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My CartCAS：1642300-52-4
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 1642300-52-4 |
| Name | Eltanexor |
| Molecular Formula | C17H10F6N6O |
| Molecular Weight | 428.29 |
| Solubility | Soluble in DMSO ≥5mg/mL |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD30489739 |
| SMILES | C1=C(C=C(C=C1C(F)(F)F)C(F)(F)F)C2=NN(C=N2)C=C(C3=CN=CN=C3)C(=O)N |
| InChIKey | JFBAVWVBLRIWHM-AWNIVKPZSA-N |
| InChI | InChI=1S/C17H10F6N6O/c18-16(19，20)11-1-9(2-12(3-11)17(21，22)23)15-27-8-29(28-15)6-13(14(24)30)10-4-25-7-26-5-10/h1-8H，(H2，24，30)/b13-6+ |
| PubChem CID | 86345880 |
| Target Point | CRM1 |
| Passage | Membrane Transporter&Ion Channel |
| Background | It is an oral bioactive inhibitor of XPO1 (exportin 1, CRM1), which inhibits XPO1-dependent nuclear output by directly targeting XPO1, showing strong anti-leukemia activity. |
| Biological Activity | Eltanexor 是具有口服生物活性的XPO1 (CRM1)抑制剂。在AML细胞系，IC50范围为20-211 nM。[1-2] |
| In Vitro | Eltanexor与selinexor表现出相似的体外药效，但eltanexor对中枢神经系统穿透力较低，因此耐受性更强，即使每日给药也是如此，而且与 selinexor 相比，eltanexor在 CLL 和 AML 小鼠模型中的存活率也有所提高。KPT-8602 的治疗窗口期更宽，还可以提高靶向疗效，从而与其他靶向抗癌疗法进行更有效的联合治疗。[2] |
| In Vivo | 由于Eltanexor 的耐受性更好，因此Eltanexor可以每天给药，而且在急性髓细胞性白血病患者衍生的异种移植模型中，Eltanexor对白血病细胞和 LICs 都有更好的抗白血病疗效。重要的是，Eltanexor不会显著降低正常造血干细胞和祖细胞(HSPC)的频率，从而为消除导致复发的LIC提供了治疗窗口，同时保护了正常的HSPC。[1] |
| Data Literature Source | [1]. Etchin J，et al. KPT-8602，a second-generation inhibitor of XPO1-mediated nuclear export，is well tolerated and highly active against AML blasts and leukemia-initiating cells. Leukemia. 2017 Jan;31(1): 143-150. [2]. Hing ZA，et al. Next-generation XPO1 inhibitor shows improved efficacy and in vivo tolerability in hematological malignancies. Leukemia. 2016 Dec;30(12): 2364-2372. |
| Unit | Bottle |
| Specification | 1mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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