Deltarasin |CAS 1440898-61-2|DC Chemicals

Cas No.:	1440898-61-2
Chemical Name:	Deltarasin
Synonyms:	Deltarasin;1H-Benzimidazole, 2-[4-[(2S)-2-(2-phenyl-1H-benzimidazol-1-yl)-2-(4-piperidinyl)ethoxy]phenyl]-1-(phenylmethyl)-;C40H37N5O;BCP20971;2363AH;BDBM50019865;s7224;SB19574;SW219816-1;A13722;1-benzyl-2-{4-[(2S)-2-(2-phenyl-1H-1,3-benzodiazol-1-yl)-2-(piperidin-4-yl)ethoxy]phenyl}-1H-1,3-benzodiazole
SMILES:	O(C1C([H])=C([H])C(C2=NC3=C([H])C([H])=C([H])C([H])=C3N2C([H])([H])C2C([H])=C([H])C([H])=C([H])C=2[H])=C([H])C=1[H])C([H])([H])[C@]([H])(C1([H])C([H])([H])C([H])([H])N([H])C([H])([H])C1([H])[H])N1C(C2C([H])=C([H])C([H])=C([H])C=2[H])=NC2=C([H])C([H])=C([H])C([H])=C12
Formula:	C₄₀H₃₇N₅O
M.Wt:	603.7547
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

Deltarasin is a novel and small molecule inhibitor which can inhibit the KRAS-PDEδ interaction(Kd= 41 nM. binding to PDEδ) and impairs oncogenic KRAS signalling.Interfering with binding of mammalian PDEδ to KRAS by means of small molecules provides a novel opportunity to suppress oncogenic RAS signalling by altering its localization to endomembranes. Biochemical screening and subsequent structure-based hit optimization yielded inhibitors of the KRAS-PDEδ interaction that selectively bind to the prenyl-binding pocket of PDEδ with nanomolar affinity, inhibit oncogenic RAS signalling and suppress in vitro and in vivo proliferation of human pancreatic ductal adenocarcinoma cells that are dependent on oncogenic KRAS. For the detailed information of Deltarasin, the solubility of Deltarasin in water, the solubility of Deltarasin in DMSO, the solubility of Deltarasin in PBS buffer, the animal experiment (test) of Deltarasin, the cell expriment (test) of Deltarasin, the in vivo, in vitro and clinical trial test of Deltarasin, the EC50, IC50,and affinity,of Deltarasin, For the detailed information of Deltarasin, the solubility of Deltarasin in water, the solubility of Deltarasin in DMSO, the solubility of Deltarasin in PBS buffer, the animal experiment (test) of Deltarasin, the cell expriment (test) of Deltarasin, the in vivo, in vitro and clinical trial test of Deltarasin, the EC50, IC50,and affinity,of Deltarasin, Please contact DC Chemicals.

MSDS

COA

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2018-0101

Cat. No.	Product name	Field of application
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DC73763	CC-11050	Dovramilast (CC-11050) is a potent and orally active phosphodiesterase 4 (PDE4) inhibitor, CC-11050 is a promising candidate for host directed therapy of patients with pulmonary TB.
DC71683	Lodenafil	Lodenafil (Hydroxyhomosildenafil) is a potent phosphodiesterase type 5 (PDE5) inhibitor for the treatment of erectile dysfunction (ED).
DC70239	BAY 2666605	BAY2666605 is a potent, small molecule PDE3A-SLFN12 complex inducer with EC50 of 7 nM.BAY2666605 triggers the formation of a complex of two proteins called SLFN12 and PDE3A. This complex drive cancer cells into cell death by a mechanism called apoptosis.
DC48226	ONO-8430506	ONO-8430506 is an orally bioavailable and potent autotaxin (ATX)/ENPP2 inhibitor with the IC90 of 100 nM for ATX activity in mouse plasma.
DC42521	MBCQ	MBCQ is a potent and selective the type V phosphodiesterase (PDE V; PDE5) inhibitor with an IC50 of 19 nM. MBCQ has IC50s >100 µM for PDE1, PDE2, PDE3, and PDE4, respectively. MBCQ dilates coronary arteries via potent and specific inhibition of cGMP-PDE.
DC40977	DSR-141562	DSR-141562 is a novel, orally active, and selective brain-penetrant phosphodiesterase 1 (PDE1) inhibitor. DSR-141562 shows preferential selectivity for human PDE1B with an IC50 of 43.9 nM, and the IC50 values for human PDE1A and 1C are 97.6 and 431.8 nM, respectively. DSR-141562 can be used for the study of positive symptoms, negative symptoms and cognitive impairments associated with schizophrenia.
DC40378	MR-L2	MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4), activates representative PDE4 long-isoform variants (PDE4A4, PDE4B1, PDE4C3, PDE4D5). MR-L2 suppresses PGE2-induced MDCK cell cyst formation with an EC50 of 1.2 μM.
DC28378	THPP-1	THPP-1, a SGC chemical probe, is a potent and orally bioavailable phosphodiesterase 10A (PDE10A) inhibitor, with Ki values of 1 nM and 1.3 nM for human and rat PDE10A, respectively. THPP-1 has excellent pharmacokinetic properties in preclinical species.
DC28354	(E/Z)HA-155	(E/Z)HA-155 is a potent and selective autotaxin (ATX) inhibitor with an IC50 of 5.7 nM.