant is probably minimal. Vedotin (monomethyl auristatin E) is a small-molecule anticancer drug that might enter milk and be absorbed by the infant. Because of the potential for serious adverse reactions in the breastfed infant, the manufacturer recommends that breastfeeding be discontinued during enfortumab vedotin therapy and for 2 months after the last dose. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date.
References	[1]. The m6A reader IGF2BP2 regulates glutamine metabolism and represents a therapeutic target in acute myeloid leukemia. Cancer Cell. 2022 Dec 12;40(12):1566-1582.e10.
Additional Infomation	See also: Polatuzumab Vedotin (annotation moved to).

Solubility Data

Solubility (In Vitro)

DMSO : 100 mg/mL (192.39 mM)

Solubility (In Vivo)

Solubility in Formulation 1: 1.25 mg/mL (2.40 mM) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	1.9239 mL	9.6196 mL	19.2393 mL
	5 mM	0.3848 mL	1.9239 mL	3.8479 mL
	10 mM	0.1924 mL	0.9620 mL	1.9239 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.